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Méthodes RMN pour la découverte de nouveaux ligands ciblant les récepteurs couplés aux protéines G

Claire Raingeval 1
1 CRMN - Centre de Résonance Magnetique Nucleaire
ICBMS - Institut de Chimie et Biochimie Moléculaires et Supramoléculaires
Abstract : G protein-coupled receptors (GPCRs) are the largest class of membrane proteins in the human genome. GPCRs act as cell surface signalling proteins and respond to a variety of external signals. They play a pivotal role in many physiological functions and are therefore associated with a multitude of diseases, including cardiovascular, metabolic, neurodegenerative, psychiatric, and oncologic diseases. The 2012 noble Prize in Chemistry was awarded jointly to Robert J. Lefkowitz and Brian K. Kobilka for studies of GPCRs, highlighting the importance of this protein superfamily. GPCRs constitute also the most important family of drug targets in the human body, with 30% of current drugs acting on GPCRs. However, drug discovery targeting GPCRs remains difficult, owing to the restricted structural information on GPCRs related to the instability of these proteins when isolated from their cell membrane environments. There is also a lack of knowledge for the structural and functional consequences of the interactions of small-molecule compounds with GPCR. The aim is to develop methods to study and characterize a full GPCR solubilized in detergents or in native lipid bilayers, both in its free form and in small molecule bound forms, using liquid-state NMR experiments. The aim is to develop NMR-based approaches that will strongly impact the structure-based drug discovery process for the GPCR family
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Submitted on : Thursday, January 30, 2020 - 1:56:17 PM
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Claire Raingeval. Méthodes RMN pour la découverte de nouveaux ligands ciblant les récepteurs couplés aux protéines G. Autre. Université de Lyon, 2019. Français. ⟨NNT : 2019LYSE1215⟩. ⟨tel-02460994⟩

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