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
BRENDA
CATH/Gene3D
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
Orphanet
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
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: 2.7.11.2

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Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
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

References

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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 24/04/2019. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2143.