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GPCR Drug Discovery
MRC Laboratory of Molecular Biology, UK
GPCRs have been implicated in a number of diseases and serve as an attractive target for the development of new therapeutics. Drugs that target GPCRs currently form the largest contribution to the overall sales across the world (27%). The annual revenue of drugs that target GPCRs totals around US$ 222... read morebillion. More than 50 different GPCRs are currently in various stages of clinical trials for drug development against a number of disorders. Thus there is enormous interest and promise for the development of new and better drugs, especially with the recent exciting developments that provide unprecedented insights into the structure and function of several medically important GPCRs.
The key objective of this series is to introduce drug discovery for GPCRs, discuss emerging concepts in GPCR signalling and using them for novel therapeutic avenues. The first set of talks will set the stage for how the recent structures are allowing drug discovery among GPCR targets. The second will discuss computational and experimentalapproaches for screening compound libraries, as well as use of model organisms and biophysical approaches for discovering GPCR drugs. The third will cover the concept of allosteric modulators, biased ligands all of which can minimise side effects and strengthen the desired response against a GPCR target. The fourth will discuss how the newly described mechanisms of GPCR signalling can be used for developing new drugs. The final set of talks will discuss the importance of natural variation in the human population and their response to the common drugs, with an emphasis on precision medicine.