Dataset Information
Single particle cryo-EM dataset of mitochondrial respiratory complex I from Bos taurus in DDM in the presence of IM1761092
Ontology highlight
ABSTRACT:
SUBMITTER: Hannah Ruth Bridges
PROVIDER: EMPIAR-10991 | biostudies-other |
REPOSITORIES: biostudies-other
Publications
Structural basis of mammalian respiratory complex I inhibition by medicinal biguanides.
Science (New York, N.Y.) 20230126 6630
The molecular mode of action of biguanides, including the drug metformin, which is widely used in the treatment of diabetes, is incompletely characterized. Here, we define the inhibitory drug-target interaction(s) of a model biguanide with mammalian respiratory complex I by combining cryo-electron microscopy and enzyme kinetics. We interpret these data to explain the selectivity of biguanide binding to different enzyme states. The primary inhibitory site is in an amphipathic region of the quinon ...[more]