國家衛生研究院 NHRI:Item 3990099045/1156

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Please use this identifier to cite or link to this item: http://ir.nhri.org.tw/handle/3990099045/1156

Title:	Evaluation of metal-conjugated compounds as inhibitors of 3CL protease of SARS-CoV
Authors:	Hsu, JTA;Kuo, CJ;Hsieh, HP;Wang, YC;Huang, KK;Lin, CPC;Huang, PF;Chen, X;Liang, PH
Contributors:	Division of Biotechnology and Pharmaceutical Research
Abstract:	3C-like (3CL) protease is essential for the life cycle of severe acute respiratory syndrome-coronavirus (SARS-CoV) and therefore represents a key anti-viral target. A compound library consisting of 960 commercially available drugs and biologically active substances was screened for inhibition of SARS-CoV 3CL protease. Potent inhibition was achieved using the mercury-containing compounds thimerosal and phenylmercurie acetate, as well as hexachlorophene. As well, 1-10 muM of each compound inhibited viral replication in Vero E6 cell culture. Detailed mechanism studies using a fluorescence-based protease assay demonstrated that the three compounds acted as competitive inhibitors (Ki = 0.7, 2.4, and 13.7 muM for phenylmercuric acetate, thimerosal, and hexachlorophene, respectively). A panel of metal ions including Zn2+ and its conjugates were then evaluated for their anti-3CL protease activities. Inhibition was more pronounced using a zinc-conjugated compound (1-hydroxypyridine-2-thione zinc; K-i = 0.17 muM) than using the ion alone (K-i = 1.1 muM). (C) 2004 Federation of European Biochemical Societies. Published by Elsevier B.V. All rights reserved.
Keywords:	Biochemistry & Molecular Biology;Biophysics;Cell Biology
Date:	2004-09-10
Relation:	FEBS Letters. 2004 Sep;574(1-3):116-120.
Link to:	http://dx.doi.org/10.1016/j.febslet.2004.08.015
JIF/Ranking 2023:	http://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcAuth=NHRI&SrcApp=NHRI_IR&KeyISSN=0014-5793&DestApp=IC2JCR
Cited Times(WOS):	https://www.webofscience.com/wos/woscc/full-record/WOS:000224041600021
Cited Times(Scopus):	http://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=4444368730
Appears in Collections:	[John Tsu-An Hsu] Periodical Articles [Hsing-Pang Hsieh] Periodical Articles [Xin Chen(2002-2015)] Periodical Articles

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