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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.

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This article was published in the following journal.

Name: Journal of medicinal chemistry
ISSN: 1520-4804
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