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

Main Category: Pharma Industry / Biotech Industry
Also Included In: Pharmacy / Pharmacist;  Biology / Biochemistry
Article Date: 21 Jul 2008 - 7:00 PDT

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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.

Although no FBLD-based drugs are on the consumer market yet, about 10 are now in clinical trials. But whether the new strategy will be judged successful or not may have to wait until 2011, the earliest year that drugs developed from FBLD techniques will hit the market, the article notes.

"Piece by Piece"
Sarah Everts
Click here to view abstract online
Chemical & Engineering News

American Chemical Society
www.acs.org