Citation: Guo Ye, Fu Lili, Fan Xiaowen, Shi Xuanling. Synthesis and Anti-HIV-1 Activity of Stapled HIV-1 Fusion Inhibitors[J]. Chinese Journal of Organic Chemistry, ;2018, 38(5): 1267-1270. doi: 10.6023/cjoc201710033 shu

Synthesis and Anti-HIV-1 Activity of Stapled HIV-1 Fusion Inhibitors

Guo Ye ^a ,
Fu Lili ^b ,
Fan Xiaowen ^a ,
Shi Xuanling ^b,,

a.
School of Pharmacy, Baotou Medical College, Baotou 014060
b.
Comprehensive AIDS Research Center, School of Medicine, Tsinghua University, Beijing 100084

Corresponding author: Shi Xuanling, shixuanlingsk@mail.tsinghua.edu.cn
Received Date: 25 October 2017
Revised Date: 8 January 2018
Available Online: 18 May 2018
Fund Project: the Doctoral Science Foundation of Baotou Medical College BSJJ201620Project supported by the National Natural Science Foundation of China (No. 21602121), the Natural Science Foundation of Inner Mongolia (No. 2016BS0201) and the Doctoral Science Foundation of Baotou Medical College (No. BSJJ201620)the National Natural Science Foundation of China 21602121the Natural Science Foundation of Inner Mongolia 2016BS0201

Figures(3)

Sifuvirtide (SFT) is a potent anti-HIV-1 (human immunodeficiency virus-1) fusion inhibitor and it shows higher potency and pharmacokinetic stability than the approved fusion inhibitor T20. At present, sifuvirtide has completed the phase Ⅱb clinical trial in China. In this study, SFT-1 and SFT-2 were synthesized via all-hydrocarbon cross-linking system with replacing the original salt bridge in SFT by hydrocarbon covalent bond, using sifuvirtide as template. The anti-HIV-1 activity was evaluated for all synthetic peptides. The results indicated that SFT stapled peptides displayed high inhibitory activity against seven HIV-1 pseudovirus strains, and SFT-1 showed the highest inhibitory activity against B' and B'C subtype virus strains, SFT-2 showed the highest inhibitory activity against B, CRF01_AE and CRF08_BC subtype virus strains.
- sifuvirtide,
- HIV-1 fusion inhibitor,
- hydrocarbon stapling,
- anti-HIV-1 activity
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