In situ Click Chemistry: a Powerful Means for Lead Discovery by K Barry Sharpless and Roman Manetsch - Featured Article From Expert Opinion
LONDON, November 20 /PRNewswire/ -- In the current issue of Expert Opinion on Discovery, Professor K Barry Sharpless (winner of the 2001 Nobel Prize in Chemistry; W. M. Keck Professor of Chemistry, The Scripps Research Institute) and Dr Roman Manetsch (Assistant Professor, Department of Chemistry, University of South Florida) provide their expert opinion on how in situ click chemistry has the potential to emerge as a powerful means for lead discovery through combining both the synthesis and screening of libraries of low molecular weight compounds into a single step.
In situ click chemistry is a novel kinetically controlled target-guided synthesis approach to lead discovery. Over the past 10 years, there has been a decline in the rate of submission and introduction of new drug candidates, a disturbing trend that, according to Sharpless and Manetsch, "provokes questions about the effectiveness of the existing approaches to drug discovery."
Sharpless and Manetsch suggest that "the new in situ approach to inhibitor discovery may help medicinal chemists by providing a dynamic search method for tracking and intercepting the dynamic biocatalysts."
SHARPLESS KB, MANETSCH R: In situ click chemistry: a powerful means for lead discovery. Expert Opin. Drug Discov. (2006) 1(6): 525-538.
About Expert Opinion
For over a decade, the Expert Opinion series has provided systematic and authoritative reviews to support every stage of the drug discovery and R&D pipeline from target to market. Each of the ten journals in the series covers a specific aspect of the pharmaceutical pipeline.
The series contains the following journals: Expert Opinion on Biological Therapy, Expert Opinion on Drug Delivery, Expert Opinion on Drug Metabolism & Toxicology, Expert Opinion on Drug Safety, Expert Opinion on Emerging Drugs, Expert Opinion on Investigational Drugs, Expert Opinion on Pharmacotherapy, Expert Opinion on Therapeutic Patents, Expert Opinion on Therapeutic Targets and Expert Opinion on Drug Discovery.
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