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New opportunities for covalent drugs published by Avila scientists
Date:4/1/2011

WALTHAM, MA April 1, 2011 Avila Therapeutics, Inc., a biotechnology company developing novel targeted covalent drugs, today announced the publication of a scientific review article in Nature Reviews Drug Discovery titled "The Resurgence of Covalent Drugs" (www.nature.com/reviews/drugdisc, Vol. 10, April 2011, Singh, J.). This article discusses the broad opportunities for covalent drugs and how structural bioinformatics coupled with structure-based drug design can enable the design of highly selective covalent drugs with unique therapeutic properties for treating diseases.

"Many important and widely-used medicines work through a covalent mechanism of action," commented Juswinder Singh, PhD, Avila's Chief Scientific Officer and lead author on the publication. "Until recently, such covalent drugs were discovered by chance. However, today it is possible to design highly-specific covalent drugs by systematically applying rational drug design techniques and leveraging the vastly greater availability of structural information on disease targets. We anticipate the next few years will see an emergence of innovative covalent drugs that can solve problems that have been challenging for traditional medicinal chemistry approaches."

The Nature Reviews Drug Discovery article examines the prevalence of covalent drugs, safety considerations, mechanistic and pharmacological features, and approaches to design and optimization of targeted covalent inhibitors. Key points include:

  • Covalent drugs have made a major positive impact on human health, and there are dozens of covalent drugs on the market worldwide including broadly used medicines such as aspirin, clopidogrel (Plavix), lansoprazole (Prevacid) and esomeprazole (Nexium).

  • Despite the many successful covalent drugs, principles for the rational design of these molecules have only recently emerged. A
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Contact: Kathryn Morris
kathryn@theyatesnetwork.com
845-635-9828
Yates Public Relations
Source:Eurekalert

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