Sunday, November 07, 2004

Intelligent Drug Design

Syrrx, a drug design company, just released the 3D structure for their main target, human 11(beta)-hydroxysteroid dehydrogenase type-1 (HSD-1). Inhibitors of this enzyme have potential in the treatment of type II diabetes. Why is this interesting? Consider the drug design pipeline :

Traditionally, the process to identify new compounds with interesting medical properties was based on luck; throw a bunch of randomly synthetized molecules, or earth/bio/plant samples, on a column containing your target of interest, and retain those who bind. Then check for medicinal properties, do some animal testing, check for dangerous degradation products by the liver, various pharmacokinetics parameters, do some modifications to improve it all... 10 years and 800 millions US$ later, you have a new drug!

When I first learned about the 'random' drug design approach, I remember being quite disappointed ("Is that the best we can do?"). The new trend is intelligent drug design. You determine the structure of the enzyme / receptor you're targeting, based on previous studies. Then, you design a compound that will bind to the active site (or prevent dimerization, etc.) with chemical groups that will assure good systemic distribution... much more intelligent than the old process, and far less random and costly! As you can guess, Bioinformatics play a crucial role in intelligent drug design... so it's good to see it become reality.



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