Dataset Information
CryoEM reconstruction of human ABCG2 transporter with inhibitor MZ29 and 5D3-Fab
Ontology highlight
ABSTRACT:
SUBMITTER: Kaspar P Locher
PROVIDER: EMPIAR-10374 | biostudies-other |
REPOSITORIES: biostudies-other
Publications
Structural basis of small-molecule inhibition of human multidrug transporter ABCG2.
Nature structural & molecular biology 20180402 4
ABCG2 is an ATP-binding cassette (ABC) transporter that protects tissues against xenobiotics, affects the pharmacokinetics of drugs and contributes to multidrug resistance. Although many inhibitors and modulators of ABCG2 have been developed, understanding their structure-activity relationship requires high-resolution structural insight. Here, we present cryo-EM structures of human ABCG2 bound to synthetic derivatives of the fumitremorgin C-related inhibitor Ko143 or the multidrug resistance mod ...[more]