CHISHIKI

Platform Technology

Enabling FBDD for GPCRs with Protein Engineering and Biophysics

By Rob Cooke | Apr 5, 2019

Conference

Fragments 2019
24 – 26 March 2019
Cambridge, United Kingdom
Royal Society of Chemistry |  Biological & Medicinal Chemistry Sector

Conference Website

Presentation Summary

Fragment-based drug discovery (FBDD) for G-protein coupled receptors (GPCRs) is a reality, enabled by structural and biophysical approaches. There is an increasing number of structures of GPCRs revealing new sites for modulation. Structures will play key roles in optimising allosteric modulators as well as determining which sites of modulation show the best potential. Fragments have been found to target allosteric sites in several GPCRs and may represent a fruitful way to identify new allosteric agents. 

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