Pyruvate dehydrogenase kinase

spinqualitylabelsall models Human pyruvate dehydrogenase kinase isozyme 4 dimer complex with AMPPNP and Mg+2 ion (green) (PDB entry 2e0a) Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image   Print3D Function Pyruvate dehydrogenase kinase (PDK) is part of the pyruvate dehydrogenase complex. This complex is located in the mitochondria and converts pyruvate to acetyl-CoA as part of the citric acid cycle. PDK phosphphorylates serine residues on pyruvate dehydrogenase using ATP. There are 4 isozymes of PDK. The isozymes differ in length, activity and phosphorylation sites. PDK1 is abundant in heart cells. PDK1 expression was found to predict future major adverse cardiovascular events. PDK2 is abundant in mitochondria. PDK3 is abundant in testis. PDK4 is abundant in muscle and heart. It is important during starvation for regulation of pyruvate dehydrogenate complex activity and glucose homoeostasis. Relevance Inhibition of PDK decreases the damage caused by heart ischemia and are used in diabetes and cancer patients. Structural highlights The active site cleft of PDK4 binds AMPPNP. Water molecules are shown as red spheres. Mg coordination site.

3D structures of pyruvate dehydrogenase kinase

Updated on 27-August-2026

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• PDK isozyme 1
  • 2q8f– hPDK1 – human
    
  • 2q8g – hPDK1 + drug
    
  • 2q8h – hPDK1 + dichloro-acetic acid
• PDK isozyme 2
  • 2btz – hPDK2
    
  • 2bu2 – hPDK2 + benzonitrile derivative + ATP
    
  • 2bu5 - hPDK2 + benzonitrile derivative
    
  • 2bu6 - hPDK2 + propanamide derivative
    
  • 2bu7 - hPDK2 + acetamide derivative
    
  • 2bu8 - hPDK2 + dichloro-acetic acid + ADP
    
  • 4mp2, 4mp7, 4mpc, 4mpe, 4mpn, 4v25, 4v26, 5j6a, 5j71, 5m4k, 5m4m, 5m4n, 5m4p, 6lil, 6lio, 6lin, 6tmp, 6tmq, 6tmz, 6tn0, 6tn2, 7eas, 7ebh, 7vbu, 7vbv, 7vbx, 8zm1, 8zm2, 9m3o, 9m3p, 9m3r, 9m3t, 9m3u – hPDK2 + inhibitor
    
  • 3crk, 3crl – hPDK2 + pyruvate dehydrogenase E2
    
  • 1jm6 – PDK2 + ADP – rat
    
• PDK isozyme 3
  • 1y8n, 1y8o, 1y8p, 2pnr – hPDK3 + acetyltransferase component of pyruvate dehydrogenase complex
    
  • 2q8i – hPDK3 + radicicol
• PDK isozyme 4
  • 2e0a – hPDK4 + AMPPNP
    
  • 2zkj, 3d2r – hPDK4 + ADP
    
  • 7ea0, 7eat, 7ebb, 7ebg – hPDK4 + inhibitor
    
  • 2zdx, 2zdy – hPDK4 (mutant) + inhibitor

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