Ontology highlight
ABSTRACT:
SUBMITTER: Zhao XZ
PROVIDER: S-EPMC4836387 | biostudies-literature | 2016 Apr
REPOSITORIES: biostudies-literature
Zhao Xue Zhi XZ Smith Steven J SJ Maskell Daniel P DP Metifiot Mathieu M Pye Valerie E VE Fesen Katherine K Marchand Christophe C Pommier Yves Y Cherepanov Peter P Hughes Stephen H SH Burke Terrence R TR
ACS chemical biology 20160205 4
HIV integrase (IN) strand transfer inhibitors (INSTIs) are among the newest anti-AIDS drugs; however, mutant forms of IN can confer resistance. We developed noncytotoxic naphthyridine-containing INSTIs that retain low nanomolar IC50 values against HIV-1 variants harboring all of the major INSTI-resistant mutations. We found by analyzing crystal structures of inhibitors bound to the IN from the prototype foamy virus (PFV) that the most successful inhibitors show striking mimicry of the bound vira ...[more]