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Issue 7, 2018
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Generation of a long-acting fusion inhibitor against HIV-1

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AIDS has evolved from a fatal infectious disease to a manageable chronic disease under the treatment of anti-AIDS medications. HIV fusion inhibitors with high activity, low side effects and strong selectivity are promising drugs against HIV. Only one fusion inhibitor is currently approved, thereby highly active long-acting fusion inhibitors need to be developed for long-term AIDS treatment. Here, we synthesised MT-SC22EK (a small HIV fusion inhibitor) derivatives containing 1–2 staples to improve its stability. Antiviral activity studies showed that MT-SC22EK-2 with two staples exhibited potent inhibitory activity against HIV-1 standard strains and Chinese epidemic strains, and at the same time, MT-SC22EK-2 presented strong anti-T20 resistance. Surprisingly, MT-SC22EK-2 possessed excellent protease stability with a half-life of 3665 min. MT-SC22EK-2 is a potential HIV fusion inhibitor considered as a long-acting anti-HIV drug candidate.

Graphical abstract: Generation of a long-acting fusion inhibitor against HIV-1

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The article was received on 04 Mar 2018, accepted on 29 May 2018 and first published on 06 Jun 2018

Article type: Research Article
DOI: 10.1039/C8MD00124C
Citation: Med. Chem. Commun., 2018,9, 1226-1231
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    Generation of a long-acting fusion inhibitor against HIV-1

    Y. Guo, P. Zhou, S. Zhang, X. Fan, Y. Dou and X. Shi, Med. Chem. Commun., 2018, 9, 1226
    DOI: 10.1039/C8MD00124C

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