Crystal Structure of the Human Cannabinoid Receptor CB₁.

ABSTRACT: Cannabinoid receptor 1 (CB₁) is the principal target of Δ⁹-tetrahydrocannabinol (THC), a psychoactive chemical from Cannabis sativa with a wide range of therapeutic applications and a long history of recreational use. CB₁ is activated by endocannabinoids and is a promising therapeutic target for pain management, inflammation, obesity, and substance abuse disorders. Here, we present the 2.8 Å crystal structure of human CB₁ in complex with AM6538, a stabilizing antagonist, synthesized and characterized for this structural study. The structure of the CB₁-AM6538 complex reveals key features of the receptor and critical interactions for antagonist binding. In combination with functional studies and molecular modeling, the structure provides

SUBMITTER: Hua T 

PROVIDER: S-EPMC5322940 | biostudies-literature | 2016 Oct

REPOSITORIES: biostudies-literature