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Article

HIV-1 Integrase Inhibitors with Modifications That Affect Their Potencies against Drug Resistant Integrase Mutants.

ACS infectious diseases - 11 Jun 2021

Smith Steven J, Zhao Xue Zhi, Passos Dario Oliveira, Pye Valerie E, Cherepanov Peter, Lyumkis Dmitry, Burke Terrence R, Hughes Stephen H

Abstract excerpt

Integrase strand transfer inhibitors (INSTIs) block the integration step of the retroviral lifecycle and are first-line drugs used for the treatment of HIV-1/AIDS. INSTIs have a polycyclic core with heteroatom triads, chelate the metal ions at the active site, and have a halobenzyl group that interacts with viral DNA attached to the core by a flexible linker. The most broadly effective INSTIs inhibit both...

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Identifiers

PMID: 33686850
DOI: 10.1021/acsinfecdis.0c00819
PMCID: PMC8205226

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