Ontology highlight
ABSTRACT:
SUBMITTER: Hung M
PROVIDER: S-EPMC6910994 | biostudies-literature | 2019
REPOSITORIES: biostudies-literature
Hung Magdeleine M Tokarsky E John EJ Lagpacan Leanna L Zhang Lijun L Suo Zucai Z Lansdon Eric B EB
Communications biology 20191213
Emtricitabine (FTC) and lamivudine (3TC), containing an oxathiolane ring with unnatural (-)-stereochemistry, are widely used nucleoside reverse transcriptase inhibitors (NRTIs) in anti-HIV therapy. Treatment with FTC or 3TC primarily selects for the HIV-1 RT M184V/I resistance mutations. Here we provide a comprehensive kinetic and structural basis for inhibiting HIV-1 RT by (-)-FTC-TP and (-)-3TC-TP and drug resistance by M184V. (-)-FTC-TP and (-)-3TC-TP have higher binding affinities (1/<i>K</i ...[more]