期刊
SCIENTIFIC REPORTS
卷 8, 期 -, 页码 -出版社
NATURE PUBLISHING GROUP
DOI: 10.1038/s41598-018-26318-3
关键词
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资金
- National Key Research and Development program of China [2016YFD0500307]
- National Natural Science Foundation of China [81271844, 31470272, 81361128017]
- National Mega-project for Innovative Drugs [2012ZX09102101-018]
- CAMS Innovation Fund for Medical Sciences [CAMS-I2M-1-012, 2016-I2M-2-002]
- National Mega-Project for Significant new drug discovery [2018ZX09711003-002-002]
- Beijing Key Laboratory of Emerging Infectious Diseases
Human APOBEC3G (hA3G) is a restriction factor that inhibits human immunodeficiency 1 virus (HIV-1) replication. The virally encoded protein Vif binds to hA3G and induces its degradation, thereby counteracting the antiviral activity of hA3G. Vif-mediated hA3G degradation clearly represents a potential target for anti-HIV drug development. Herein, we have performed virtual screening to discover small molecule inhibitors that target the binding interface of the Vif/hA3G complex. Subsequent biochemical studies have led to the identification of a small molecule inhibitor, IMB-301 that binds to hA3G, interrupts the hA3G-Vif interaction and inhibits Vif-mediated degradation of hA3G. As a result, IMB-301 strongly inhibits HIV-1 replication in a hA3G-dependent manner. Our study further demonstrates the feasibility of inhibiting HIV replication by abrogating the Vif-hA3G interaction with small molecules.
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