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pyruvate dehydrogenase kinase 4

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Target not currently curated in GtoImmuPdb

Target id: 2144

Nomenclature: pyruvate dehydrogenase kinase 4

Abbreviated Name: LOC389533

Family: PDHK family

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 411 7q21.3 PDK4 pyruvate dehydrogenase kinase 4
Mouse - 412 6 2.06 cM Pdk4 pyruvate dehydrogenase kinase, isoenzyme 4
Rat - 412 4q13 Pdk4 pyruvate dehydrogenase kinase 4
Previous and Unofficial Names Click here for help
pyruvate dehydrogenase kinase, isozyme 4 | pyruvate dehydrogenase kinase
Database Links Click here for help
Alphafold Q16654 (Hs), O70571 (Mm), O54937 (Rn)
BRENDA 2.7.11.2
CATH/Gene3D 1.20.140.20, 3.30.565.10
ChEMBL Target CHEMBL4141 (Hs)
Ensembl Gene ENSG00000004799 (Hs), ENSMUSG00000019577 (Mm), ENSRNOG00000009565 (Rn)
Entrez Gene 5166 (Hs), 27273 (Mm), 89813 (Rn)
Human Protein Atlas ENSG00000004799 (Hs)
KEGG Enzyme 2.7.11.2
KEGG Gene hsa:5166 (Hs), mmu:27273 (Mm), rno:89813 (Rn)
OMIM 602527 (Hs)
Pharos Q16654 (Hs)
RefSeq Nucleotide NM_002612 (Hs), NM_013743 (Mm), NM_053551 (Rn)
RefSeq Protein NP_002603 (Hs), NP_038771 (Mm), NP_446003 (Rn)
UniProtKB Q16654 (Hs), O70571 (Mm), O54937 (Rn)
Wikipedia PDK4 (Hs)
Selected 3D Structures Click here for help
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 Click here for help
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 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure 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 19/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2144.