2jiz

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spinqualitylabelsall models 2jiz, resolution 2.30Å Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image

THE STRUCTURE OF F1-ATPASE INHIBITED BY RESVERATROL.

Overview

The structures of F(1)-ATPase from bovine heart mitochondria inhibited, with the dietary phytopolyphenol, resveratrol, and with the related, polyphenols quercetin and piceatannol have been determined at 2.3-, 2.4-, and 2.7-A resolution, respectively. The inhibitors bind to a common site, in the inside surface of an annulus made from loops in the three alpha-, and three beta-subunits beneath the "crown" of beta-strands in their, N-terminal domains. This region of F(1)-ATPase forms a bearing to allow, the rotation of the tip of the gamma-subunit inside the annulus during, catalysis. The binding site is a hydrophobic pocket between the C-terminal, tip of the gamma-subunit and the beta(TP) subunit, and the inhibitors are, bound via H-bonds mostly to their hydroxyl moieties mediated by bound, water molecules and by hydrophobic interactions. There are no equivalent, sites between the gamma-subunit and either the beta(DP) or the beta(E), subunit. The inhibitors probably prevent both the synthetic and hydrolytic, activities of the enzyme by blocking both senses of rotation of the, gamma-subunit. The beneficial effects of dietary resveratrol may derive in, part by preventing mitochondrial ATP synthesis in tumor cells, thereby, inducing apoptosis.

About this Structure

2JIZ is a Protein complex structure of sequences from Bos taurus with MG, AZI, PO4, ANP, ADP, STL and GOL as ligands. Active as Transferred entry: 3.6.3.14, with EC number 3.6.1.34 Known structural/functional Site: . Full crystallographic information is available from OCA.

Reference

Mechanism of inhibition of bovine F1-ATPase by resveratrol and related polyphenols., Gledhill JR, Montgomery MG, Leslie AG, Walker JE, Proc Natl Acad Sci U S A. 2007 Aug 21;104(34):13632-7. Epub 2007 Aug 13. PMID:17698806

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