pyruvate dehydrogenase kinase 2 | PDHK family | IUPHAR/BPS Guide to PHARMACOLOGY

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pyruvate dehydrogenase kinase 2

Target not currently curated in GtoImmuPdb

Target id: 2142

Nomenclature: pyruvate dehydrogenase kinase 2

Abbreviated Name: PDHK2

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 - 407 17q21.33 PDK2 pyruvate dehydrogenase kinase 2
Mouse - 407 11 D Pdk2 pyruvate dehydrogenase kinase, isoenzyme 2
Rat - 407 10 q31 Pdk2 pyruvate dehydrogenase kinase 2
Previous and Unofficial Names
pyruvate dehydrogenase kinase, isoenzyme 2 | PDK P45 | pyruvate dehydrogenase kinase
Database Links
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
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
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 Hs Inhibition 8.2 pIC50 3
pIC50 8.2 (IC50 6.4x10-9 M) [3]
Description: In a biochemical enzyme assay
VER-246608 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 15/07/2020. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2142.