An analog of camptothecin inactive against Topoisomerase I is broadly neutralizing of HIV-1 through inhibition of Vif-dependent APOBEC3G degradation

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• 作者：Ryan P. Bennett^a ; Ryan A. Stewart^a ; Priscilla A. Hogan^b ; Roger G. Ptak^b ; Marie K. Mankowski^b ; Tracy L. Hartman^c ; Robert W. Buckheit Jr.^c ; Beth A. Snyder^b ; Jason D. Salter^a ; Guillermo A. Morales^d ; Harold C. Smith^a ; ^e ; ^{harold.smith@rochester.edu}
• 刊名：Antiviral Research
• 出版年：2016
• 出版时间：December 2016
• 年：2016
• 卷：136
• 期：Complete
• 页码：51-59
• 全文大小：1946 K
• 卷排序：136

文摘

This study identifies Vif as the TOP1 independent anti-HIV target of CPT analogs. Vif multimerization and Vif-dependent A3G and A3F degradation are inhibited by the CPT analog, O2-16. This Vif inhibition leads to A3G packaging and HIV hypermutations and is broadly neutralizing to all HIV clades. A highly active Vif antagonist enables a potential new combinatorial strategy for therapy, prevention and eradication.