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UMass Chan Affiliations
Department of Biochemistry and Molecular PharmacologyDocument Type
Journal ArticlePublication Date
2016-04-15Keywords
BiochemistryMedicinal Chemistry and Pharmaceutics
Medicinal-Pharmaceutical Chemistry
Molecular Biology
Structural Biology
Virology
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Show full item recordAbstract
Drug resistance is a major problem in health care, undermining therapy outcomes and necessitating novel approaches to drug design. Extensive studies on resistance to viral protease inhibitors, particularly those of HIV-1 and hepatitis C virus (HCV) protease, revealed a plethora of information on the structural and molecular mechanisms underlying resistance. These insights led to several strategies to improve viral protease inhibitors to counter resistance, such as exploiting the essential biological function and leveraging evolutionary constraints. Incorporation of these strategies into structure-based drug design can minimize vulnerability to resistance, not only for viral proteases but for other quickly evolving drug targets as well, toward designing inhibitors one step ahead of evolution to counter resistance with more intelligent and rational design.Source
Trends Microbiol. 2016 Apr 15. pii: S0966-842X(16)30002-6. doi: 10.1016/j.tim.2016.03.010. [Epub ahead of print] Link to article on publisher's websiteDOI
10.1016/j.tim.2016.03.010Permanent Link to this Item
http://hdl.handle.net/20.500.14038/48864PubMed ID
27090931Related Resources
Link to article in PubMedae974a485f413a2113503eed53cd6c53
10.1016/j.tim.2016.03.010