Literature DB >> 17709464

Novel small-molecule inhibitors of transmissible gastroenteritis virus.

Cheng-Wei Yang1, Yung-Ning Yang, Po-Huang Liang, Chi-Min Chen, Wei-Liang Chen, Hwan-You Chang, Yu-Sheng Chao, Shiow-Ju Lee.   

Abstract

We used swine testicle (ST) cells infected with transmissible gastroenteritis virus (TGEV) and an indirect immunofluorescent assay with antibodies against TGEV spike and nucleocapsid proteins to screen small-molecule compounds that inhibit TGEV replication. Analogues of initial hits were collected and subjected to a 3CL protease (3CL(pro)) inhibition assay with recombinant 3CL(pro) and a fluorogenic peptide substrate. A series of benzothiazolium compounds were found to have inhibitory activity against TGEV 3CL(pro) and to exert anti-TGEV activities in terms of viral protein and RNA replication in TGEV-infected ST cells, with consequent protection of TGEV-infected ST cells from cytopathic effect by blocking the activation of caspase-3.

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Year:  2007        PMID： 17709464      PMCID： PMC2151441          DOI： 10.1128/AAC.00408-07

Source DB:  PubMed          Journal:  Antimicrob Agents Chemother        ISSN： 0066-4804            Impact factor:   5.191


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