Ontology highlight
ABSTRACT:
SUBMITTER: Zhu Y
PROVIDER: S-EPMC6462036 | biostudies-literature | 2019 Apr
REPOSITORIES: biostudies-literature
Acta pharmacologica Sinica 20180625 4
The chemokine receptor CCR5 is an important anti-HIV (human immunodeficiency virus) drug target owning to its pivotal role in HIV-1 viral entry as a co-receptor. Here, we present a 2.9 Å resolution crystal structure of CCR5 bound to PF-232798, a second-generation oral CCR5 antagonist currently in phase II clinical trials. PF-232798 and the marketed HIV drug maraviroc share a similar tropane scaffold with different amino (N)- and carboxyl (C)- substituents. Comparison of the CCR5-PF-232798 struct ...[more]