Integrase Strand Transfer Inhibitors Are Effective Anti-HIV Drugs |
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| Authors: | Steven J. Smith Xue Zhi Zhao Dario Oliveira Passos Dmitry Lyumkis Terrence R. Burke Jr. Stephen H. Hughes |
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| Affiliation: | 1.HIV Dynamics and Replication Program, Center for Cancer Research, National Cancer Institute, Frederick, MD 21702, USA;2.Chemical Biology Laboratory, Center for Cancer Research, National Cancer Institute, Frederick, MD 21702, USA; (X.Z.Z.); (T.R.B.J.);3.Laboratory of Genetics, The Salk Institute for Biological Studies, La Jolla, CA 92037, USA; (D.O.P.); (D.L.);4.Department of Integrative Structural and Computational Biology, The Scripps Research Institute, La Jolla, CA 92037, USA |
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| Abstract: | Integrase strand transfer inhibitors (INSTIs) are currently recommended for the first line treatment of human immunodeficiency virus type one (HIV-1) infection. The first-generation INSTIs are effective but can select for resistant viruses. Recent advances have led to several potent second-generation INSTIs that are effective against both wild-type (WT) HIV-1 integrase and many of the first-generation INSTI-resistant mutants. The emergence of resistance to these new second-generation INSTIs has been minimal, which has resulted in alternative treatment strategies for HIV-1 patients. Moreover, because of their high antiviral potencies and, in some cases, their bioavailability profiles, INSTIs will probably have prominent roles in pre-exposure prophylaxis (PrEP). Herein, we review the current state of the clinically relevant INSTIs and discuss the future outlook for this class of antiretrovirals. |
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| Keywords: | HIV integration INSTIs drug resistance antiviral therapy |
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