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

• Published in: European journal of medicinal chemistry Vol. 174; pp. 277 - 291
• Main Authors: Gu, Shuang-Xi, Xiao, Ting, Zhu, Yuan-Yuan, Liu, Gen-Yan, Chen, Fen-Er
• Format: Journal Article
• Language: English
• Published: France Elsevier Masson SAS 15.07.2019
• Subjects: AIDS; Animals; Anti-HIV Agents - chemistry; Anti-HIV Agents - pharmacology; Binding Sites; Cell Line, Tumor; Diarylpyrimidines; Entrance channel; Heterocyclic Compounds - chemistry; Heterocyclic Compounds - pharmacology; HIV Reverse Transcriptase - antagonists & inhibitors; HIV Reverse Transcriptase - chemistry; HIV-1; HIV-1 - drug effects; Humans; Molecular Docking Simulation; NNRTIs; Reverse Transcriptase Inhibitors - chemistry; Reverse Transcriptase Inhibitors - pharmacology; HIV-1; Diarylpyrimidines; AIDS; Entrance channel; NNRTIs
• ISSN: 0223-5234; 1768-3254
• DOI: 10.1016/j.ejmech.2019.04.054

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. [Display omitted] •The recent progress in HIV-1 inhibitors targeting the entrance channel of HIV-1 NNIBP was reviewed.•The prospect of HIV-1 inhibitors targeting the entrance channel of HIV-1 NNIBP was discussed.•The directions of future efforts were pointed out.