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Guo Y, Zhou PP, Zhang SY, et al. Generation of a long-acting fusion inhibitor against HIV-1. Medchemcomm. 2018;9(7):1226-1231doi: 10.1039/c8md00124c.
Guo, Y., Zhou, P. P., Zhang, S. Y., Fan, X. W., Dou, Y. W., & Shi, X. L. (2018). Generation of a long-acting fusion inhibitor against HIV-1. MedChemComm, 9(7), 1226-1231. https://doi.org/10.1039/c8md00124c
Guo, Ye, et al. "Generation of a long-acting fusion inhibitor against HIV-1." MedChemComm vol. 9,7 (2018): 1226-1231. doi: https://doi.org/10.1039/c8md00124c
Guo Y, Zhou PP, Zhang SY, Fan XW, Dou YW, Shi XL. Generation of a long-acting fusion inhibitor against HIV-1. Medchemcomm. 2018 Jun 06;9(7):1226-1231. doi: 10.1039/c8md00124c. eCollection 2018 Jul 01. PMID: 30109011; PMCID: PMC6071707.
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Medchemcomm. 2018 Jun 06;9(7):1226-1231. doi: 10.1039/c8md00124c. eCollection 2018 Jul 01.

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

MedChemComm

Ye Guo, Pan-Pan Zhou, Sen-Yan Zhang, Xiao-Wen Fan, Yu-Wei Dou, Xuan-Ling Shi

Affiliations

  1. School of Pharmacy , Baotou Medical College , Baotou 014060 , China.
  2. Comprehensive AIDS Research Center , School of Medicine , Tsinghua University , Beijing 100084 , China . Email: [email protected].

PMID: 30109011 PMCID: PMC6071707 DOI: 10.1039/c8md00124c

Abstract

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.

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