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Screening Of Tiny Chemical Fragments May Pay Big Dividends In Drug Discovery

22 Jul 08

Scientists who develop new drugs are closely following the progress through clinical trials of a cache of drugs developed with counter-intuitive strategy that defies conventional wisdom, according to an article scheduled for the July 21 issue of Chemical & Engineering News.

In the cover story, C&EN Associate Editor Sarah Everts points out that in traditional drug discovery approaches researchers sort through millions of large, full-sized molecules to find promising substances that can bind strongly to their intended biological targets, a strategy called high-throughput screening (HTS). In so-called fragment-based lead discovery (FBLD), researchers instead sort through a few thousand tiny chemical fragments that bind weakly to their targets. After screening, these weakly-binding fragments are then expanded into more potent substances by adding chemical groups or linking a sequence of promising fragments together piece by piece, the article states.

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