一种靶向共价的HIV-1融合小分子抑制剂。
A targeted covalent small molecule inhibitor of HIV-1 fusion.
作者信息
Zhou Guangyan, He Li, Li Kathy H, Pedroso Cássio C S, Gochin Miriam
机构信息
Department of Basic Sciences, Touro University California, 1310 Club Drive, Mare Island, Vallejo, CA 94592, USA.
Department of Pharmaceutical Chemistry, UCSF School of Pharmacy, San Francisco, CA 94143, USA.
出版信息
Chem Commun (Camb). 2021 May 6;57(37):4528-4531. doi: 10.1039/d1cc01013a.
Abstract
We describe a low molecular weight covalent inhibitor targeting a conserved lysine residue within the hydrophobic pocket of HIV-1 glycoprotein-41. The inhibitor bound selectively to the hydrophobic pocket and exhibited an order of magnitude enhancement of anti-fusion activity against HIV-1 compared to its non-covalent counterpart. The findings represent a significant advance in the quest to obtain non-peptide fusion inhibitors.
摘要
我们描述了一种低分子量共价抑制剂，它靶向HIV-1糖蛋白-41疏水口袋内的一个保守赖氨酸残基。该抑制剂选择性地结合到疏水口袋，并与其非共价对应物相比，对HIV-1的抗融合活性增强了一个数量级。这些发现代表了在寻求非肽类融合抑制剂方面的重大进展。
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