Cryo-EM Structure of HIV-1 Reverse Transcriptase with N-Phenyl-1-(phenylsulfonyl)-1H-1,2,4-triazol-3-amine: A New HIV-1 Non-nucleoside Inhibitor DOI
Megan A. Young, Thomas R. Lane, Renuka Raman

и другие.

ACS Infectious Diseases, Год журнала: 2025, Номер unknown

Опубликована: Апрель 30, 2025

The use of highly active antiretroviral therapy (HAART) has made the human immunodeficiency virus (HIV) a chronic disease rather than terminal disease. Non-nucleoside reverse transcriptase inhibitors (NNRTIs) are an important component HAART, although we seeing clinically relevant drug-resistant mutants such that there is need to develop new molecules. We recently identified class N-phenyl-1-(phenylsulfonyl)-1H-1,2,4-triazol-3-amine HIV-1 NNRTI, with one known as compound 12126065, sub nanomolar (nM) potency in TZM-bl cells (HeLa expressing CD4, CCR5, and CXCR4) no vivo acute or subacute toxicity. now describe cryo-EM structure this molecule (resolution 3.53 Å) compare it analogues other NNRTIs. also synthesis activity five additional compounds, some which have promising against K103N/Y181C (A17) double mutant, will enable design future

Язык: Английский

Cryo-EM Structure of HIV-1 Reverse Transcriptase with N-Phenyl-1-(phenylsulfonyl)-1H-1,2,4-triazol-3-amine: A New HIV-1 Non-nucleoside Inhibitor DOI
Megan A. Young, Thomas R. Lane, Renuka Raman

и другие.

ACS Infectious Diseases, Год журнала: 2025, Номер unknown

Опубликована: Апрель 30, 2025

The use of highly active antiretroviral therapy (HAART) has made the human immunodeficiency virus (HIV) a chronic disease rather than terminal disease. Non-nucleoside reverse transcriptase inhibitors (NNRTIs) are an important component HAART, although we seeing clinically relevant drug-resistant mutants such that there is need to develop new molecules. We recently identified class N-phenyl-1-(phenylsulfonyl)-1H-1,2,4-triazol-3-amine HIV-1 NNRTI, with one known as compound 12126065, sub nanomolar (nM) potency in TZM-bl cells (HeLa expressing CD4, CCR5, and CXCR4) no vivo acute or subacute toxicity. now describe cryo-EM structure this molecule (resolution 3.53 Å) compare it analogues other NNRTIs. also synthesis activity five additional compounds, some which have promising against K103N/Y181C (A17) double mutant, will enable design future

Язык: Английский

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