Structural Basis of HIV-1 Inhibition by the Nucleotide-Competing Reverse Transcriptase Inhibitor INDOPY-1.

08:00 EDT 11th October 2019 | BioPortfolio

Summary of "Structural Basis of HIV-1 Inhibition by the Nucleotide-Competing Reverse Transcriptase Inhibitor INDOPY-1."

HIV-1 reverse transcriptase (RT) is an essential enzyme, targeting half of approved anti-AIDS drugs. While nucleoside RT inhibitors (NRTIs) are DNA chain terminators, the nucleotide-competing RT inhibitor (NcRTI) INDOPY-1 blocks dNTP binding to RT. Lack of structural information hindered INDOPY-1 improvement. Here we report the HIV-1 RT/DNA/INDOPY-1 crystal structure, revealing a unique mode of inhibitor binding at the polymerase active site without involving catalytic metal ions. The structure may enable new strategies for developing NcRTIs.


Journal Details

This article was published in the following journal.

Name: Journal of medicinal chemistry
ISSN: 1520-4804


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