Novel small-molecule inhibitors of transmissible gastroenteritis virus

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

doi:10.1128/AAC.00408-07

Novel small-molecule inhibitors of transmissible gastroenteritis virus

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

^*此作品的通信作者

研究成果: 期刊稿件 › 文章 › 同行評審

14 引文斯高帕斯（Scopus）

摘要

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.

原文	英語
頁（從 - 到）	3924-3931
頁數	8
期刊	Antimicrobial Agents and Chemotherapy
卷	51
發行號	11
DOIs	https://doi.org/10.1128/AAC.00408-07
出版狀態	已出版 - 11 2007
對外發佈	是

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title = "Novel small-molecule inhibitors of transmissible gastroenteritis virus",

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 (3CLpro) inhibition assay with recombinant 3CLpro and a fluorogenic peptide substrate. A series of benzothiazolium compounds were found to have inhibitory activity against TGEV 3CLpro 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.",

author = "Yang, {Cheng Wei} and Yang, {Yung Ning} and Liang, {Po Huang} and Chen, {Chi Min} and Chen, {Wei Liang} and Chang, {Hwan You} and Chao, {Yu Sheng} and Lee, {Shiow Ju}",

year = "2007",

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doi = "10.1128/AAC.00408-07",

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T1 - Novel small-molecule inhibitors of transmissible gastroenteritis virus

AU - Yang, Cheng Wei

AU - Yang, Yung Ning

AU - Liang, Po Huang

AU - Chen, Chi Min

AU - Chen, Wei Liang

AU - Chang, Hwan You

AU - Chao, Yu Sheng

AU - Lee, Shiow Ju

PY - 2007/11

Y1 - 2007/11

N2 - 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 (3CLpro) inhibition assay with recombinant 3CLpro and a fluorogenic peptide substrate. A series of benzothiazolium compounds were found to have inhibitory activity against TGEV 3CLpro 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.

AB - 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 (3CLpro) inhibition assay with recombinant 3CLpro and a fluorogenic peptide substrate. A series of benzothiazolium compounds were found to have inhibitory activity against TGEV 3CLpro 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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U2 - 10.1128/AAC.00408-07

DO - 10.1128/AAC.00408-07

M3 - 文章

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AN - SCOPUS:35848942777

SN - 0066-4804

VL - 51

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JO - Antimicrobial Agents and Chemotherapy

JF - Antimicrobial Agents and Chemotherapy

IS - 11

ER -

Novel small-molecule inhibitors of transmissible gastroenteritis virus

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