Ontology highlight
ABSTRACT:
SUBMITTER: Smith SJ
PROVIDER: S-EPMC8205226 | biostudies-literature | 2021 Jun
REPOSITORIES: biostudies-literature
Smith Steven J SJ Zhao Xue Zhi XZ Passos Dario Oliveira DO Pye Valerie E VE Cherepanov Peter P Lyumkis Dmitry D Burke Terrence R TR Hughes Stephen H SH
ACS infectious diseases 20210309 6
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 wild-type (WT) integrase (IN) and a variety of well-known mutants. However, because there a ...[more]