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pyruvate dehydrogenase kinase 2

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Target not currently curated in GtoImmuPdb

Target id: 2142

Nomenclature: pyruvate dehydrogenase kinase 2

Abbreviated Name: PDHK2

Family: PDHK family

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 407 17q21.33 PDK2 pyruvate dehydrogenase kinase 2
Mouse - 407 11 59.01 cM Pdk2 pyruvate dehydrogenase kinase, isoenzyme 2
Rat - 407 10q26 Pdk2 pyruvate dehydrogenase kinase 2
Previous and Unofficial Names Click here for help
pyruvate dehydrogenase kinase, isoenzyme 2 | PDK P45 | pyruvate dehydrogenase kinase
Database Links Click here for help
BRENDA
CATH/Gene3D
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
Pharos
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Selected 3D Structures Click here for help
Image of receptor 3D structure from RCSB PDB
Description:  CRYSTAL STRUCTURES OF HUMAN PYRUVATE DEHYDROGENASE KINASE 2 CONTAINING PHYSIOLOGICAL AND SYNTHETIC LIGANDS
PDB Id:  2BTZ
Resolution:  2.2Å
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
AZD7545 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 8.2 pIC50 3
pIC50 8.2 (IC50 6.4x10-9 M) [3]
Description: In a biochemical enzyme assay
VER-246608 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.1 pIC50 2
pIC50 7.1 (IC50 8.4x10-8 M) [2]
Description: In vitro functional assay

References

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1. Knoers NV, van den Ouweland AM, Verdijk M, Monnens LA, van Oost BA. (1994) Inheritance of mutations in the V2 receptor gene in thirteen families with nephrogenic diabetes insipidus. Kidney Int, 46 (1): 170-6. [PMID:7933835]

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]

3. Morrell JA, Orme J, Butlin RJ, Roche TE, Mayers RM, Kilgour E. (2003) AZD7545 is a selective inhibitor of pyruvate dehydrogenase kinase 2. Biochem Soc Trans, 31: 1168-70. [PMID:14641019]

How to cite this page

PDHK family: pyruvate dehydrogenase kinase 2. Last modified on 07/11/2016. Accessed on 11/04/2021. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2142.