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The SARfaris: GPCR, Kinase, ADME

Tuesday, 3 July 2012

Seminar: Discovery of Viagra/Revatio (aka sildenafil aka UK-92480)

A reminder of an on campus, open, seminar from Andy Bell (now at Imperial College), detailing the discovery and development of UK-92,480 (also known as sildenafil and even better known as V1agra and R3vat10). Andy was one of the medicinal chemists and inventors on the PDE-5 inhibitor programme at Pfizer, and the story covers many aspects of drug discovery including, of course, the discovery of the side effect, and also one where the pharmacology led to many new molecular insights into NO signalling and PDE biology.

There are many myths about the discovery of V1agra, so this is a rare opportunity to hear the exciting story first-hand.

Here's Andy's abstract....

"Viagra™ (sildenafil) is a unique example of a chemical tool being used to
discover the linkage between a biological mechanism and a disease through
clinical trials. The presentation will describe the discovery of sildenafil
and its use in defining the role of cGMP phosphodiesterases (particularly
PDE5) in human diseases such as Male Erectile Dysfunction (MED) and Pulmonary
Arterial Hypertension (PAH). These clinical studies, combined with the
discovery of additional PDE isoforms, were used to define a desirable profile
for subsequent 2nd generation PDE5 inhibitors. The impact of structural
biology and high throughput screening on the discovery of further clinical
candidates will also be discussed."

The seminar  is on Tuesday July 17th 2012 at 2pm in room M203 (room change alert for those who put it in their diary earlier) - you will need to mail me in order to get registered with campus security if you don't work on campus. If you do, you can just turn up.

Andy will also be giving a more detailed technical seminar on screening file analysis, diversity, chemical space, etc - again, let me know if you are interested in attending this too......

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