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Libraries for target pathway id pathway modulators eg

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Unformatted text preview: he target protein in vitro, the small molecule may also inhibit other proteins that cause undesired effects (let). When both discovery and use occur in vivo, it is possible to idenBfy small molecules that perform the desired funcBon, someBmes through complementary acBviBes against mulBple protein targets (right). (b) Some clinically successful compounds funcBon through beneficial promiscuity. Although staBns lower cholesterol and provide a cardiac benefit, noncholesterol effects of the staBns also appear to be essenBal. Lowering cholesterol alone appears to be insufficient to provide a cardiac benefit. 10 5/7/13 Protein Diversity •  •  The accumulated por}olio of the pharmaceuBcal industry is esBmated to target 483 proteins (Drews, Nature Biotechnology, 1997). Concept of druggable genome = the number of proteins with potenBal drug ­binding domains at which small ­ molecule therapeuBc agents could act. The esBmate is about 10,000 genes contain such proteins. Nearly half of the targets fall into just six gene families: G ­protein ­coupled receptors (GPCRs), serine/threonine and tyrosine protein kinases,...
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