Cryo-EM structures of a human ABCG2 mutant trapped in ATP-bound and substrate-bound states.

ABSTRACT: ABCG2 is a transporter protein of the ATP-binding-cassette (ABC) family that is expressed in the plasma membrane in cells of various tissues and tissue barriers, including the blood-brain, blood-testis and maternal-fetal barriers^1-4. Powered by ATP, it translocates endogenous substrates, affects the pharmacokinetics of many drugs and protects against a wide array of xenobiotics, including anti-cancer drugs^5-12. Previous studies have revealed the architecture of ABCG2 and the structural basis of its inhibition by small molecules and antibodies^13,14. However, the mechanisms of substrate recognition and ATP-driven transport are unknown. Here we present high-resolution cryo-electron microscopy (cryo-EM) structures of human ABCG2 in a substrate-bound pre-translo

SUBMITTER: Manolaridis I 

PROVIDER: S-EPMC6379061 | biostudies-literature | 2018 Nov

REPOSITORIES: biostudies-literature