Impact of GPCR Structures on Drug Discovery | Zendy

Miles Congreve | Zendy; Chris de Graaf | Zendy; Nigel A. Swain | Zendy; Christopher G. Tate | Zendy

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Impact of GPCR Structures on Drug Discovery

Author(s) -

Miles Congreve,

Chris de Graaf,

Nigel A. Swain,

Christopher G. Tate

Publication year - 2020

Publication title -

cell

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 26.304

H-Index - 776

eISSN - 1097-4172

pISSN - 0092-8674

DOI - 10.1016/j.cell.2020.03.003

Subject(s) - biology , drug discovery , g protein coupled receptor , computational biology , drug , bioinformatics , pharmacology , receptor , genetics

Structures of 70 unique G protein-coupled receptors (GPCRs) have been determined, with over 370 structures in total bound to different ligands and the receptors in various conformational states. Structure-based drug design has been applied to an increasing number of GPCR targets over the past decade and now a few of these drug candidates have entered clinical trials. Given the length of time required for a drug to reach the market, there are no documented examples of licensed drugs being developed with the aid of a structure, but this is likely to change as current efforts come to fruition.

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