pyruvate dehydrogenase kinase 3 | PDHK family | IUPHAR/BPS Guide to PHARMACOLOGY

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pyruvate dehydrogenase kinase 3

Target not currently curated in GtoImmuPdb

Target id: 2143

Nomenclature: pyruvate dehydrogenase kinase 3

Abbreviated Name: PDHK3

Family: PDHK family

Annotation status:  image of a grey circle Awaiting annotation/under development. Please contact us if you can help with annotation.  » Email us

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 415 Xp22.12 PDK3 pyruvate dehydrogenase kinase 3
Mouse - 415 X C3 Pdk3 pyruvate dehydrogenase kinase
Rat - 415 X q22 Pdk3 pyruvate dehydrogenase kinase 3
Previous and Unofficial Names
pyruvate dehydrogenase kinase, isozyme 3 | pyruvate dehydrogenase kinase
Database Links
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
RefSeq Nucleotide
RefSeq Protein
Selected 3D Structures
Image of receptor 3D structure from RCSB PDB
Description:  Crystal structure of the PDK3-L2 complex
PDB Id:  1Y8O
Ligand:  ADP   This ligand is endogenous
Resolution:  2.48Å
Species:  Human
References:  1
Enzyme Reaction
EC Number:

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Ligand Sp. Action Affinity Parameter Reference
VER-246608 Hs Inhibition 7.4 pIC50 2
pIC50 7.4 (IC50 4x10-8 M) [2]
Description: In vitro functional assay
Clinically-Relevant Mutations and Pathophysiology
Disease:  Charcot-Marie-Tooth disease, X-linked dominant, 6
Synonyms: X-linked Charcot-Marie-Tooth disease type 6 [Orphanet: ORPHA352675]
OMIM: 300905
Orphanet: ORPHA352675


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1. Kato M, Chuang JL, Tso SC, Wynn RM, Chuang DT. (2005) Crystal structure of pyruvate dehydrogenase kinase 3 bound to lipoyl domain 2 of human pyruvate dehydrogenase complex. EMBO J., 24 (10): 1763-74. [PMID:15861126]

2. Moore JD, Staniszewska A, Shaw T, D'Alessandro J, Davis B, Surgenor A, Baker L, Matassova N, Murray J, Macias A et al.. (2014) VER-246608, a novel pan-isoform ATP competitive inhibitor of pyruvate dehydrogenase kinase, disrupts Warburg metabolism and induces context-dependent cytostasis in cancer cells. Oncotarget, 5 (24): 12862-76. [PMID:25404640]

How to cite this page

PDHK family: pyruvate dehydrogenase kinase 3. Last modified on 03/11/2016. Accessed on 20/02/2019. IUPHAR/BPS Guide to PHARMACOLOGY,