Novel triacsin C analogs as potential antivirals against rotavirus infections

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dc.contributor.author Kim, Yunjeong
dc.contributor.author George, David
dc.contributor.author Prior, Allan M.
dc.contributor.author Prasain, Keshar
dc.contributor.author Hao, Shuanghong
dc.contributor.author Le, Duy D.
dc.contributor.author Hua, Duy H.
dc.contributor.author Chang, Kyeong-Ok
dc.date.accessioned 2012-06-26T18:34:20Z
dc.date.available 2012-06-26T18:34:20Z
dc.date.issued 2012-06-26
dc.identifier.uri http://hdl.handle.net/2097/13958
dc.description.abstract Recently our group has demonstrated that cellular triglycerides (TG) levels play an important role in rotavirus replication. In this study, we further examined the roles of the key enzymes for TG synthesis (lipogenesis) in the replication of rotaviruses by using inhibitors of fatty acid synthase, long chain fatty acid acyl-CoA synthetase (ACSL), and diacylglycerol acyltransferase and acyl-CoA:cholesterol acyltransferase in association with lipid droplets of which TG is a major component. Triacsin C, a natural ACSL inhibitor from Streptomyces aureofaciens, was found to be highly effective against rotavirus replication. Thus, novel triacsin C analogs were synthesized and evaluated for their efficacies against the replication of rotaviruses in cells. Many of the analogs significantly reduced rotavirus replication, and one analog (1e) was highly effective at a nanomolar concentration range (ED[subscript 50] 0.1 μM) with a high therapeutic index in cell culture. Our results suggest a crucial role of lipid metabolism in rotavirus replication, and triacsin C and/or its analogs as potential therapeutic options for rotavirus infections. en_US
dc.relation.uri http://www.sciencedirect.com/science/article/pii/S0223523412000864 en_US
dc.subject Rotavirus en_US
dc.subject Antivirals en_US
dc.subject Triacsin C analogs en_US
dc.subject Lipogenesis en_US
dc.title Novel triacsin C analogs as potential antivirals against rotavirus infections en_US
dc.type Article (author version) en_US
dc.date.published 2012 en_US
dc.citation.doi doi:10.1016/j.ejmech.2012.02.010 en_US
dc.citation.epage 318 en_US
dc.citation.jtitle European Journal of Medicinal Chemistry en_US
dc.citation.spage 311 en_US
dc.citation.volume 50 en_US
dc.contributor.authoreid ykim en_US
dc.contributor.authoreid dgeorge en_US
dc.contributor.authoreid allanp en_US
dc.contributor.authoreid keshar en_US
dc.contributor.authoreid duyle en_US
dc.contributor.authoreid duy en_US
dc.contributor.authoreid kchang en_US

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