3jrx | pdb_00003jrx

Crystal structure of the BC domain of ACC2 in complex with soraphen A

spinqualitylabelsall models 3jrx, resolution 2.50Å Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image   Print3D Structural highlights 3jrx is a 1 chain structure with sequence from Homo sapiens. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance. Ligands: S1A Related: 2hjw, 3jrw Gene: ACACB, ACC2, ACCB (Homo sapiens) Resources: FirstGlance, OCA, RCSB, PDBsum Evolutionary Conservation Check, as determined by ConSurfDB. You may read the explanation of the method and the full data available from ConSurf. Publication Abstract from PubMed Acetyl-CoA carboxylases (ACCs) have been highlighted as therapeutic targets for obesity and diabetes, as they play crucial roles in fatty acid metabolism. ACC activity is regulated through the short-term mechanism of inactivation by reversible phosphorylation. Here, we report the crystal structures of the biotin carboxylase (BC) domain of human ACC2 phosphorylated by AMP-activated protein kinase (AMPK). The phosphorylated Ser222 binds to the putative dimer interface of BC, disrupting polymerization and providing the molecular mechanism of inactivation by AMPK. We also determined the structure of the human BC domain in complex with soraphen A, a macrocyclic polyketide natural product. This structure shows that the compound binds to the binding site of phosphorylated Ser222, implying that its inhibition mechanism is the same as that of phosphorylation by AMPK. Molecular mechanism for the regulation of human ACC2 through phosphorylation by AMPK.,Cho YS, Lee JI, Shin D, Kim HT, Jung HY, Lee TG, Kang LW, Ahn YJ, Cho HS, Heo YS Biochem Biophys Res Commun. 2010 Jan 1;391(1):187-92. Epub 2009 Nov 10. PMID:19900410 From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine. See Also Biotin carboxylase

Proteopedia Page Contributors and Editors (what is this?)

OCA