pyruvate dehydrogenase kinase 4 | PDHK family | IUPHAR/BPS Guide to PHARMACOLOGY

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pyruvate dehydrogenase kinase 4

Target not currently curated in GtoImmuPdb

Target id: 2144

Nomenclature: pyruvate dehydrogenase kinase 4

Abbreviated Name: LOC389533

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 - 411 7q21.3-q22.1 PDK4 pyruvate dehydrogenase kinase 4
Mouse - 412 6 A1 Pdk4 pyruvate dehydrogenase kinase, isoenzyme 4
Rat - 412 4 q13 Pdk4 pyruvate dehydrogenase kinase 4
Previous and Unofficial Names
pyruvate dehydrogenase kinase, isozyme 4 | pyruvate dehydrogenase kinase
Database Links
BRENDA
CATH/Gene3D
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Selected 3D Structures
Image of receptor 3D structure from RCSB PDB
Description:  Crystal structure of human pyruvate dehydrogenase kinase 4 in complex with AMPPNP
PDB Id:  2E0A
Ligand:  AMP-PNP
Resolution:  1.86Å
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 Value Parameter Reference
VER-246608 Hs Inhibition 7.0 pIC50 2
pIC50 7.0 (IC50 9.1x10-8 M) [2]
Description: In vitro functional assay

References

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1. Kukimoto-Niino M, Tokmakov A, Terada T, Ohbayashi N, Fujimoto T, Gomi S, Shiromizu I, Kawamoto M, Matsusue T, Shirouzu M et al.. (2011) Inhibitor-bound structures of human pyruvate dehydrogenase kinase 4. Acta Crystallogr. D Biol. Crystallogr., 67 (Pt 9): 763-73. [PMID:21904029]

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 4. Last modified on 03/11/2016. Accessed on 12/11/2019. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2144.