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G-Protein coupled receptors in drug discovery

Published on February 4, 2014   42 min

A selection of talks on Biochemistry

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0:00
Hello, and welcome to the Henry Stewart lecture series on Small Molecule Drug Discovery. My name is Mark Wigglesworth, and I'm the Director at the Global High Throughput Screening organization within AstraZeneca. Today I have a presentation for you on, G-Protein Coupled Receptors in Drug Discovery. I've had a long interest in both screening and in G-protein coupled receptors. I hope the presentation that follows will give you some insight into both and how their impacting to discovery both today and in the future.
0:36
I'm going to start with some information which I'm sure you're all already aware of, and that is GPCRs, the size of the super family, and that this is actually a very significant opportunity for all of us that work within drug discovery. The graph that you're looking at on this slide simply shows the number of proteins targets within some major target super families. And GPCR showed, on this graph, as having around 800 family members, by far the largest single protein class that are successfully targeted by drugs today.
1:17
And as drug targets, GPCRs are involved in almost all diseases throughout the human body. Perhaps more importantly for drug discovery, of course, is that this family of proteins are highly tractable and highly profitable. They are the most exploited class of drug targets, with approximately 36% of all drugs targeting them. And just taking a moment to think about that, that's quite phenomenal. The effects that this target class and drugs acting upon them has had on human health historically is very significant. Indeed, according to data from IMS Health, six out of the top 20 drugs in terms of global sales in 2010, targeted GPCRs. That is 30%.

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