4MPN

Crystal structure of pyruvate dehydrogenase kinase isoform 2 in complex with inhibitor PS10

Summary for 4MPN

Entry DOI	10.2210/pdb4mpn/pdb
Related	4MP2 4MP7 4MPC 4MPE
Descriptor	[Pyruvate dehydrogenase [lipoamide]] kinase isozyme 2, mitochondrial, 2-[(2,4-dihydroxyphenyl)sulfonyl]-2,3-dihydro-1H-isoindole-4,6-diol, L(+)-TARTARIC ACID, ... (4 entities in total)
Functional Keywords	ghkl protein kinase, pyruvate dehydrogenase complex, mitochondrial protein kinases, impaired glucose oxidation, hepatic steatosis, type 2 diabetes, cancer, bergerat nucleotide-binding fold, protein kinase, transferase
Biological source	Homo sapiens (human)
Cellular location	Mitochondrion matrix: Q15119
Total number of polymer chains	1
Total formula weight	45706.81
Authors	Gui, W.J.,Tso, S.C.,Chuang, J.L.,Wu, C.Y.,Qi, X.,Tambar, U.K.,Wynn, R.M.,Chuang, D.T. (deposition date: 2013-09-13, release date: 2014-01-01, Last modification date: 2024-02-28)
Primary citation	Tso, S.C.,Qi, X.,Gui, W.J.,Wu, C.Y.,Chuang, J.L.,Wernstedt-Asterholm, I.,Morlock, L.K.,Owens, K.R.,Scherer, P.E.,Williams, N.S.,Tambar, U.K.,Wynn, R.M.,Chuang, D.T. Structure-guided Development of Specific Pyruvate Dehydrogenase Kinase Inhibitors Targeting the ATP-binding Pocket. J.Biol.Chem., 289:4432-4443, 2014 Cited by PubMed: 24356970 DOI: 10.1074/jbc.M113.533885 PDB entries with the same primary citation
Experimental method	X-RAY DIFFRACTION (1.752 Å)

Structure validation