Oxford FOP Research Report - Summer 2012

Wednesday, 10 October, 2012 (All day)

Can malaria research benefit FOP?

This quarter has witnessed some exciting and most unexpected developments. The first step in drug discovery is often a screen of a chemical library to identify small drug-like molecules that bind to a target protein. The Oxford FOP Research Team is very fortunate to have the Structural Genomics Consortium (SGC) as its host laboratory.

The SGC, a non-profit international public-private partnership, has put together a valuable library of drug-like molecules collected from different chemical suppliers. As previously described, our screening of this collection allowed us to identify a new ACVR1/ALK2 inhibitor referenced as K02288. This starting point is known as a “hit” molecule. Typically, several years are required to optimise a “hit” into a potential lead drug candidate. The Oxford FOP hit “K02288” was purchased from a UK supplier named BioFocus. By serendipity, an expert in chemical biology at SGC, Dr Oleg Fedorov, noticed that the same BioFocus chemical library was being used by the “Medicines for Malaria Venture” (MMV).

In comparison to FOP, malaria attracts huge research investment as one of the most widespread infectious diseases of our time, with half of the world’s population at risk. MMV is a separate non-profit foundation created to discover, develop and deliver new affordable antimalarial drugs through effective public-private partnership. Remarkably, their “hit” molecule was a near carbon copy of our FOP “hit” (see Figure 1 below). Most encouragingly, they have optimised their hit into a drug candidate which will enter clinical trials in 2013.


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