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Novel indolylarylsulfone derivatives as covalent HIV-1 reverse transcriptase inhibitors specifically targeting the drug-resistant mutant Y181C.

Bioorganic & medicinal chemistry - 15 Jan 2021

Gao Ping, Song Shu, Frutos-Beltrán Estrella, Li Wenxin, Sun Bin, Kang Dongwei, Zou Jinmi, Zhang Jian, Pannecouque Christophe, De Clercq Erik, Menéndez-Arias Luis, Zhan Peng, Liu Xinyong

Abstract excerpt

Non-nucleoside reverse transcriptase inhibitors (NNRTIs) are widely used in combination therapies against HIV-1. However, emergent and transmitted drug resistance compromise their efficacy in the clinical setting. Y181C is selected in patients receiving nevirapine, etravirine and rilpivirine, and together with K103N is the most prevalent NNRTI-associated mutation in HIV-infected patients. Herein, we report on the...

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Methodology Data sources Editorial policy Privacy About Contact Helena Bioinformatics

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Identifiers

PMID: 33352387
DOI: 10.1016/j.bmc.2020.115927

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PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 3 Sept 2026.

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