Pyruvate dehydrogenase kinase

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Line 31: Line 31:
**[[2bu7]] - hPDK2 + acetamide derivative<br />
**[[2bu7]] - hPDK2 + acetamide derivative<br />
**[[2bu8]] - hPDK2 + dichloro-acetic acid + ADP<BR />
**[[2bu8]] - hPDK2 + dichloro-acetic acid + ADP<BR />
-
**[[4mp2]], [[4mp7]], [[4mpc]], [[4mpe]], [[4mpn]], [[4v25]], [[4v26]], [[5j6a]], [[5j71]], [[5m4k]], [[5m4m]], [[5m4n]], [[5m4p]], [[6lil]], [[6lio]], [[6lin]], [[6tmz]], [[6tmp]], [[6tmq]], [[6tn0]], [[6tn2]] – hPDK2 + inhibitor<br />
+
**[[4mp2]], [[4mp7]], [[4mpc]], [[4mpe]], [[4mpn]], [[4v25]], [[4v26]], [[5j6a]], [[5j71]], [[5m4k]], [[5m4m]], [[5m4n]], [[5m4p]], [[6lil]], [[6lio]], [[6lin]], [[6tmz]], [[6tmp]], [[6tmq]], [[6tn0]], [[6tn2]], [[7ebh]], [[7eas]] – hPDK2 + inhibitor<br />
**[[3crk]], [[3crl]] – hPDK2 + pyruvate dehydrogenase E2
**[[3crk]], [[3crl]] – hPDK2 + pyruvate dehydrogenase E2
Line 43: Line 43:
**[[2e0a]] – hPDK4 + AMPPNP<br />
**[[2e0a]] – hPDK4 + AMPPNP<br />
**[[2zkj]], [[3d2r]] – hPDK4 + ADP<BR />
**[[2zkj]], [[3d2r]] – hPDK4 + ADP<BR />
 +
**[[7ea0]], [[7eat]], [[7ebb]], [[7ebg]] – hPDK4 + inhibitor<br />
**[[2zdx]], [[2zdy]] – hPDK4 (mutant) + inhibitor
**[[2zdx]], [[2zdy]] – hPDK4 (mutant) + inhibitor
}}
}}

Revision as of 08:28, 9 February 2022

Human pyruvate dehydrogenase kinase isozyme 4 dimer complex with AMPPNP and Mg+2 ion (green) (PDB entry 2e0a)

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3D structures of pyruvate dehydrogenase kinase

Updated on 09-February-2022

References

  1. Korotchkina LG, Patel MS. Site specificity of four pyruvate dehydrogenase kinase isoenzymes toward the three phosphorylation sites of human pyruvate dehydrogenase. J Biol Chem. 2001 Oct 5;276(40):37223-9. Epub 2001 Aug 2. PMID:11486000 doi:10.1074/jbc.M103069200
  2. Roche TE, Hiromasa Y. Pyruvate dehydrogenase kinase regulatory mechanisms and inhibition in treating diabetes, heart ischemia, and cancer. Cell Mol Life Sci. 2007 Apr;64(7-8):830-49. PMID:17310282 doi:10.1007/s00018-007-6380-z
  3. Sutendra G, Michelakis ED. Pyruvate dehydrogenase kinase as a novel therapeutic target in oncology. Front Oncol. 2013 Mar 7;3:38. doi: 10.3389/fonc.2013.00038. eCollection 2013. PMID:23471124 doi:http://dx.doi.org/10.3389/fonc.2013.00038
  4. Kukimoto-Niino M, Tokmakov A, Terada T, Ohbayashi N, Fujimoto T, Gomi S, Shiromizu I, Kawamoto M, Matsusue T, Shirouzu M, Yokoyama S. Inhibitor-bound structures of human pyruvate dehydrogenase kinase 4. Acta Crystallogr D Biol Crystallogr. 2011 Sep;67(Pt 9):763-73. doi:, 10.1107/S090744491102405X. Epub 2011 Aug 9. PMID:21904029 doi:10.1107/S090744491102405X

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Michal Harel, Alexander Berchansky, Joel L. Sussman

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