Recent progress in HIV-1 inhibitors targeting the entrance channel of HIV-1 non-nucleoside reverse transcriptase inhibitor binding pocket

Gu Shuang-Xi; Xiao Ting; Zhu Yuan-Yuan; Liu Gen-Yan; Chen Fen-Er

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Recent progress in HIV-1 inhibitors targeting the entrance channel of HIV-1 non-nucleoside reverse transcriptase inhibitor binding pocket

机译：HIV-1抑制剂的最新进展靶向HIV-1非核苷逆转录酶抑制剂结合口袋的入口通道

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Since the entrance channel was proposed as a new binding site in non-nucleoside reverse transcriptase inhibitor binding pocket (NNIBP) of HIV-1 reverse transcriptase (RT) in 2012, a huge number of HIV-1 inhibitors acting on this target have sprung up, aiming to discover promising inhibitors with excellent antiviral activities, physicochemical properties, and so on. From 2012 to 2018, many noteworthy compounds have been continuously discovered. In this review, the recent progress in HIV-1 inhibitors targeting the entrance channel of HIV-1 NNIBP was summarized and reviewed, which would provide useful clues and inspiration for further design of HIV-1 inhibitors. (C) 2019 Elsevier Masson SAS. All rights reserved.

机译：由于2012年在HIV-1逆转录酶（RT）的非核苷逆转录酶抑制剂结合口袋（NNIBP）中的新结合位点提出了入口通道，因此作用于该目标的大量HIV-1抑制剂涌现，旨在发现有前途的抑制剂，具有优异的抗病毒活性，物理化学性质等。从2012年到2018年，许多值得注意的化合物被持续发现。在本文中，总结和审查了靶向HIV-1 NNIBP的入口通道的HIV-1抑制剂的进展，这将为HIV-1抑制剂的进一步设计提供有用的线索和灵感。（c）2019年Elsevier Masson SAS。版权所有。

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来源
《European Journal of Medicinal Chemistry: Chimie Therapeutique》 |2019年第2019期|共15页
作者
Gu Shuang-Xi; Xiao Ting; Zhu Yuan-Yuan; Liu Gen-Yan; Chen Fen-Er;
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作者单位

Wuhan Inst Technol Key Lab Green Chem Proc Minist Educ Sch Chem Engn &

Pharm Wuhan 430205;

Wuhan Inst Technol Key Lab Green Chem Proc Minist Educ Sch Chem Engn &

Pharm Wuhan 430205;

Wuhan Inst Technol Sch Chem &

Environm Engn Wuhan 430205 Hubei Peoples R China;

Wuhan Inst Technol Key Lab Green Chem Proc Minist Educ Sch Chem Engn &

Pharm Wuhan 430205;

Wuhan Inst Technol Key Lab Green Chem Proc Minist Educ Sch Chem Engn &

Pharm Wuhan 430205;

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原文格式 PDF
正文语种 eng
中图分类药学;
关键词
AIDS; HIV-1; NNRTIs; Entrance channel; Diarylpyrimidines;

机译：艾滋病;艾滋病毒1;nnrtis;入口通道;二芳基嘧啶;

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专利

1. Recent progress in HIV-1 inhibitors targeting the entrance channel of HIV-1 non-nucleoside reverse transcriptase inhibitor binding pocket [J] . Gu Shuang-Xi, Xiao Ting, Zhu Yuan-Yuan, European Journal of Medicinal Chemistry: Chimie Therapeutique . 2019,第期

机译：HIV-1抑制剂的最新进展靶向HIV-1非核苷逆转录酶抑制剂结合口袋的入口通道
2. Structure of the HIV-1 reverse transcriptase Q151M mutant: insights into the inhibitor resistance of HIV-1 reverse transcriptase and the structure of the nucleotide-binding pocket of Hepatitis B virus polymerase [J] . Nakamura Akiyoshi, Tamura Noriko, Yasutake Yoshiaki Acta crystallographica. Section F, Structural biology communications . 2015,第11期

机译：HIV-1逆转录酶的结构Q151M突变体：见解HIV-1逆转录酶的抑制剂抗性以及乙型肝炎病毒聚合酶的核苷酸结合口袋的结构
3. Exploiting the Tolerant Region I of the Non-Nucleoside Reverse Transcriptase Inhibitor (NNRTI) Binding Pocket: Discovery of Potent Diarylpyrimidine-Typed HIV-1 NNRTIs against Wild-Type and E138K Mutant Virus with Significantly Improved Water Solubility and Favorable Safety Profiles [J] . Huang Boshi, Chen Wenmin, Zhao Tong, Journal of Medicinal Chemistry . 2019,第4期

机译：利用非核苷逆转录酶抑制剂（NNRTI）结合口袋的耐受区域I：对野生型和E138K突变病毒的有效二芳基胺类型的HIV-1nNRTIS的发现具有显着改善的水溶解度和有利的安全性
4. A Novel Detection of Non-nucleoside Reverse Transcriptase Inhibitors (NNRTIs) for HIV-1 with AlGaN/GaN High Electron Mobility Transistors [C] . Yen-Wen Kang, Geng-Yen Lee, Jen-Inn Chyi, Symposium on wide bandgap semiconductor materials and devices;Meeting of the Electrochemical Society . 2013

机译：AlGaN / GaN高电子迁移率晶体管对HIV-1的非核苷逆转录酶抑制剂（NNRTIs）的新型检测
5. Binding of the Nonnucleoside Reverse Transcriptase Inhibitor Efavirenz to HIV-1 Reverse Transcriptase Monomers and Dimers. [D] . Braz, Valerie Ann. 2011

机译：非核苷逆转录酶抑制剂依非韦伦对HIV-1逆转录酶单体和二聚体的结合。
6. A computational study for rational HIV-1 non-nucleoside reverse transcriptase inhibitor selection and the discovery of novel allosteric pockets for inhibitor design [O] . Ron Zhi-Hui Chiang, Samuel Ken-En Gan, Chinh Tran-To Su 2018

机译：合理选择HIV-1非核苷逆转录酶抑制剂的计算研究以及发现新颖的变构口袋来设计抑制剂
7. Crystal structure of tert -butyldimethylsilyl-spiroaminooxathioledioxide- thymine (TSAO-T) in complex with HIV-1 reverse transcriptase (RT) redefines the elastic limits of the non-nucleoside inhibitor-binding pocket [O] . Das, Krishna, Bauman, J. D., Rim, A. S., 2015

机译：叔丁基二甲基甲硅烷基-螺氨基氧杂硫代氧化二氧胸腺嘧啶（TSAO-T）与HIV-1逆转录酶（RT）复合的晶体结构重新定义了非核苷抑制剂结合口袋的弹性极限

Recent progress in HIV-1 inhibitors targeting the entrance channel of HIV-1 non-nucleoside reverse transcriptase inhibitor binding pocket

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