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Article

Development of enhanced HIV-1 non-nucleoside reverse transcriptase inhibitors with improved resistance and pharmacokinetic profiles.

Science advances - 30 May 2025

Wang Zhao, Rumrill Shawn, Kang Dongwei, Guma Samuel Desta, Feng Da, De Clercq Erik, Pannecouque Christophe, Chen Chin Ho, Arnold Eddy, Ruiz Francesc Xavier, Liu Xinyong, Zhan Peng

Abstract excerpt

HIV-1 infection is a manageable chronic condition, with non-nucleoside HIV-1 reverse transcriptase inhibitors (NNRTIs) remaining a cornerstone of antiretroviral therapy. Nevertheless, drug resistance to existing therapeutics is a serious and immediate concern. Using structure-based and scaffold-hopping approaches, we designed evolved diarylpyrimidine analogs targeting reverse transcriptase (RT), exploiting...

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Methodology Data sources Editorial policy Privacy About Contact Helena Bioinformatics

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Source

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Identifiers

PMID: 40446037
DOI: 10.1126/sciadv.adt8916
PMCID: PMC12124364

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