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Generation of a long-acting fusion inhibitor against HIV-1


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, strong selectivity, are promising drugs against HIV. Only one fusion inhibitor is currently approved, thereby highly active long-acting fusion inhibitors are needed to develop for long-term AIDS treament. Here, we synthesised MT-SC22EK (a small HIV fusion inhibitor) derivatives containing 1-2 staples to impove it stability. Antiviral activity study showed that MT-SC22EK-2 with two staples exhibited the potent inhibitory activity agaisnt HIV-1 standard strains and Chinese epidemic strains, at the same time MT-SC22EK-2 presented the strong anti-T20 resistance. Surprisingly, MT-SC22EK-2 possessed excellent protease stability with the half-life value of 3665 min. MT-SC22EK-2 is the potential HIV fusion inhibitors to be a candidate of long-acting anti-HIV drug.

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Publication details

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, Accepted Manuscript
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    Generation of a long-acting fusion inhibitor against HIV-1

    Y. Guo, P. P. Zhou, X. W. Fan, Y. W. Dou and X. L. Shi, Med. Chem. Commun., 2018, Accepted Manuscript , DOI: 10.1039/C8MD00124C

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