2Q8G

Structure of pyruvate dehydrogenase kinase isoform 1 in complex with glucose-lowering drug AZD7545

Summary for 2Q8G

Entry DOI	10.2210/pdb2q8g/pdb
Related	2Q8F 2Q8H 2Q8I
Descriptor	[Pyruvate dehydrogenase [lipoamide]] kinase isozyme 1, POTASSIUM ION, 4-[(3-CHLORO-4-{[(2R)-3,3,3-TRIFLUORO-2-HYDROXY-2-METHYLPROPANOYL]AMINO}PHENYL)SULFONYL]-N,N-DIMETHYLBENZAMIDE, ... (4 entities in total)
Functional Keywords	ghkl atpase/kinase family, pyruvate dehydrogenase complex, mitochondrial kinase, glucose-lowering drug azd7545, transferase
Biological source	Homo sapiens (human)
Cellular location	Mitochondrion matrix : Q15118
Total number of polymer chains	1
Total formula weight	46879.58
Authors	Kato, M.,Li, J.,Chuang, J.L.,Chuang, D.T. (deposition date: 2007-06-10, release date: 2007-07-24, Last modification date: 2024-03-13)
Primary citation	Kato, M.,Li, J.,Chuang, J.L.,Chuang, D.T. Distinct Structural Mechanisms for Inhibition of Pyruvate Dehydrogenase Kinase Isoforms by AZD7545, Dichloroacetate, and Radicicol. Structure, 15:992-1004, 2007 Cited by PubMed: 17683942 DOI: 10.1016/j.str.2007.07.001 PDB entries with the same primary citation
Experimental method	X-RAY DIFFRACTION (1.9 Å)

Structure validation