Summary information and primary citation
- PDB-id
- 6o9e; SNAP-derived features in text and JSON formats;
DNAproDB
- Class
- transferase-DNA
- Method
- X-ray (2.4 Å)
- Summary
- Structure of hiv-1 reverse transcriptase in complex with DNA and indopy-1
- Reference
- Ruiz FX, Hoang A, Das K, Arnold E (2019): "Structural Basis of HIV-1 Inhibition by Nucleotide-Competing Reverse Transcriptase Inhibitor INDOPY-1." J.Med.Chem., 62, 9996-10002. doi: 10.1021/acs.jmedchem.9b01289.
- Abstract
- 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.
