Stapled SC34EK fusion inhibitors with high potency against HIV-1 and improved protease resistance
Stapled SC34EK fusion inhibitors with high potency against HIV-1 and improved protease resistance
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具有高效抗 HIV-1 并改善蛋白酶抗性的装订 SC34EK 融合抑制剂
DOI：
10.1016/j.cclet.2018.03.024
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发表时间：
2018-07
影响因子：
9.1
通讯作者：
Shi Xuan-Ling
中科院分区：
文献类型：
--
作者：
Guo Ye;Fu Li-Li;Fan Xiao-Wen;Shi Xuan-Ling
HIV fusion inhibitors are promising therapeutic agents for AIDS treatment. One fusion inhibitor has been approved as anti-HIV drug, while more of them are in preclinical studies or clinical trials. Highly active fusion inhibitors with excellent pharmacokinetic properties are still needed for development of anti-HIV drugs. We found that all-hydrocarbon staples inserted in SC34EK could not only enhance the inhibitory activity of inhibitors against HIV-1, but also improve protease resistance. Further study revealed that SC34EK-1 containing a staple was a potent fusion inhibitor with IC50value of 0.04–6.4 nmol/L towards diverse HIV-1 subtypes and half-life value of 112 min against protease hydrolysis. X-ray crystallography studies indicated that introduction of a hydrocarbon staple in SC34EK could make the amino acid at the interaction surface form perfect conformation to promote inhibitor peptide interacting with target.
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DOI：
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发表时间：
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期刊：
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