Considérations générales sur les propriétés enzymologiques de la Caspase-2 ,
, Peptides aldéhydes -Inhibiteurs réversibles de première génération
,
Inhibiteurs irréversibles de seconde et troisième génération ,
, Présentation des molécules et hiérarchisation de l'effet
, Étude de l'effet des inhibiteurs sur un modèle d'apoptose dépendant de la Caspase-2 ... 216 4.1. Présentation du modèle HeLa -Vincristine
, Cytotoxicité des composés sur des neurones corticaux primaires
Effets croisés des inhibiteurs des premières générations sur les Cathepsines ,
, Quantification des paramètres cinétiques de l'inhibition et efficacité des composés, p.223
,
Cytotoxicité sur des cultures primaires de neurones du Cortex ,
,
Hiérarchisation de l'effet et mécanisme d'action ,
, Type d'inhibition et quantification des paramètres cinétiques
,
Évaluation de la toxicité de h33 sur culture primaire de neurones corticaux ,
234 1. Structure et quantification des premiers effets sur les Caspases-2 et -3 ,
,
, 239 2. Hiérarchisation de l'effet grâce aux données IC50
, Efficacités inhibitrices des composés LJ2a, LJ2b, LJ3a et LJ3b
, Sélectivité vis-à-vis des protéases concurrentes
A novel protease homolog differentially expressed in breast and ovarian cancer, Mol. Med, vol.2, pp.624-636, 1996. ,
The physiology and pathobiology of human kallikrein-related peptidase 6 (KLK6), Clin. Chem. Lab. Med, vol.50, pp.211-233, 2011. ,
Crystal structure and biochemical characterization of human kallikrein 6 reveals that a trypsin-like kallikrein is expressed in the central nervous system, J. Biol. Chem, vol.277, pp.24562-24570, 2002. ,
Non-combinatorial library screening reveals subsite cooperativity and identifies new high-efficiency substrates for kallikreinrelated peptidase 14, Biol. Chem, vol.393, pp.331-341, 2012. ,
Kinetics of allosteric activation, Methods Enzymol, vol.466, pp.259-271, 2009. ,
Serine proteases, IUBMB Life, vol.61, pp.510-515, 2009. ,
6-Substituted 2-oxo-2H-1-benzopyran-3-carboxylic acid as a core structure for specific inhibitors of human leukocyte elastase, J. Med. Chem, vol.42, pp.4161-4171, 1999. ,
The structure of human prokallikrein 6 reveals a novel activation mechanism for the kallikrein family, J. Biol. Chem, vol.277, pp.27273-27281, 2002. ,
An ensemble view of thrombin allostery, Biol. Chem, vol.393, pp.889-898, 2012. ,
Virtual screening and X-ray crystallography for human kallikrein 6 inhibitors with an amidinothiophene P1 group, ACS Med. Chem. Lett, vol.3, pp.159-164, 2012. ,
Zyme, a novel and potentially amyloidogenic enzyme cDNA isolated from Alzheimer's disease brain, J. Biol. Chem, vol.272, pp.25135-25142, 1997. ,
, , 2014.
, Isomannide-based peptidomimetics as inhibitors for human tissue kallikreins 5 and 7, ACS Med. Chem. Lett, vol.5, pp.128-132
Conformational selection in trypsin-like proteases, Curr. Opin. Struct. Biol, vol.22, pp.421-431, 2012. ,
Crystal structure of prothrombin reveals conformational flexibility and mechanism of activation, J. Biol. Chem, vol.288, pp.22734-22744, 2013. ,
Unleashing the therapeutic potential of human kallikrein-related serine proteases, Nat. Rev. Drug Discov, vol.14, pp.183-202, 2015. ,
Kallikrein-related peptidase 6, Handbook of Proteolytic Enzymes, pp.2778-2788, 2013. ,
Synthesis, biological evaluation, and docking studies of PAR2-AP-derived pseudopeptides as inhibitors of kallikrein 5 and 6, Biol. Chem, vol.396, pp.45-52, 2015. ,
Structurefunction analyses of human kallikrein-related peptidase 2 establish the 99-loop as master regulator of activity, J. Biol. Chem, vol.289, pp.34267-34283, 2014. ,
A review on pharmacological properties of coumarins, Mini Rev. Med. Chem, vol.18, pp.113-141, 2018. ,
Toward the first class of suicide inhibitors of kallikreins involved in skin diseases, J. Med. Chem, vol.58, pp.598-612, 2015. ,
URL : https://hal.archives-ouvertes.fr/hal-01543965
MolDock: a new technique for high-accuracy molecular docking, J. Med. Chem, vol.49, pp.3315-3321, 2006. ,
Trypsin and trypsin-like proteases in the brain: proteolysis and cellular functions, Cell Mol. Life Sci, vol.65, pp.237-252, 2008. ,
Molecular cloning of a novel brain-specific serine protease with a kringle-like structure and three scavenger receptor cysteine-rich motifs, Biochem. Biophys. Res. Commun, vol.239, pp.386-392, 1997. ,
Overview of the therapeutic potential of piplartine (piperlongumine), Eur. J. Pharmaceut. Sci, vol.48, pp.453-463, 2013. ,
Targeting antioxidants for cancer therapy, Biochem. Pharmacol, vol.92, pp.90-101, 2014. ,
Synthetic analogue of the natural product piperlongumine as a potent inhibitor of breast cancer cell line migration, J. Braz. Chem. Soc, vol.28, pp.475-484, 2017. ,
Selective killing of cancer cells by a small molecule targeting the stress response to ROS, Nature, vol.475, pp.231-234, 2011. ,
Synthesis, cellular evaluation, and mechanism of action of piperlongumine analogs, Proc. Natl. Acad. Sci. U. S. A, vol.109, pp.15115-15120, 2012. ,
Cytotoxicity of compounds 1 and 4 against HeLa cell line. Cells were incubated with compounds 1 and 4 in the concentration range 10 nMe50 mM for 48 h. Cell survival was then measured using MTT assay ,
Piperlongumine induces inhibition of the ubiquitin-proteasome system in cancer cells, Biochem. Biophys. Res. Commun, vol.431, pp.117-123, 2013. ,
The proteasome in modern drug discovery: second life of a highly valuable drug target, ACS Cent. Sci, vol.3, pp.830-838, 2017. ,
Structure-driven developments of 26S proteasome inhibitors, Annu. Rev. Pharmacol. Toxicol, vol.56, pp.191-209, 2016. ,
The logic of the 26S proteasome, Cell, vol.169, pp.792-806, 2017. ,
Dimerized linear mimics of a natural cyclopeptide (TMC-95A) are potent noncovalent inhibitors of the eukaryotic 20S proteasome, J. Med. Chem, vol.56, pp.3367-3378, 2013. ,
URL : https://hal.archives-ouvertes.fr/hal-00842686
, Hydroxyureas as noncovalent proteasome inhibitors, vol.51, pp.247-249, 2012.
Proteasome inhibitors: recent advances and new perspectives in medicinal chemistry, Curr. Top. Med. Chem, vol.10, pp.232-256, 2010. ,
URL : https://hal.archives-ouvertes.fr/hal-00807658
Villoutreix, 1,2,4-Oxadiazoles identified by virtual screening and their non-covalent inhibition of the human 20S proteasome, Curr. Med. Chem, vol.20, pp.2351-2362, 2013. ,
Development of the proteasome inhibitor Velcade (bortezomib), Canc. Invest, vol.22, pp.304-311, 2004. ,
Durie, Carfilzomib, pomalidomide, and dexamethasone for relapsed or refractory myeloma, Blood, vol.126, pp.2284-2290, 2015. ,
Oral ixazomib, lenalidomide, and dexamethasone for multiple myeloma, N. Engl. J. Med, vol.374, pp.1621-1634, 2016. ,
Syringolin A selectively labels the 20 S proteasome in murine EL4 and wild-type and bortezomib-adapted leukaemic cell lines, Chembiochem, vol.10, pp.2638-2643, 2009. ,
Activity-based probes for the multicatalytic proteasome, FEBS J, vol.284, pp.1540-1554, 2017. ,
ROS inhibitor N-acetyl-L-cysteine antagonizes the activity of proteasome inhibitors, Biochem. J, vol.454, pp.201-208, 2013. ,
Proteasomes in immune cells: more than peptide producers?, Nat. Rev. Immunol, vol.10, pp.73-78, 2010. ,
Degradation of nuclear oncoproteins by the ubiquitin system in vitro, Proc. Natl. Acad. Sci. U. S. A, vol.88, pp.139-143, 1991. ,
PR-924, a selective inhibitor of the immunoproteasome subunit LMP-7, blocks multiple myeloma cell growth both in vitro and in vivo, Br. J. Haematol, vol.152, pp.155-163, 2011. ,
Molecular basis of resistance to proteasome inhibitors in hematological malignancies, Drug Resist. Updates, vol.18, pp.18-35, 2015. ,
Proteasome inhibitors in cancer therapy, Nat. Rev. Clin. Oncol, vol.14, pp.417-433, 2017. ,
Emerging role of immunoproteasomes in pathophysiology, Immunol. Cell Biol, vol.94, pp.812-820, 2016. ,
Inhibition and deficiency of the immunoproteasome subunit LMP7 suppress the development and progression of colorectal carcinoma in mice, Oncotarget, vol.8, pp.50873-50888, 2017. ,
A selective inhibitor of the immunoproteasome subunit LMP7 blocks cytokine production and attenuates progression of experimental arthritis, Nat. Med, vol.15, pp.781-787, 2009. ,
, considérablement le pouvoir des inhibiteur sur les CASP-2 et -3 in vitro, avec des rapports kinact/KI de 1,2 .10 6 et 1,6.10 6 M -1 .s -1 respectivement
, Les résultats que nous avons obtenus sont différents de ceux obtenus par Chauvier
, M -1 .s -1 publié sur la CASP-3. Enfin, nous avons montré que le composé Q-D
, TRP-901, sur la CASP-3, nous pouvons supposer que si le peptide TRP-901 était déméthylé, l'effet du composé Q-DEVD-OPh serait nettement supérieur à celui du, pp.2-601
, Enfin, nous avons évalué la sélectivité du composé D2Me-TRP601 sur les Cathepsines
, M -1 .s -1 . L'effet étant nettement moins efficace que sur les CASP-2 et -3
en 2011 avaient démontré le composé n'altérait pas de manière significative l'activité de 56 enzymes testées à 10 µM, parmi lesquelles : des kinases, des phosphatases, des protéases à sérine, cystéine et aspartate, des enzymes du métabolisme etc,? . De plus ,
, En effet, le composé Q-VD-OPh a un effet inactivateur modéré sur l'activité CASP-2 dans les tests enzymatiques in vitro, d'une part
, Dans d'autres modèles cellulaires il est connu que la vincristine induit une apoptose CASP
, Par exemple, il a été montré que dans lignées de neuroblastomes SH-SY5Y, la précurseur amyloïde humaine (mutations Swedish (K670N/M671L) et Indiana (V717F)), constituent de bons modèles d'étude. En effet, les animaux développent rapidement des plaques amyloïdes et ont un déclin de la mémoire âge-dépendant. À partir de ces modèles soumis à l'effet des molécules
, De plus, pour étudier un rôle de la CASP-2 à des étapes précoces de la pathologie, l'effet des molécules pourrait aussi être évalué sur des animaux où les oligomères Ab sont injectés par stéréotaxie
Inhibition of the Inflammasome NLRP3 by Arglabin Attenuates Inflammation, Protects Pancreatic ?-Cells from Apoptosis, and Prevents Type 2 Diabetes Mellitus Development in ApoE2Ki Mice on a Chronic High-Fat Diet, J. Pharmacol. Exp. Ther, vol.357, pp.487-494, 2016. ,
URL : https://hal.archives-ouvertes.fr/hal-01544052
The Bcl-2 protein family: arbiters of cell survival, Science, vol.281, pp.1322-1326, 1998. ,
NALP3 forms an IL-1beta-processing inflammasome with increased activity in Muckle-Wells autoinflammatory disorder, Immunity, vol.20, pp.319-325, 2004. ,
Ocular neuroprotection by siRNA targeting caspase-2, Cell Death Dis, vol.2, p.173, 2011. ,
Intranasal delivery of caspase-9 inhibitor reduces caspase-6-dependent axon/neuron loss and improves neurological function after stroke, J Neurosci, vol.31, pp.8894-8904, 2011. ,
, , 2013.
, Mol. Biol. (Mosk.), vol.47, pp.187-204
Apoptosis and autophagy: Regulation of caspase-9 by phosphorylation, FEBS J, vol.276, pp.6063-6073, 2009. ,
Inhibition of caspase-9 through phosphorylation at Thr 125 by ERK MAPK, Nat. Cell Biol, vol.5, pp.647-654, 2003. ,
Human ICE/CED-3 protease nomenclature, Cell, vol.87, p.171, 1996. ,
p38-MAPK Signals Survival by Phosphorylation of Caspase-8 and Caspase-3 in Human Neutrophils, J Exp Med, vol.199, pp.449-458, 2004. ,
Mitochondrial targeting and a novel transmembrane arrest of Alzheimer's amyloid precursor protein impairs mitochondrial function in neuronal cells, J. Cell Biol, vol.161, pp.41-54, 2003. ,
Restraint of apoptosis during mitosis through interdomain phosphorylation of caspase-2, EMBO J, vol.28, pp.3216-3227, 2009. ,
PIDD death-domain phosphorylation by ATM controls prodeath versus prosurvival PIDDosome signaling, Mol. Cell, vol.47, pp.681-693, 2012. ,
NPM1 directs PIDDosome-dependent caspase-2 activation in the nucleolus, J. Cell Biol, vol.216, pp.1795-1810, 2017. ,
, , 2006.
, Substrate specificity of human kallikrein 6: salt and glycosaminoglycan activation effects, J. Biol. Chem, vol.281, pp.3116-3126
The synthesis of lysylfluoromethanes and their properties as inhibitors of trypsin, plasmin and cathepsin B, Biochem. J, vol.241, pp.871-875, 1987. ,
, Pyrido-imidazodiazepinones as a new class of reversible inhibitors of human kallikrein 7, 2015.
URL : https://hal.archives-ouvertes.fr/hal-01120269
, Eur J Med Chem, vol.93, pp.202-213
Classification of the caspase-hemoglobinase fold: detection of new families and implications for the origin of the eukaryotic separins, Proteins, vol.46, pp.355-367, 2002. ,
Different voltage-dependent thresholds for inducing long-term depression and long-term potentiation in slices of rat visual cortex, Nature, vol.347, pp.69-72, 1990. ,
Death receptors: signaling and modulation, Science, vol.281, pp.1305-1308, 1998. ,
Regulated cell death: signaling and mechanisms, Annu. Rev. Cell Dev. Biol, vol.30, pp.337-356, 2014. ,
Drugs in Clinical Trials for Alzheimer's Disease: The Major Trends, Cell Death Dis, vol.5, pp.1186-1225, 1526. ,
Non-apoptotic Caspase regulation of stem cell properties, Seminars in Cell & Developmental Biology, 2017. ,
Targeted Covalent Inhibitors for Drug Design, Angew. Chem. Int. Ed. Engl, vol.55, pp.13408-13421, 2016. ,
The biochemical mechanism of caspase-2 activation, Cell Death Differ, vol.11, pp.1234-1241, 2004. ,
Caspase 2 is both required for p53-mediated apoptosis and downregulated by p53 in a p21-dependent manner, Cell Cycle, vol.7, pp.1133-1138, 2008. ,
The CD95 type I/type II model, Semin. Immunol, vol.15, pp.185-193, 2003. ,
Evolutionary lines of cysteine peptidases, Biol. Chem, vol.382, pp.727-733, 2001. ,
Mammalian G1-and S-phase checkpoints in response to DNA damage, Curr. Opin. Cell Biol, vol.13, pp.738-747, 2001. ,
Covalent inhibitors in drug discovery: from accidental discoveries to avoided liabilities and designed therapies, Drug Discovery Today, vol.20, pp.1061-1073, 2015. ,
Regulation of AMPA receptor endocytosis by a signaling mechanism shared with LTD, Nat. Neurosci, vol.3, pp.1291-1300, 2000. ,
, Biochemistry, 2002.
Defects in regulation of apoptosis in caspase-2-deficient mice, Genes Dev, vol.12, pp.1304-1314, 1998. ,
A Water-Bridged Cysteine-Cysteine Redox Regulation Mechanism in Bacterial Protein Tyrosine Phosphatases, vol.3, pp.665-677, 2017. ,
The genetic epidemiology of neurodegenerative disease, J Clin Invest, vol.115, pp.1449-1457, 2005. ,
Microtubule-targeted anticancer agents and apoptosis, Oncogene, vol.22, pp.9075-9086, 2003. ,
A Unified Model for Apical Caspase Activation, Molecular Cell, vol.11, pp.529-541, 2003. ,
Activation of caspases-8 and -10 by FLIP(L), Biochem. J, vol.382, pp.651-657, 2004. ,
Promoting the clearance of neurotoxic proteins in neurodegenerative disorders of ageing, Nat Rev Drug Discov, vol.17, pp.660-688, 2018. ,
The potential role of rho GTPases in Alzheimer's disease pathogenesis, Mol. Neurobiol, vol.50, pp.406-422, 2014. ,
Caspase-2-induced Apoptosis Requires Bid Cleavage: A Physiological Role for Bid in Heat Shock-induced Death, Mol Biol Cell, vol.17, pp.2150-2157, 2006. ,
Familial Alzheimer's disease-linked presenilin 1 variants elevate Abeta1-42/1-40 ratio in vitro and in vivo, Neuron, vol.17, pp.1005-1013, 1996. ,
Piperlongumine and some of its analogs inhibit selectively the human immunoproteasome over the constitutive proteasome, Biochem. Biophys. Res. Commun, vol.496, pp.961-966, 2018. ,
The role of caspase-2 in stress-induced apoptosis, J Cell Mol Med, vol.14, pp.1212-1224, 2010. ,
Caspase-2: the orphan caspase, Cell Death Differ, vol.19, pp.51-57, 2012. ,
Characterization of cytoplasmic caspase-2 activation by induced proximity, Mol. Cell, vol.35, pp.830-840, 2009. ,
Demonstration of amyloid deposits and neurofibrillary changes in whole brain sections, Brain Pathol, vol.1, pp.213-216, 1991. ,
Abnormally phosphorylated tau protein related to the formation of neurofibrillary tangles and neuropil threads in the cerebral cortex of sheep and goat, Neurosci. Lett, vol.171, pp.1-4, 1994. ,
Staging of Alzheimer diseaseassociated neurofibrillary pathology using paraffin sections and immunocytochemistry, Acta Neuropathol, vol.112, pp.389-404, 2006. ,
Regulation of Caspase 9 through Phosphorylation by Protein Kinase C Zeta in Response to Hyperosmotic Stress, Mol Cell Biol, vol.25, pp.10543-10555, 2005. ,
Involvement of oxidative stress and caspase 2-mediated intrinsic pathway signaling in age-related increase in muscle cell apoptosis in mice, Apoptosis, vol.13, pp.822-832, 2008. ,
Potent inactivation of cathepsins S and L by peptidyl (acyloxy)methyl ketones, Biol. Chem. Hoppe-Seyler, vol.375, pp.343-347, 1994. ,
Caspase-2 mediates a Brucella abortus RB51-induced hybrid cell death having features of apoptosis and pyroptosis, Front Cell Infect Microbiol, vol.3, p.83, 2013. ,
, , 2015.
, Endoplasmic Reticulum Stress Activates the Inflammasome via NLRP3-and Caspase-2-Driven Mitochondrial Damage, Immunity, vol.43, pp.451-462
Rational design of enzyme inhibitors: multisubstrate analogue inhibitors, J. Med. Chem, vol.32, pp.2-7, 1989. ,
Caspase substrates and neurodegenerative diseases, Brain Res. Bull, vol.80, pp.251-267, 2009. ,
Dimerization and autoprocessing of the Nedd2 (caspase-2) precursor requires both the prodomain and the carboxyl-terminal regions, J. Biol. Chem, vol.273, pp.6763-6768, 1998. ,
Caspase inhibitors: viral, cellular and chemical, Cell Death Differ, vol.14, pp.73-78, 2007. ,
Apoptotic Pathway and MAPKs Differentially Regulate Chemotropic Responses of Retinal Growth Cones, Neuron, vol.37, pp.939-952, 2003. ,
Local caspase activation interacts with Slit-Robo signaling to restrict axonal arborization, J Cell Biol, vol.203, pp.657-672, 2013. ,
Genetic inhibition of caspase-2 reduces hypoxicischemic and excitotoxic neonatal brain injury, Ann. Neurol, vol.70, pp.781-789, 2011. ,
Q-VD-OPh, a broad spectrum caspase inhibitor with potent antiapoptotic properties, Apoptosis, vol.8, pp.345-352, 2003. ,
The fine-tuning of proteolytic pathways in Alzheimer's disease, Cell. Mol. Life Sci, vol.73, pp.3433-3451, 2016. ,
Molecular cloning of the interleukin-1 beta converting enzyme, Science, vol.256, pp.97-100, 1992. ,
Crystal structure of a procaspase-7 zymogen: mechanisms of activation and substrate binding, Cell, vol.107, pp.399-407, 2001. ,
Screening for the beta-amyloid precursor protein mutation (APP717: Val----Ile) in extended pedigrees with early onset Alzheimer's disease, Neurosci. Lett, vol.129, pp.134-135, 1991. ,
Upstream control of apoptosis by caspase-2 in serum-deprived primary neurons, Apoptosis, vol.10, pp.1243-1259, 2005. ,
URL : https://hal.archives-ouvertes.fr/hal-00082231
Broad-spectrum caspase inhibitors: from myth to reality?, Cell Death and Differentiation, vol.14, pp.387-391, 2007. ,
URL : https://hal.archives-ouvertes.fr/hal-00258847
Targeting neonatal ischemic brain injury with a pentapeptidebased irreversible caspase inhibitor, Cell Death Dis, vol.2, p.203, 2011. ,
URL : https://hal.archives-ouvertes.fr/hal-00630609
Apoptotic cells provide an unexpected source of Wnt3 signaling to drive hydra head regeneration, Dev. Cell, vol.17, pp.279-289, 2009. ,
Gamma secretase-activating protein is a substrate for caspase-3: implications for Alzheimer's disease, Biol. Psychiatry, vol.77, pp.720-728, 2015. ,
Caspase Allostery and Conformational Selection, Chem. Rev, vol.116, pp.6666-6706, 2016. ,
Prodomain-dependent nuclear localization of the caspase-2 (Nedd2) precursor. A novel function for a caspase prodomain, J. Biol. Chem, vol.273, pp.24535-24542, 1998. ,
Pro-inflammatory programmed cell death, Trends Microbiol, vol.9, pp.113-114, 2001. ,
Evaluation of enzyme inhibitors in drug discovery. A guide for medicinal chemists and pharmacologists, Methods Biochem Anal, vol.46, pp.1-265, 2005. ,
Targeting enzyme inhibitors in drug discovery, Expert Opin. Ther. Targets, vol.11, pp.967-978, 2007. ,
Caspase-2 pre-mRNA alternative splicing: Identification of an intronic element containing a decoy 3? acceptor site, Proc Natl Acad Sci U S A, vol.98, pp.938-943, 2001. ,
Polypyrimidine Track-binding Protein Binding Downstream of Caspase-2 Alternative Exon 9 Represses Its Inclusion*, J Biol Chem, vol.276, pp.8535-8543, 2001. ,
The Proteasome in Modern Drug Discovery: Second Life of a Highly Valuable Drug Target, ACS Cent Sci, vol.3, pp.830-838, 2017. ,
An apoptosis-inhibiting baculovirus gene with a zinc finger-like motif, J. Virol, vol.67, pp.2168-2174, 1993. ,
Caspase activation pathways: some recent progress, Cell Death and Differentiation, vol.16, pp.935-938, 2009. ,
Alzheimer's disease drug development pipeline, Alzheimers Dement (N Y), vol.4, pp.195-214, 2018. ,
Distinct pathways mediate axon degeneration during apoptosis and axon-specific pruning, Nat Commun, vol.4, p.1876, 2013. ,
Bax crystal structures reveal how BH3 domains activate Bax and nucleate its oligomerization to induce apoptosis, Cell, vol.152, pp.519-531, 2013. ,
Control of apoptosis by the BCL-2 protein family: implications for physiology and therapy, Nat. Rev. Mol. Cell Biol, vol.15, pp.49-63, 2014. ,
A multi-pronged approach for compiling a global map of allosteric regulation in the apoptotic caspases, Methods Enzymol, vol.544, pp.215-249, 2014. ,
Caspase-2 cleaves DNA fragmentation factor (DFF45)/Inhibitor of caspase-activated DNase (ICAD), Archives of Biochemistry and Biophysics, vol.468, pp.134-139, 2007. ,
The identification of markers of macrophage differentiation in PMA-stimulated THP-1 cells and monocyte-derived macrophages, PLoS ONE, vol.5, p.8668, 2010. ,
Substrate and Inhibitor-induced Dimerization and Cooperativity in Caspase-1 but Not Caspase-3, J. Biol. Chem, vol.288, pp.9971-9981, 2013. ,
Caspase-2-mediated cell death is required for deleting aneuploid cells, Oncogene, vol.36, pp.2704-2714, 2017. ,
Platelet formation is the consequence of caspase activation within megakaryocytes, Blood, vol.100, pp.1310-1317, 2002. ,
Covalent inhibitors design and discovery, European Journal of Medicinal Chemistry, vol.138, pp.96-114, 2017. ,
Proteases and proteolysis in Alzheimer disease: a multifactorial view on the disease process, Physiol. Rev, vol.90, pp.465-494, 2010. ,
The secretases: enzymes with therapeutic potential in Alzheimer disease, Nat Rev Neurol, vol.6, pp.99-107, 2010. ,
A decade of caspases, Oncogene, vol.22, pp.8543-8567, 2003. ,
?-amyloid induces a dying-back process and remote trans-synaptic alterations in a microfluidic-based reconstructed neuronal network, Acta Neuropathol Commun, vol.2, p.145, 2014. ,
Caspase-14 protects against epidermal UVB photodamage and water loss, Nat. Cell Biol, vol.9, pp.666-674, 2007. ,
Caspase-14 reveals its secrets, J Cell Biol, vol.180, pp.451-458, 2008. ,
Dimerized linear mimics of a natural cyclopeptide (TMC-95A) are potent noncovalent inhibitors of the eukaryotic 20S proteasome, J. Med. Chem, vol.56, pp.3367-3378, 2013. ,
URL : https://hal.archives-ouvertes.fr/hal-00842686
IAP family proteins--suppressors of apoptosis, Genes Dev, vol.13, pp.239-252, 1999. ,
Human kallikrein 6 as a biomarker of alzheimer's disease, Clin. Biochem, vol.33, pp.663-667, 2000. ,
, , 2012.
, Chain Assembly in Mediating Apoptotic Cell Death. Mol Cell, vol.47, pp.291-305
Caspase-2 deficiency promotes aberrant DNA-damage response and genetic instability, Cell Death Differ, vol.19, pp.1288-1298, 2012. ,
An unexpected role for caspase-2 in neuroblastoma, Cell Death Dis, vol.5, 1383. ,
New insights into apoptosome structure and function, Cell Death Differ, vol.25, pp.1194-1208, 2018. ,
Emerging principles in protease-based drug discovery, Nat Rev Drug Discov, vol.9, pp.690-701, 2010. ,
Recent development of peptide drugs and advance on theory and methodology of peptide inhibitor design, Med Chem, vol.11, pp.235-247, 2015. ,
RAIDD is a new "death" adaptor molecule, Nature, vol.385, pp.86-89, 1997. ,
Human inhibitor of apoptosis proteins: why XIAP is the black sheep of the family, EMBO Rep, vol.7, pp.988-994, 2006. ,
Caspase inhibitors, Cell Death Differ, vol.6, pp.1081-1086, 1999. ,
Aza-peptide Michael acceptors: a new class of inhibitors specific for caspases and other clan CD cysteine proteases, J. Med. Chem, vol.47, pp.1889-1892, 2004. ,
A caspase-activated DNase that degrades DNA during apoptosis, and its inhibitor ICAD, Nature, vol.391, pp.43-50, 1998. ,
PKA phosphorylation of AMPA receptor subunits controls synaptic trafficking underlying plasticity, Nat. Neurosci, vol.6, pp.136-143, 2003. ,
Multiple species of CPP32 and Mch2 are the major active caspases present in apoptotic cells, EMBO J, vol.16, pp.2271-2281, 1997. ,
Caspase-2 at a glance, J. Cell. Sci, vol.125, pp.5911-5915, 2012. ,
The pyroptosome: a supramolecular assembly of ASC dimers mediating inflammatory cell death via caspase-1 activation, Cell Death Differ, vol.14, pp.1590-1604, 2007. ,
Neural stem cell differentiation is dependent upon endogenous caspase 3 activity, FASEB J, vol.19, pp.1671-1673, 2005. ,
New approaches and therapeutics targeting apoptosis in disease, Pharmacol. Rev, vol.57, pp.187-215, 2005. ,
Apoptosis and caspases in neurodegenerative diseases, N. Engl. J. Med, vol.348, pp.1365-1375, 2003. ,
Expression of a dominant negative mutant of interleukin-1 beta converting enzyme in transgenic mice prevents neuronal cell death induced by trophic factor withdrawal and ischemic brain injury, J. Exp. Med, vol.185, pp.933-940, 1997. ,
Cryo-EM Structure of Caspase-8 Tandem DED Filament Reveals Assembly and Regulation Mechanisms of the Death-Inducing Signaling Complex, Mol. Cell, vol.64, pp.236-250, 2016. ,
The protein structures that shape caspase activity, specificity, activation and inhibition, Biochem J, vol.384, pp.201-232, 2004. ,
Dependence of ?-helical and ?-sheet amino acid propensities on the overall protein fold type, BMC Struct Biol, vol.12, p.18, 2012. ,
Up-regulation of the proapoptotic caspase 2 splicing isoform by a candidate tumor suppressor, RBM5, Proc Natl Acad Sci U S A, vol.105, pp.15708-15713, 2008. ,
Caspases Connect Cell-Death Signaling to Organismal Homeostasis, Immunity, vol.44, pp.221-231, 2016. ,
Molecular mechanisms of cell death: recommendations of the Nomenclature Committee on Cell Death, Cell Death Differ, vol.25, pp.486-541, 2018. ,
URL : https://hal.archives-ouvertes.fr/hal-01727577
Caspase cleavage of tau: linking amyloid and neurofibrillary tangles in Alzheimer's disease, Proc. Natl. Acad. Sci. U.S.A, vol.100, pp.10032-10037, 2003. ,
Inhibition of human caspases by peptide-based and macromolecular inhibitors, J. Biol. Chem, vol.273, pp.32608-32613, 1998. ,
Purification and catalytic properties of human caspase family members, Cell Death Differ, vol.6, pp.362-369, 1999. ,
Classification of Proteases without tears, Biochemical Education, vol.25, pp.161-167, 1997. ,
Involvement of caspases in proteolytic cleavage of Alzheimer's amyloidbeta precursor protein and amyloidogenic A beta peptide formation, Cell, vol.97, pp.395-406, 1999. ,
DLK induces developmental neuronal degeneration via selective regulation of proapoptotic JNK activity, J. Cell Biol, vol.194, pp.751-764, 2011. ,
Engineering ?-sheets employing Nmethylated heterochiral amino acids, Chem. Sci, vol.7, pp.5212-5218, 2016. ,
A century of Alzheimer's disease, Science, vol.314, pp.777-781, 2006. ,
Kosmotropic salt activation and substrate specificity of poliovirus protease 3C, Biochemistry, vol.45, pp.12083-12089, 2006. ,
Cleavage at the caspase-6 site is required for neuronal dysfunction and degeneration due to mutant huntingtin, Cell, vol.125, pp.1179-1191, 2006. ,
Cell Death Signaling, Cold Spring Harb Perspect Biol, vol.7, 2015. ,
ICE heats up, Cell Death Differ, vol.8, pp.549-550, 2001. ,
Vincristine induced apoptosis in acute lymphoblastic leukaemia cells: a mitochondrial controlled pathway regulated by reactive oxygen species?, Int. J. Oncol, vol.21, pp.1339-1345, 2002. ,
CASPASE 2-MEDIATED TUMOR SUPPRESSION INVOLVES SURVIVIN GENE SILENCING, Oncogene, vol.29, pp.1280-1292, 2010. ,
Caspase-2 induces apoptosis by releasing proapoptotic proteins from mitochondria, J. Biol. Chem, vol.277, pp.13430-13437, 2002. ,
Synthesis and biological evaluation of novel 1,2-benzisothiazol-3-one, 2015. ,
, Med Chem Res, vol.24, pp.1814-1829
Formation and structure of a NAIP5-NLRC4 inflammasome induced by direct interactions with conserved N-and Cterminal regions of flagellin, J. Biol. Chem, vol.287, pp.38460-38472, 2012. ,
The NALP3 inflammasome is involved in the innate immune response to amyloid-beta, Nat. Immunol, vol.9, pp.857-865, 2008. ,
The novel caspase-3 substrate Gap43 is involved in AMPA receptor endocytosis and long-term depression, Mol. Cell Proteomics, vol.12, pp.3719-3731, 2013. ,
Inhibition of interleukin 1beta converting enzyme family proteases reduces ischemic and excitotoxic neuronal damage, Proc. Natl. Acad. Sci. U.S.A, vol.94, pp.2007-2012, 1997. ,
Discovery of an allosteric site in the caspases, Proc. Natl. Acad. Sci. U.S.A, vol.101, pp.12461-12466, 2004. ,
Functional activation of Nedd2/ICH-1 (caspase-2) is an early process in apoptosis, J. Biol. Chem, vol.272, pp.13134-13139, 1997. ,
The hierarchical structural architecture of inflammasomes, supramolecular inflammatory machines, Curr. Opin. Struct. Biol, vol.31, pp.75-83, 2015. ,
Inflammatory processes in Alzheimer's disease, J. Neuroimmunol, vol.184, pp.69-91, 2007. ,
NLRP3 is activated in Alzheimer's disease and contributes to pathology in APP/PS1 mice, Nature, vol.493, pp.674-678, 2013. ,
The Current State of Peptide Drug Discovery: Back to the Future?, J. Med. Chem, vol.61, pp.1382-1414, 2018. ,
Specific caspase interactions and amplification are involved in selective neuronal vulnerability in Huntington's disease, Cell Death Differ, vol.11, pp.424-438, 2004. ,
The interleukin 1beta-converting enzyme, caspase 1, is activated during Shigella flexneri-induced apoptosis in human monocyte-derived macrophages, Infect. Immun, vol.65, pp.5165-5170, 1997. ,
Caspase-2 is required for cell death induced by cytoskeletal disruption, Oncogene, vol.27, pp.3393-3404, 2008. ,
A tumor suppressor function for caspase-2, Proc. Natl. Acad. Sci. U.S.A, vol.106, pp.5336-5341, 2009. ,
Caspase-2 is resistant to inhibition by inhibitor of apoptosis proteins (IAPs) and can activate caspase-7, FEBS J, vol.272, pp.1401-1414, 2005. ,
Two adjacent trimeric Fas ligands are required for Fas signaling and formation of a death-inducing signaling complex, Mol. Cell. Biol, vol.23, pp.1428-1440, 2003. ,
Physiological functions of non-apoptotic caspase activity in the nervous system, Semin. Cell Dev. Biol, 2017. ,
Cathepsin B is a New Drug Target for Traumatic Brain Injury Therapeutics: Evidence for E64d as a Promising Lead Drug Candidate, Front Neurol, vol.6, p.178, 2015. ,
AIM2 recognizes cytosolic dsDNA and forms a caspase-1-activating inflammasome with ASC, Nature, vol.458, pp.514-518, 2009. ,
Caspases as therapeutic targets, J. Cell. Mol. Med, vol.12, pp.1502-1516, 2008. ,
Molecular determinants of caspase-9 activation by the Apaf-1 apoptosome, Proceedings of the National Academy of Sciences, vol.111, pp.16254-16261, 2014. ,
Modulation of recombinant human prostate-specific antigen: activation by Hofmeister salts and inhibition by azapeptides. Appendix: thermodynamic interpretation of the activation by concentrated salts, Biochemistry, vol.40, pp.11734-11741, 2001. ,
Apoptotic and non-apoptotic roles of caspases in neuronal physiology and pathophysiology, Nat. Rev. Neurosci, vol.13, pp.395-406, 2012. ,
The inflammasome adaptor ASC regulates the function of adaptive immune cells by controlling Dock2-mediated Rac activation and actin polymerization, Nat. Immunol, vol.12, pp.1010-1016, 2011. ,
A role for caspases in lens fiber differentiation, J. Cell Biol, vol.140, pp.153-158, 1998. ,
The p35 relative, p49, inhibits mammalian and Drosophila caspases including DRONC and protects against apoptosis, Cell Death Differ, vol.9, pp.1311-1320, 2002. ,
Colony-stimulating factor-1-induced oscillations, p.3, 2009. ,
, kinase/AKT are required for caspase activation in monocytes undergoing differentiation into macrophages, Blood, vol.114, pp.3633-3641
PIDD mediates and stabilizes the interaction between RAIDD and Caspase-2 for the PIDDosome assembly, BMB Rep, vol.46, pp.471-476, 2013. ,
The PIDDosome, DNA-damage-induced apoptosis and beyond, Cell Death Differ, vol.19, pp.13-20, 2012. ,
, , 2013.
, Caspase-2 is essential for c-Jun transcriptional activation and Bim induction in neuron death, Biochem. J, vol.455, pp.15-25
Non-apoptotic function of BAD and BAX in long-term depression of synaptic transmission, Neuron, vol.70, pp.758-772, 2011. ,
Inflammatory caspases: key regulators of inflammation and cell death, Biol. Chem, vol.396, pp.193-203, 2015. ,
Cullin3-based polyubiquitination and p62-dependent aggregation of caspase-8 mediate extrinsic apoptosis signaling, Cell, vol.137, pp.721-735, 2009. ,
Mechanisms of hypoxic neurodegeneration in the developing brain, Neuroscientist, vol.8, pp.212-220, 2002. ,
Pyroptotic cell death defends against intracellular pathogens, Immunol. Rev, vol.265, pp.130-142, 2015. ,
Caspases and their substrates, Cell Death Differ, vol.24, pp.1380-1389, 2017. ,
mTOR regulation of autophagy, FEBS Lett, vol.584, pp.1287-1295, 2010. ,
Non-canonical inflammasome activation targets caspase-11, Nature, vol.479, pp.117-121, 2011. ,
Discovery of ritonavir, a potent inhibitor of HIV protease with high oral bioavailability and clinical efficacy, J. Med. Chem, vol.41, pp.602-617, 1998. ,
Caspase Activation Is Required for T Cell Proliferation, J Exp Med, vol.190, pp.1891-1896, 1999. ,
Apoptosis: a basic biological phenomenon with wide-ranging implications in tissue kinetics, Br. J. Cancer, vol.26, pp.239-257, 1972. ,
Amyotrophic lateral sclerosis, The Lancet, vol.377, pp.942-955, 2011. ,
URL : https://hal.archives-ouvertes.fr/hal-01785450
ER Stress Drives Lipogenesis and Steatohepatitis via Caspase-2 Activation of S1P, Cell, vol.175, pp.133-145, 2018. ,
Nitric oxide prevents tumor necrosis factor alpha-induced rat hepatocyte apoptosis by the interruption of mitochondrial apoptotic signaling through S-nitrosylation of caspase-8, Hepatology, vol.32, pp.770-778, 2000. ,
Caspase-2: controversial killer or checkpoint controller?, Apoptosis, vol.14, pp.829-848, 2009. ,
Structural and functional diversity of caspase homologues in non-metazoan organisms, Protoplasma, vol.255, pp.387-397, 2018. ,
Raf-1 Antagonizes Erythroid Differentiation by Restraining Caspase Activation, J Exp Med, vol.196, pp.1347-1353, 2002. ,
Pro-apoptotic cascade activates BID, which oligomerizes BAK or BAX into pores that result in the release of cytochrome c, Cell Death Differ, vol.7, pp.1166-1173, 2000. ,
Peptidyl (acyloxy)methyl ketones and the quiescent affinity label concept: the departing group as a variable structural element in the design of inactivators of cysteine proteinases, Biochemistry, vol.30, pp.4678-4687, 1991. ,
Serine proteases: structure and mechanism of catalysis, Annu. Rev. Biochem, vol.46, pp.331-358, 1977. ,
, , 2005.
, quinoline-1,3-diones as potent caspase-3 inhibitors. Synthesis and SAR of 2-substituted 4-methyl-8-(morpholine-4-sulfonyl)-pyrrolo[3,4-c]quinoline-1,3-diones, Eur J Med Chem, vol.40, pp.1377-1383
Caspase-2: killer, savior and safeguard-emerging versatile roles for an ill-defined caspase, Oncogene, vol.28, pp.3093-3096, 2009. ,
The enigma of caspase-2: the laymen's view, Cell Death Differ, vol.16, pp.195-207, 2009. ,
Pharmacological caspase inhibitors: research towards therapeutic perspectives, J. Physiol. Pharmacol, vol.66, pp.473-482, 2015. ,
Altered cytokine export and apoptosis in mice deficient in interleukin-1 beta converting enzyme, Science, vol.267, pp.2000-2003, 1995. ,
Caspase 2 in apoptosis, the DNA damage response and tumour suppression: enigma no more?, Nat. Rev. Cancer, vol.9, pp.897-903, 2009. ,
, Apoptosis. A cinderella caspase takes center stage. Science, vol.297, pp.1290-1291, 2002.
Identification of a set of genes with developmentally downregulated expression in the mouse brain, Biochem. Biophys. Res. Commun, vol.185, pp.1155-1161, 1992. ,
Induction of apoptosis by the mouse Nedd2 gene, which encodes a protein similar to the product of the Caenorhabditis elegans cell death gene ced-3 and the mammalian IL-1 beta-converting enzyme, Genes Dev, vol.8, pp.1613-1626, 1994. ,
Apoptosis regulatory gene NEDD2 maps to human chromosome segment 7q34-35, a region frequently affected in haematological neoplasms, Hum. Genet, vol.95, pp.641-644, 1995. ,
Identification of E2/E3 ubiquitinating enzymes and caspase activity regulating Drosophila sensory neuron dendrite pruning, Neuron, vol.51, pp.283-290, 2006. ,
, , 2006.
, Drosophila IKK-related kinase regulates nonapoptotic function of caspases via degradation of IAPs, Cell, vol.126, pp.583-596
Covalent inhibitors: an opportunity for rational target selectivity, Curr Opin Chem Biol, vol.39, pp.54-63, 2017. ,
Mechanisms and functions of inflammasomes, Cell, vol.157, pp.1013-1022, 2014. ,
Alice in caspase land. A phylogenetic analysis of caspases from worm to man, Cell Death Differ, vol.9, pp.358-361, 2002. ,
Caspases leave the beaten track: caspase-mediated activation of NF-kappaB, J. Cell Biol, vol.173, pp.165-171, 2006. ,
Caspase 3/caspaseactivated DNase promote cell differentiation by inducing DNA strand breaks, Proc. Natl. Acad. Sci. U.S.A, vol.107, pp.4230-4235, 2010. ,
Requirement for caspase-2 in stress-induced apoptosis before mitochondrial permeabilization, Science, vol.297, pp.1352-1354, 2002. ,
Therapeutic peptides: Historical perspectives, current development trends, and future directions, Bioorganic & Medicinal Chemistry, vol.26, pp.2700-2707, 2018. ,
Vital functions for lethal caspases, Oncogene, vol.24, pp.5137-5148, 2005. ,
Caspase-6 Role in Apoptosis of Human Neurons, Amyloidogenesis, and Alzheimer's Disease, J. Biol. Chem, vol.274, pp.23426-23436, 1999. ,
Potent and Selective Nonpeptide Inhibitors of Caspases 3 and 7 Inhibit Apoptosis and Maintain Cell Functionality, J. Biol. Chem, vol.275, pp.16007-16014, 2000. ,
Potent and selective nonpeptide inhibitors of caspases 3 and 7, J. Med. Chem, vol.44, pp.2015-2026, 2001. ,
Cop, a caspase recruitment domain-containing protein and inhibitor of caspase-1 activation processing, J. Biol. Chem, vol.276, pp.34495-34500, 2001. ,
Apoptotic cells activate the "phoenix rising" pathway to promote wound healing and tissue regeneration, Sci Signal, vol.3, p.13, 2010. ,
Cleavage of BID by caspase 8 mediates the mitochondrial damage in the Fas pathway of apoptosis, Cell, vol.94, pp.491-501, 1998. ,
Functional role of caspase-1 and caspase-3 in an ALS transgenic mouse model, Science, vol.288, pp.335-339, 2000. ,
Mechanistic insights into caspase-9 activation by the structure of the apoptosome holoenzyme, Proc. Natl. Acad. Sci. U.S.A, vol.114, pp.1542-1547, 2017. ,
Caspase-3 activation via mitochondria is required for long-term depression and AMPA receptor internalization, Cell, vol.141, pp.859-871, 2010. ,
Caspase inhibitors: a pharmaceutical industry perspective, Curr Top Med Chem, vol.5, pp.1697-1717, 2005. ,
First-in-class pan caspase inhibitor developed for the treatment of liver disease, J. Med. Chem, vol.48, pp.6779-6782, 2005. ,
Epidermal differentiation does not involve the proapoptotic executioner caspases, but is associated with caspase-14 induction and processing, Cell Death and Differentiation, vol.7, pp.1218-1224, 2000. ,
Design, synthesis and evaluation of 1,2-benzisothiazol-3-one derivatives as potent caspase-3 inhibitors, Bioorg. Med. Chem, vol.21, pp.2960-2967, 2013. ,
Inflammasome-activated gasdermin D causes pyroptosis by forming membrane pores, Nature, vol.535, pp.153-158, 2016. ,
Molecular mechanisms linking amyloid ? toxicity and Tau hyperphosphorylation in Alzheimer???s disease. Free Radic, Biol. Med, vol.83, pp.186-191, 2015. ,
The human caspase-2 gene: alternative promoters, pre-mRNA splicing and AUG usage direct isoform-specific expression, Oncogene, vol.22, pp.935-946, 2003. ,
Identification of a functional DNA binding site for the SREBP-1c transcription factor in the first intron of the human caspase-2 gene, Biochim. Biophys. Acta, vol.1738, pp.1-5, 2005. ,
Structure-based design of targeted covalent inhibitors, Chem Soc Rev, vol.47, pp.3816-3830, 2018. ,
Caspases are not localized in mitochondria during life or death, Cell Death and Differentiation, vol.9, pp.1207-1211, 2002. ,
Loss of caspase-2 accelerates age-dependent alterations in mitochondrial production of reactive oxygen species, Biogerontology, vol.14, pp.121-130, 2013. ,
Proteases: multifunctional enzymes in life and disease, J. Biol. Chem, vol.283, pp.30433-30437, 2008. ,
Structural mechanisms of inflammasome assembly, FEBS J, vol.282, pp.435-444, 2015. ,
Unified polymerization mechanism for the assembly of ASC-dependent inflammasomes, Cell, vol.156, pp.1193-1206, 2014. ,
HIV protease inhibitors: a review of molecular selectivity and toxicity, HIV AIDS (Auckl), vol.7, pp.95-104, 2015. ,
Redesigning the procaspase-8 dimer interface for improved dimerization, Protein Sci, vol.23, pp.442-453, 2014. ,
Molecular Cell Death Platforms and Assemblies, Curr Opin Cell Biol, vol.22, pp.828-836, 2010. ,
Caspase enzymology and activation mechanisms, Meth. Enzymol, vol.544, pp.161-178, 2014. ,
, , 2016.
, Caspase-2 promotes obesity, the metabolic syndrome and nonalcoholic fatty liver disease, Cell Death Dis, vol.7, 2096.
DEATH BY CASPASE DIMERIZATION, Adv Exp Med Biol, vol.747, 2012. ,
The potential for caspases in drug discovery, Curr Opin Drug Discov Devel, vol.13, pp.568-576, 2010. ,
Execution of superoxide-induced cell death by the proapoptotic Bcl-2-related proteins Bid and Bak, Mol. Cell. Biol, vol.29, pp.3099-3112, 2009. ,
Drug discovery considerations in the development of covalent inhibitors, Bioorganic & Medicinal Chemistry Letters, vol.24, pp.33-39, 2014. ,
Exploiting differences in caspase-2 and -3 S? subsites for selectivity: structure-based design, solid-phase synthesis and in vitro activity of novel substrate-based caspase-2 inhibitors, Bioorg. Med. Chem, vol.19, pp.5833-5851, 2011. ,
Aging and calorie restriction regulate the expression of miR-125a-5p and its target genes Stat3, Casp2 and Stard13, Aging (Albany NY), vol.9, pp.1825-1843, 2017. ,
Regulation of inflammasome activation, Immunol. Rev, vol.265, pp.6-21, 2015. ,
Caspase-2 is localized at the Golgi complex and cleaves golgin-160 during apoptosis, J. Cell Biol, vol.149, pp.603-612, 2000. ,
Caspase-2 activation in the absence of PIDDosome formation, J. Cell Biol, vol.185, pp.291-303, 2009. ,
URL : https://hal.archives-ouvertes.fr/hal-02088184
PIDDosome-independent tumor suppression by Caspase-2, Cell Death Differ, vol.19, pp.1722-1732, 2012. ,
Differential activation of the inflammasome by caspase-1 adaptors ASC and Ipaf, Nature, vol.430, pp.213-218, 2004. ,
Phosphatidylserine externalization during CD95-induced apoptosis of cells and cytoplasts requires ICE/CED-3 protease activity, J. Biol. Chem, vol.271, pp.28753-28756, 1996. ,
Inflammatory caspases: linking an intracellular innate immune system to autoinflammatory diseases, Cell, vol.117, pp.561-574, 2004. ,
Inflammatory caspases and inflammasomes: master switches of inflammation, Cell Death Differ, vol.14, pp.10-22, 2007. ,
The inflammasome: a molecular platform triggering activation of inflammatory caspases and processing of proIL-beta, Mol. Cell, vol.10, pp.417-426, 2002. ,
SynapCountJ: A Validated Tool for Analyzing Synaptic Densities in Neurons, Biomedical Engineering Systems and Technologies, pp.41-55, 2017. ,
Cdk1/cyclin B1 controls Fas-mediated apoptosis by regulating caspase-8 activity, Mol. Cell. Biol, vol.30, pp.5726-5740, 2010. ,
Apoptotic Caspases: Multiple or Mistaken Identities?, Trends Cell Biol, vol.28, pp.475-493, 2018. ,
Caspase functions in cell death and disease, Cold Spring Harb Perspect Biol, vol.5, p.8656, 2013. ,
Caspase functions in cell death and disease, Cold Spring Harb Perspect Biol, vol.7, 2015. ,
Comparative structural analysis of the caspase family with other clan CD cysteine peptidases, Biochem J, vol.466, pp.219-232, 2015. ,
Cyclin D3 activates Caspase 2, connecting cell proliferation with cell death, Proc. Natl. Acad. Sci. U.S.A, vol.99, pp.6871-6876, 2002. ,
Inflammatory process in Alzheimer's Disease, Front Integr Neurosci, vol.7, p.59, 2013. ,
Activation and substrate specificity of caspase-14, Biochemistry, vol.43, pp.10560-10569, 2004. ,
Old and Novel Functions of Caspase-2, Int Rev Cell Mol Biol, vol.332, pp.155-212, 2017. ,
RIM proteins and their role in synapse function, Biol. Chem, vol.391, pp.599-606, 2010. ,
Structure of recombinant human CPP32 in complex with the tetrapeptide acetyl-Asp-Val-Ala-Asp fluoromethyl ketone, J. Biol. Chem, vol.272, pp.6539-6547, 1997. ,
Autophagosome formation in mammalian cells, Cell Struct. Funct, vol.27, pp.421-429, 2002. ,
A retrograde apoptotic signal originating in NGF-deprived distal axons of rat sympathetic neurons in compartmented cultures, Cell Res, vol.19, pp.546-560, 2009. ,
Caspase-12 ablation preserves muscle function in the mdx mouse, Hum. Mol. Genet, vol.23, pp.5325-5341, 2014. ,
X-linked inhibitor of apoptosis functions as ubiquitin ligase toward mature caspase-9 and cytosolic Smac/DIABLO, J. Biochem, vol.137, pp.125-132, 2005. ,
E64d, a membrane-permeable cysteine protease inhibitor, attenuates the effects of parathyroid hormone on osteoblasts in vitro, Metab. Clin. Exp, vol.46, pp.1090-1094, 1997. ,
An induced proximity model for caspase-8 activation, J. Biol. Chem, vol.273, pp.2926-2930, 1998. ,
Apoptosis by death factor, Cell, vol.88, pp.355-365, 1997. ,
The Fas death factor, Science, vol.267, pp.1449-1456, 1995. ,
Immuno-and constitutive proteasomes do not differ in their abilities to degrade ubiquitinated proteins, Cell, vol.152, pp.1184-1194, 2013. ,
Physiological Functions of Caspases Beyond Cell Death, Am J Pathol, vol.169, pp.729-737, 2006. ,
Caspase structure, proteolytic substrates, and function during apoptotic cell death, Cell Death Differ, vol.6, pp.1028-1042, 1999. ,
Inducible dimerization and inducible cleavage reveal a requirement for both processes in caspase-8 activation, J. Biol. Chem, vol.285, pp.16632-16642, 2010. ,
Maturation of the olfactory sensory neurons by Apaf-1/caspase-9-mediated caspase activity, Proc. Natl. Acad. Sci. U.S.A, vol.107, pp.13366-13371, 2010. ,
High commitment of embryonic keratinocytes to terminal differentiation through a Notch1-caspase 3 regulatory mechanism, Dev. Cell, vol.6, pp.551-562, 2004. ,
Caspase-2-mediated cleavage of Mdm2 creates a p53-induced positive feedback loop, Mol. Cell, vol.43, pp.57-71, 2011. ,
Caspase activity is required for stimulated B lymphocytes to enter the cell cycle, J. Immunol, vol.170, pp.6065-6072, 2003. ,
Natural and synthetic inhibitors of caspases: targets for novel drugs, Curr Drug Targets CNS Neurol Disord, vol.3, pp.333-340, 2004. ,
Bergmann glia utilize active caspase-3 for differentiation, Brain Res, vol.1078, pp.19-34, 2006. ,
Structural Features of Caspase-Activating Complexes, Int J Mol Sci, vol.13, pp.4807-4818, 2012. ,
Optimized THP-1 differentiation is required for the detection of responses to weak stimuli, Inflamm. Res, vol.56, pp.45-50, 2007. ,
Death domain assembly mechanism revealed by crystal structure of the oligomeric PIDDosome core complex, Cell, vol.128, pp.533-546, 2007. ,
Caspase-2 can trigger cytochrome C release and apoptosis from the nucleus, J. Biol. Chem, vol.277, pp.15147-15161, 2002. ,
Cellular mechanisms controlling caspase activation and function, Cold Spring Harb Perspect Biol, vol.5, 2013. ,
Cathepsins: Proteases that are vital for survival but can also be fatal, Biomed. Pharmacother, vol.105, pp.526-532, 2018. ,
Assessment of kallikrein 6 as a cross-sectional and longitudinal biomarker for Alzheimer's disease, Alzheimer's Research & Therapy, vol.10, p.9, 2018. ,
LTP Inhibits LTD in the Hippocampus via Regulation of GSK3?, Neuron, vol.53, pp.703-717, 2007. ,
URL : https://hal.archives-ouvertes.fr/inserm-00776885
Alternative, Non-secretase Processing of Alzheimer's ?-Amyloid Precursor Protein during Apoptosis by Caspase-6 and -8, J. Biol. Chem, vol.274, pp.21011-21016, 1999. ,
When dying is not the end: Apoptotic caspases as drivers of proliferation, Semin. Cell Dev. Biol, 2017. ,
, The CD95(APO-1/Fas) DISC and beyond, vol.10, pp.26-35, 2003.
Axon diodes for the reconstruction of oriented neuronal networks in microfluidic chambers, Lab Chip, vol.11, pp.3663-3673, 2011. ,
URL : https://hal.archives-ouvertes.fr/hal-02372610
Coumarinic derivatives as mechanism-based inhibitors of alpha-chymotrypsin and human leukocyte elastase, Bioorg. Med. Chem, vol.8, pp.1489-1501, 2000. ,
Decreased apoptosis in proliferative and postmitotic regions of the Caspase 3-deficient embryonic central nervous system, J. Comp. Neurol, vol.423, pp.1-12, 2000. ,
Caspase gene expression in the brain as a function of the clinical progression of Alzheimer disease, Arch. Neurol, vol.60, pp.369-376, 2003. ,
Human Caspases: Activation, Specificity, and Regulation, J Biol Chem, vol.284, pp.21777-21781, 2009. ,
Caspase assays: identifying caspase activity and substrates in vitro and in vivo, Meth. Enzymol, vol.446, pp.351-367, 2008. ,
FLIPL induces caspase-8 activity in the absence of interdomain caspase-8 cleavage and alters substrate specificity, 2011. ,
, Biochem J, vol.433, pp.447-457
Caspase substrates and inhibitors, Cold Spring Harb Perspect Biol, vol.5, p.8680, 2013. ,
Small Molecule Active Site Directed Tools for Studying Human Caspases, Chem. Rev, vol.115, pp.12546-12629, 2015. ,
Irreversible inhibitors of serine, cysteine, and threonine proteases, Chem. Rev, vol.102, pp.4639-4750, 2002. ,
Caspase-2 is required for dendritic spine and behavioral alterations in J20 APP transgenic mice, Nat Commun, vol.4, 1939. ,
Unleashing the therapeutic potential of human kallikrein-related serine proteases, Nat Rev Drug Discov, vol.14, pp.183-202, 2015. ,
Caspase-2 as a tumour suppressor, Cell Death Differ, vol.20, pp.1133-1139, 2013. ,
Loss of caspase-2 augments lymphomagenesis and enhances genomic instability in Atm-deficient mice, Proc. Natl. Acad. Sci. U.S.A, vol.110, 2013. ,
Induction of BIM, a proapoptotic BH3-only BCL-2 family member, is critical for neuronal apoptosis, Neuron, vol.29, pp.615-628, 2001. ,
The keystone of Alzheimer pathogenesis might be sought in A? physiology, Neuroscience, vol.307, pp.26-36, 2015. ,
A primer on caspase mechanisms, Semin. Cell Dev. Biol, 2018. ,
A combinatorial approach for determining protease specificities: application to interleukin-1beta converting enzyme (ICE), Chem. Biol, vol.4, pp.149-155, 1997. ,
Tau is essential to beta -amyloidinduced neurotoxicity, Proc. Natl. Acad. Sci. U.S.A, vol.99, pp.6364-6369, 2002. ,
Regulation of inflammasome signaling, Nat. Immunol, vol.13, pp.333-342, 2012. ,
Evolutionary families of peptidases, Biochem. J, vol.290, pp.205-218, 1993. ,
MEROPS: the database of proteolytic enzymes, their substrates and inhibitors, Nucleic Acids Res, vol.40, pp.343-350, 2012. ,
Twenty years of the MEROPS database of proteolytic enzymes, their substrates and inhibitors, Nucleic Acids Res, vol.44, pp.343-350, 2016. ,
A novel Apaf-1-independent putative caspase-2 activation complex, J Cell Biol, vol.159, pp.739-745, 2002. ,
Quinone Methides and Aza-Quinone Methides as Latent Alkylating Species in the Design of Mechanism-Based Inhibitors of Serine Proteases and ?-Lactamases, Quinone Methides, pp.357-383, 2009. ,
Dimer formation drives the activation of the cell death protease caspase 9, Proc. Natl. Acad. Sci. U.S.A, vol.98, pp.14250-14255, 2001. ,
Neuronal caspase 2 activity and function requires RAIDD, but not PIDD, Biochem. J, vol.444, pp.591-599, 2012. ,
Structure-based design of human immuno-and constitutive proteasomes inhibitors, Eur J Med Chem, vol.145, pp.570-587, 2018. ,
URL : https://hal.archives-ouvertes.fr/hal-01713510
The apoptosome: signalling platform of cell death, Nat. Rev. Mol. Cell Biol, vol.8, pp.405-413, 2007. ,
Structural basis for the activation of human procaspase-7, Proc. Natl. Acad. Sci. U.S.A, vol.98, pp.14790-14795, 2001. ,
Mechanism-based inactivation of caspases by the apoptotic suppressor p35, Biochemistry, vol.40, pp.13274-13280, 2001. ,
Structure of the apoptotic protease-activating factor 1 bound to ADP, Nature, vol.434, pp.926-933, 2005. ,
Rational design of peptide-based HIV proteinase inhibitors, Science, vol.248, pp.358-361, 1990. ,
Mechanistic basis of enzyme-targeted drugs, Biochemistry, vol.44, pp.5561-5571, 2005. ,
The role of caspases in Alzheimer's disease; potential novel therapeutic opportunities, Apoptosis, vol.15, pp.1403-1409, 2010. ,
Caspase Cleaved Tau in Alzheimer's Disease: A Therapeutic Target Realized, Int J Neurol Neurother, vol.2, p.14, 2015. ,
Caspases as Therapeutic Targets in Alzheimer's Disease: Is It Time to "Cut" to the Chase?, Int J Clin Exp Pathol, vol.2, pp.108-118, 2008. ,
Caspase activation independent of cell death is required for proper cell dispersal and correct morphology in PC12 cells, Exp Cell Res, vol.295, pp.215-225, 2004. ,
Huntington's disease: from molecular pathogenesis to clinical treatment, Lancet Neurol, vol.10, pp.83-98, 2011. ,
The Critical Role of Organic Chemistry in Drug Discovery, ACS Chem. Neurosci, vol.7, pp.1315-1316, 2016. ,
AlphaII-spectrin is an in vitro target for caspase-2, and its cleavage is regulated by calmodulin binding, Biochem. J, vol.378, pp.161-168, 2004. ,
Regulation of NF-kappaB-dependent lymphocyte activation and development by paracaspase, Science, vol.302, pp.1581-1584, 2003. ,
Differential modulation of endotoxin responsiveness by human caspase-12 polymorphisms, Nature, vol.429, pp.75-79, 2004. ,
Enhanced bacterial clearance and sepsis resistance in caspase-12-deficient mice, Nature, vol.440, pp.1064-1068, 2006. ,
Caspase-8 deficiency in T cells leads to a lethal lymphoinfiltrative immune disorder, J Exp Med, vol.202, pp.727-732, 2005. ,
Essential role for caspase 8 in T-cell homeostasis and T-cellmediated immunity, Genes Dev, vol.17, pp.883-895, 2003. ,
Bax assembly into rings and arcs in apoptotic mitochondria is linked to membrane pores, EMBO J, vol.35, pp.389-401, 2016. ,
Caspase activation: the induced-proximity model, Proc. Natl. Acad. Sci. U.S.A, vol.96, pp.10964-10967, 1999. ,
, , 2006.
, Thrombin-induced endothelial microparticle generation: identification of a novel pathway involving ROCK-II activation by caspase-2, Blood, vol.108, pp.1868-1876
Kallikreins are associated with secondary progressive multiple sclerosis and promote neurodegeneration, Biol. Chem, vol.389, pp.739-745, 2008. ,
On the size of the active site in proteases, I. Papain. Biochem. Biophys. Res. Commun, vol.27, pp.157-162, 1967. ,
On the size of the active site in proteases. I. Papain, Biochem. Biophys. Res. Commun, vol.425, pp.497-502, 1967. ,
Mechanisms of developmental neurite pruning, Cell. Mol. Life Sci, vol.72, pp.101-119, 2015. ,
The morphology of various types of cell death in prenatal tissues, Teratology, vol.7, pp.253-266, 1973. ,
Crystal structure of caspase-2, apical initiator of the intrinsic apoptotic pathway, J. Biol. Chem, vol.278, pp.42441-42447, 2003. ,
Inhibition of caspase-2 by a designed ankyrin repeat protein: specificity, structure, and inhibition mechanism, Structure, vol.15, pp.625-636, 2007. ,
The inflammatory caspases: guardians against infections and sepsis, Cell Death Differ, vol.14, pp.23-31, 2007. ,
Novel small molecule inhibitors of caspase-3 block cellular and biochemical features of apoptosis, J. Pharmacol. Exp. Ther, vol.304, pp.433-440, 2003. ,
Cacidases: caspases can cleave after aspartate, glutamate and phosphoserine residues, Cell Death Differ, vol.23, pp.1717-1726, 2016. ,
Caspase-3-mediated cleavage of ROCK I induces MLC phosphorylation and apoptotic membrane blebbing, Nat. Cell Biol, vol.3, pp.346-352, 2001. ,
Activity-based probes for the study of proteases: recent advances and developments, ChemMedChem, vol.7, pp.1146-1159, 2012. ,
Neuropathological alterations in Alzheimer disease, Cold Spring Harb Perspect Med, vol.1, p.6189, 2011. ,
Structure and mechanism of the complex between cytochrome P4503A4 and ritonavir, Proc Natl Acad Sci U S A, vol.107, pp.18422-18427, 2010. ,
A mitosis-sensing caspase activation platform? New insights into the PIDDosome, Mol Cell Oncol, vol.3, 2015. ,
Caspase-2 and the oxidative stress response, Mol Cell Oncol, vol.2, 2015. ,
Impaired antioxidant defence and accumulation of oxidative stress in caspase-2-deficient mice, Cell Death Differ, vol.19, pp.1370-1380, 2012. ,
Old, new and emerging functions of caspases, Cell Death Differ, vol.22, pp.526-539, 2015. ,
Caspase-2 maintains bone homeostasis by inducing apoptosis of oxidatively-damaged osteoclasts, PLoS ONE, vol.9, p.93696, 2014. ,
Evidence for an Active-Center Histidine in Trypsin through Use of a Specific Reagent, 1-Chloro-3-tosylamido-7-amino-2-heptanone, the Chloromethyl Ketone Derived from N?-Tosyl-L-lysine*, Biochemistry, vol.4, pp.2219-2224, 1965. ,
Mechanisms of caspase activation and inhibition during apoptosis, Mol. Cell, vol.9, pp.459-470, 2002. ,
Caspase activation: revisiting the induced proximity model, Cell, vol.117, pp.855-858, 2004. ,
Caspase activation, inhibition, and reactivation: A mechanistic view, Protein Sci, vol.13, pp.1979-1987, 2004. ,
Inflammatory caspases are innate immune receptors for intracellular LPS, Nature, vol.514, pp.187-192, 2014. ,
Cleavage of GSDMD by inflammatory caspases determines pyroptotic cell death, Nature, vol.526, pp.660-665, 2015. ,
Pyroptosis: Gasdermin-Mediated Programmed Necrotic Cell Death, Trends Biochem. Sci, vol.42, pp.245-254, 2017. ,
Mechanism of XIAP-mediated inhibition of caspase-9, Mol. Cell, vol.11, pp.519-527, 2003. ,
Chk1 Suppresses a Caspase-2 Apoptotic Response to DNA Damage that Bypasses p53, Bcl-2, and Caspase-3, Cell, vol.133, pp.864-877, 2008. ,
Death-effector filaments: novel cytoplasmic structures that recruit caspases and trigger apoptosis, J. Cell Biol, vol.141, pp.1243-1253, 1998. ,
The resurgence of covalent drugs, Nature Reviews Drug Discovery, vol.10, pp.307-317, 2011. ,
The resurrection of the PIDDosome -emerging roles in the DNA-damage response and centrosome surveillance, J. Cell. Sci, vol.130, pp.3779-3787, 2017. ,
14-3-3 protein masks the nuclear localization sequence of caspase-2, The FEBS Journal, vol.0 ,
Non-steroidal Anti-inflammatory Drugs Are Caspase Inhibitors, Cell Chem Biol, vol.24, pp.281-292, 2017. ,
Detection of caspases activation by fluorochrome-labeled inhibitors: Multiparameter analysis by laser scanning cytometry, Cytometry, vol.44, pp.73-82, 2001. ,
An updated view on the functions of caspases in inflammation and immunity, Semin. Cell Dev. Biol, 2018. ,
Specific involvement of caspases in the differentiation of monocytes into macrophages, Blood, vol.100, pp.4446-4453, 2002. ,
Insights into the activity control of the kallikrein-related peptidase 6: small-molecule modulators and allosterism, Biol. Chem, vol.399, pp.1073-1078, 2018. ,
A brain-targeted, modified neurosin (kallikrein-6) reduces ?-synuclein accumulation in a mouse model of multiple system atrophy, Mol Neurodegener, vol.10, pp.150-159, 2009. ,
Catalytic properties of the caspases, Cell Death Differ, vol.6, pp.1054-1059, 1999. ,
Internally quenched fluorescent peptide substrates disclose the subsite preferences of human caspases 1, 3, 6, 7 and 8, Biochem. J. 350 Pt, vol.2, pp.563-568, 2000. ,
Reprieval from execution: the molecular basis of caspase inhibition, Trends Biochem. Sci, vol.27, pp.94-101, 2002. ,
Mitochondria and cell death: outer membrane permeabilization and beyond, Nat. Rev. Mol. Cell Biol, vol.11, pp.621-632, 2010. ,
Substrate specificities of caspase family proteases, J. Biol. Chem, vol.272, pp.9677-9682, 1997. ,
The NLRP3 inflammasome in Alzheimer's disease, Mol. Neurobiol, vol.48, pp.875-882, 2013. ,
Toward the first class of suicide inhibitors of kallikreins involved in skin diseases, J. Med. Chem, vol.58, pp.598-612, 2015. ,
URL : https://hal.archives-ouvertes.fr/hal-01543965
Structural and enzymatic insights into caspase-2 protein substrate recognition and catalysis, J. Biol. Chem, vol.286, pp.34147-34154, 2011. ,
Regulation of dendritic spine motility and stability by Rac1 and Rho kinase: evidence for two forms of spine motility, Mol. Cell. Neurosci, vol.26, pp.429-440, 2004. ,
Regulation of dendritic spine morphology by the rho family of small GTPases: antagonistic roles of Rac and Rho, Cereb. Cortex, vol.10, pp.927-938, 2000. ,
Extracellular neurosin degrades ?-synuclein in cultured cells, Neurosci. Res, vol.67, pp.341-346, 2010. ,
Depletion of GGA3 stabilizes BACE and enhances beta-secretase activity, Neuron, vol.54, pp.721-737, 2007. ,
Caspase-2 Mediates Site-Specific Retinal Ganglion Cell Death After Blunt Ocular Injury, Invest. Ophthalmol. Vis. Sci, vol.59, pp.4453-4462, 2018. ,
An Inhibitor of PIDDosome Formation, Mol. Cell, vol.58, pp.767-779, 2015. ,
Caspases: key mediators of apoptosis, Chem. Biol, vol.5, pp.97-103, 1998. ,
A novel heterodimeric cysteine protease is required for interleukin-1 beta processing in monocytes, Nature, vol.356, pp.768-774, 1992. ,
Inactivation of interleukin-1 beta converting enzyme by peptide (acyloxy)methyl ketones, Biochemistry, vol.33, pp.3934-3940, 1994. ,
A combinatorial approach defines specificities of members of the caspase family and granzyme B. Functional relationships established for key mediators of apoptosis, J. Biol. Chem, vol.272, pp.17907-17911, 1997. ,
The PIDDosome, a protein complex implicated in activation of caspase-2 in response to genotoxic stress, Science, vol.304, pp.843-846, 2004. ,
Autoproteolysis of PIDD marks the bifurcation between pro-death caspase-2 and pro-survival NF-?B pathway, EMBO J, vol.26, pp.197-208, 2007. ,
The Race of 10 Synthetic RNAi-Based Drugs to the Pharmaceutical Market, Pharm. Res, vol.34, pp.1339-1363, 2017. ,
Loss of caspase-2-dependent apoptosis induces autophagy after mitochondrial oxidative stress in primary cultures of young adult cortical neurons, J. Biol. Chem, vol.286, pp.8493-8506, 2011. ,
A nonapoptotic role for CASP2/caspase 2, Autophagy, vol.10, pp.1054-1070, 2014. ,
Nitric oxide inhibits apoptosis downstream of cytochrome C release by nitrosylating caspase 9, Cancer Res, vol.62, pp.1648-1653, 2002. ,
Caspases: Therapeutic Targets in Neurologic Disease, Neurotherapeutics, vol.12, pp.42-48, 2015. ,
Caspases on the brain, J. Neurosci. Res, vol.69, pp.145-150, 2002. ,
Caspase-2 redux, Cell Death Differ, vol.10, pp.101-107, 2003. ,
Caspase-2 and tau-a toxic partnership, Nat. Med, vol.22, pp.1207-1208, 2016. ,
Nedd2 is required for apoptosis after trophic factor withdrawal, but not superoxide dismutase (SOD1) downregulation, in sympathetic neurons and PC12 cells, J. Neurosci, vol.17, pp.1911-1918, 1997. ,
Caspase-2 mediates neuronal cell death induced by beta-amyloid, J. Neurosci, vol.20, pp.1386-1392, 2000. ,
Regulation of caspases in the nervous system implications for functions in health and disease, Prog Mol Biol Transl Sci, vol.99, pp.265-305, 2011. ,
Carboxyl-terminal proteolytic processing of CUX1 by a caspase enables transcriptional activation in proliferating cells, J. Biol. Chem, vol.282, pp.30216-30226, 2007. ,
Vincristine induces cell cycle arrest and apoptosis in SH-SY5Y human neuroblastoma cells, Int. J. Mol. Med, vol.31, pp.113-119, 2013. ,
Targeting proteases: successes, failures and future prospects, Nat Rev Drug Discov, vol.5, pp.785-799, 2006. ,
Protease signalling: the cutting edge, EMBO J, vol.31, pp.1630-1643, 2012. ,
Cysteine cathepsins: from structure, function and regulation to new frontiers, Biochim. Biophys. Acta, vol.1824, pp.68-88, 2012. ,
Caspase-9 cleavage, do you need it?, Biochem J, vol.405, 2007. ,
Functional connection between p53 and caspase-2 is essential for apoptosis induced by DNA damage, Oncogene, vol.25, pp.5683-5692, 2006. ,
The unpredictable caspase-2: what can it do?, Trends Cell Biol, vol.20, pp.150-159, 2010. ,
Axon guidance proteins in neurological disorders, Lancet Neurol, vol.14, pp.532-546, 2015. ,
The history of Z-VAD-FMK, a tool for understanding the significance of caspase inhibition, Acta Histochem, vol.103, pp.241-251, 2001. ,
Programmed Cell Death in Parkinson's Disease. Cold Spring Harb Perspect Med 2, 2012. ,
Pharmacological Inhibition of Caspase-2 Protects Axotomised Retinal Ganglion Cells from Apoptosis in Adult Rats, PLOS ONE, vol.7, p.53473, 2012. ,
Caspase-2 is upregulated after sciatic nerve transection and its inhibition protects dorsal root ganglion neurons from apoptosis after serum withdrawal, PLoS ONE, vol.8, p.57861, 2013. ,
p53-and drug-induced apoptotic responses mediated by BH3-only proteins puma and noxa, Science, vol.302, pp.1036-1038, 2003. ,
Amyloid ? oligomers in Alzheimer's disease pathogenesis, treatment, and diagnosis, Acta Neuropathol, vol.129, pp.183-206, 2015. ,
Caspase-9 activation results in downstream caspase-8 activation and bid cleavage in 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine-induced Parkinson's disease, J. Neurosci, vol.21, pp.9519-9528, 2001. ,
Crystal structure of the cysteine protease interleukin-1?-converting enzyme: A (p20/p10)2 homodimer, Cell, vol.78, pp.343-352, 1994. ,
Functional divergence in the caspase gene family and altered functional constraints: statistical analysis and prediction, Genetics, vol.158, pp.1311-1320, 2001. ,
Ich-1, an Ice/ced-3-related gene, encodes both positive and negative regulators of programmed cell death, Cell, vol.78, pp.739-750, 1994. ,
Murine caspase-11, an ICE-interacting protease, is essential for the activation of ICE, Cell, vol.92, pp.501-509, 1998. ,
Discovery of piperlongumine as a potential novel lead for the development of senolytic agents, Aging (Albany NY), vol.8, pp.2915-2926, 2016. ,
Kinetic and structural characterization of caspase-3 and caspase-8 inhibition by a novel class of irreversible inhibitors, Biochim. Biophys. Acta, vol.1804, pp.1817-1831, 2010. ,
Activated caspase-6 and caspase-6-cleaved fragments of huntingtin specifically colocalize in the nucleus, Hum. Mol. Genet, vol.17, pp.2390-2404, 2008. ,
Caspase cleavage of mutant huntingtin precedes neurodegeneration in Huntington's disease, J. Neurosci, vol.22, pp.7862-7872, 2002. ,
Caspase-mediated programmed cell death pathways as potential therapeutic targets in cancer, Cell Prolif, vol.45, pp.217-224, 2012. ,
Clustering of the neural cell adhesion molecule (NCAM) at the neuronal cell surface induces caspase-8-and -3-dependent changes of the spectrin meshwork required for NCAM-mediated neurite outgrowth, J. Biol. Chem, vol.285, pp.42046-42057, 2010. ,
Local caspase activity directs engulfment of dendrites during pruning, Nat. Neurosci, vol.9, pp.1234-1236, 2006. ,
Age-related proteostasis and metabolic alterations in Caspase-2-deficient mice, Cell Death Dis, vol.6, 1615. ,
Structure and mechanism of interleukin-1 beta converting enzyme, Cell Death Dis, vol.7, pp.270-275, 1994. ,
Death receptor signal transducers: nodes of coordination in immune signaling networks, Nat. Immunol, vol.10, pp.348-355, 2009. ,
Caspase-3 regulates cell cycle in B cells: a consequence of substrate specificity, Nat. Immunol, vol.4, pp.1016-1022, 2003. ,
Structural approach of the mechanism of inhibition of alpha-chymotrypsin by coumarins, Bioorg. Med. Chem. Lett, vol.12, pp.1109-1112, 2002. ,
Caspase-dependent apoptotic pathways in CNS injury, Mol. Neurobiol, vol.24, pp.131-144, 2001. ,
Expression of active caspase-3 in mitotic and postmitotic cells of the rat forebrain, J. Comp. Neurol, vol.433, pp.4-22, 2001. ,
The IAP family: endogenous caspase inhibitors with multiple biological activities, Cell Res, vol.10, pp.169-177, 2000. ,
Molecular mechanism and regulation of autophagy, Acta Pharmacol. Sin, vol.26, pp.1421-1434, 2005. ,
Bid, a BH3-only multi-functional molecule, is at the cross road of life and death, Gene, vol.369, pp.7-19, 2006. ,
Kallikrein-related peptidase 6 exacerbates disease in an autoimmune model of multiple sclerosis, Biol Chem, vol.397, pp.1277-1286, 2016. ,
Mechanism of procaspase-8 activation by c-FLIPL, Proc. Natl. Acad. Sci. U.S.A, vol.106, pp.8169-8174, 2009. ,
Apoptosis in the nervous system, Nature, vol.407, pp.802-809, 2000. ,
The C. elegans cell death gene ced-3 encodes a protein similar to mammalian interleukin-1 beta-converting enzyme, Cell, vol.75, pp.641-652, 1993. ,
URL : https://hal.archives-ouvertes.fr/hal-02178577
Role of the executioner caspases during lens development, J. Biol. Chem, vol.280, pp.30263-30272, 2005. ,
The size-dependent apoptotic effect of titanium dioxide nanoparticles on endothelial cells by the intracellular pathway, Environ. Toxicol, 2018. ,
Caspase Activation Is Required for Terminal Erythroid Differentiation, J Exp Med, vol.193, pp.247-254, 2001. ,
Caspase-2 deficiency enhances aging-related traits in mice, Mech. Ageing Dev, vol.128, pp.213-221, 2007. ,
Nuclear Condensation during Mouse Erythropoiesis Requires Caspase-3-Mediated Nuclear Opening, Dev. Cell, vol.36, pp.498-510, 2016. ,
Caspase-2 cleavage of tau reversibly impairs memory, Nat. Med, vol.22, pp.1268-1276, 2016. ,
Caspases: their intracellular localization and translocation during apoptosis, Molecular Neurodegeneration, vol.1, pp.644-651, 1999. ,
Shrinkage of dendritic spines associated with long-term depression of hippocampal synapses, Neuron, vol.44, pp.749-757, 2004. ,
Novel compounds and their use as selective inhibitors of Caspase-2 ,
, Toward a selective irreversible Caspase-2 inhibitor, Liste des publications
Piperlongumine and some of its analogs inhibit selectively the human immunoproteasome over the constitutive proteasome, Biochem. Biophys. Res. Commun, vol.496, pp.961-966, 2018. ,
Insights into the activity control of the kallikrein-related peptidase 6: small-molecule modulators and allosterism, Biol. Chem, vol.399, pp.1073-1078, 2018. ,
, Inhibition of the Inflammasome NLRP3 by Arglabin Attenuates Inflammation, Protects Pancreatic ?-Cells from Apoptosis, and Prevents Type, 2016.
URL : https://hal.archives-ouvertes.fr/hal-01544052
, Diabetes Mellitus Development in ApoE2Ki Mice on a Chronic High-Fat Diet, J. Pharmacol. Exp. Ther, vol.357, pp.487-494
, , 2015.
Insights into the activity control of the kallikrein-related peptidase 6: small-molecule modulators and allosterism, 2018. ,
Toward a selective irreversible Caspase-2 inhibitor. 24th Conference of the European Cell Death Organization, Cell Death in Health and Disease, 2016. ,
,
Inhibiting preferentially Caspase-2 with a new irreversible pentapeptide derivate, Colloque Enzymes et Biocatalyse ,
, Dans ce contexte, des études récentes ont contribué à la validation de la CASP-2 en tant que cible thérapeutique potentielle de la maladie d'Alzheimer. Par conséquent, le développement d'inhibiteurs spécifiques constituerait des outils pharmacologiques qui permettraient de mieux appréhender les rôles de cette protéase dans la physiologie et pathologie du neurone. Les inhibiteurs de Caspases actuels sont majoritairement des séquences tétra ou pentapeptidiques qui reproduisent les motifs préférentiellement reconnus par les différents membres. Par exemple, la CASP-2 reconnait un motif pentapeptidique VDVAD qui est aussi reconnu par les CASP-3 et -7. Dans le cadre de ce travail de thèse, trois stratégies d'identification d'inhibiteurs ont été suivies ; (i) une approche de conception rationnelle de peptides inhibiteurs ciblant le site actif, (ii) conception in silico de peptides inhibiteurs de l'interface de dimérisation, (iii) criblage aléatoire et rationnel de petites molécules organiques. Parmi ces stratégies, l'inhibition du site actif s'est révélée être la plus fructueuse. Nous avons ainsi pu démontrer que des variations du résidu Alanine en P2 sur le motif initial VDVAD permettaient d'améliorer les paramètres de sélectivité et d'efficacité. Sur ce constat une série de peptides « LJ » avec des mécanismes d'inhibition variés a été développée. Parmi eux, deux composés LJ2 et LJ3 ont démontré un excellent potentiel inactivateur de la CASP-2, tout en conservant un effet préférentiel sur cette dernière. Nous avons également montré que ces deux composés protègent de la perte synaptique induite par des oligomères Ab1-42 dans des réseaux de neurones reconstruits in vitro, Les Caspases sont des endoprotéases à cystéine connues pour leurs rôles clé dans la régulation de l'apoptose et de l'inflammation. Parmi elles, la Caspase-2 (NEDD-2, ICH-1, CASP-2) est singulière de par ses multiples rôles dans le maintien de la stabilité génomique, la régulation du stress oxydant, la suppression de tumeur et également dans les processus neurodégénératifs aigus et chroniques. D'ailleurs, son rôle en tant qu'initiateur de la mort cellulaire a été démontré dans de nombreux modèles de stress neuronaux
Caspase-2 ; peptides inhibiteurs ; conception rationnelle ; inactivateurs sélectifs ; maladie d'Alzheimer ,