E. coli MsbA in nanodiscs in complex with G247
Ontology highlight
ABSTRACT:
SUBMITTER: Maofu Liao
PROVIDER: EMPIAR-10799 | biostudies-other |
REPOSITORIES: biostudies-other
Publications
Distinct allosteric mechanisms of first-generation MsbA inhibitors.
Thélot François A FA Zhang Wenyi W Song KangKang K Xu Chen C Huang Jing J Liao Maofu M
Science (New York, N.Y.) 20210923 6567
ATP-binding cassette (ABC) transporters couple adenosine 5′-triphosphate (ATP) hydrolysis to substrate transport across biological membranes. Although many are promising drug targets, their mechanisms of modulation by small-molecule inhibitors remain largely unknown. Two first-generation inhibitors of the MsbA transporter, tetrahydrobenzothiophene 1 (TBT1) and G247, induce opposite effects on ATP hydrolysis. Using single-particle cryo–electron microscopy and functional assays, we show that TBT1 ...[more]
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