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:
Based on this review article, it is apparent that structural bioinformatics approaches, coupled with structure-based drug design, may enable the engineering of highly selective covalent drugs and a resurgence of interest in this important class of therapeutics.
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Yates Public Relations