4.7 Review

Progress and prospects on DENV protease inhibitors

期刊

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 117, 期 -, 页码 125-143

出版社

ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2016.04.008

关键词

Dengue; NS2B-NS3 protease; Proteolytic mechanism; Peptide inhibitors; Peptide conjugates; Small molecule inhibitors; Natural products; HTS; HTVS

资金

  1. Department of Biotechnology, Govt. of India [BT/IN/GERMAN/15/DV/2010]

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New treatments are desperately required to combat increasing rate of dengue fever cases reported in tropical and sub-tropical parts of the world. Among the ten proteins (structural and non-structural) encoded by dengue viral genome, NS2B-NS3 protease is an ideal target for drug discovery. It is responsible for the processing of poly protein that is required for genome replication of the virus. Moreover, inhibitors designed against proteases were found successful in Human Immuno-deficiency Virus (HIV) and Hepatitis C Virus (HCV). Complete molecular mechanism and a survey of inhibitors reported against dengue protease will be helpful in designing effective and potent inhibitors. This review provides an insight on molecular mechanism of dengue virus protease and covers up-to-date information on different inhibitors reported against dengue proteases with medicinal chemistry perspective. (C) 2016 Elsevier Masson SAS. All rights reserved.

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