Key Laboratory for Green Chemical Process of Ministry of Education, School of Chemical Engineering and Pharmacy, Wuhan Institute of Technology, Wuhan 430205, PR China.
Key Laboratory for Green Chemical Process of Ministry of Education, School of Chemical Engineering and Pharmacy, Wuhan Institute of Technology, Wuhan 430205, PR China.
Eur J Med Chem. 2019 Jul 15;174:277-291. doi: 10.1016/j.ejmech.2019.04.054. Epub 2019 Apr 24.
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.
自 2012 年以来，入口通道被提议作为 HIV-1 逆转录酶（RT）非核苷逆转录酶抑制剂结合口袋（NNIBP）中的一个新结合位点，大量针对该靶点的 HIV-1 抑制剂如雨后春笋般涌现，旨在发现具有优异抗病毒活性、物理化学性质等的有前途的抑制剂。从 2012 年到 2018 年，不断有许多值得注意的化合物被发现。本文对近年来针对 HIV-1 NNIBP 入口通道的 HIV-1 抑制剂的研究进展进行了综述，为进一步设计 HIV-1 抑制剂提供了有价值的线索和启示。
