pyruvate dehydrogenase kinase 1 | PDHK family | IUPHAR/BPS Guide to PHARMACOLOGY

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pyruvate dehydrogenase kinase 1

Target not currently curated in GtoImmuPdb

Target id: 2915

Nomenclature: pyruvate dehydrogenase kinase 1

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 - 456 2q31.1 PDK1 pyruvate dehydrogenase kinase 1
Mouse - 434 2 C3 Pdk1 pyruvate dehydrogenase kinase, isoenzyme 1
Rat - 434 3q23 Pdk1 pyruvate dehydrogenase kinase 1
Gene and Protein Information Comments
Human isoform 2 (NP_002601) has 436 amino acids and lacks an in-frame exon in the coding region, compared to isoform 1.
Previous and Unofficial Names
pyruvate dehydrogenase kinase, isoenzyme 1 | pyruvate dehydrogenase kinase
Database Links
CATH/Gene3D
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Gene
RefSeq Nucleotide
RefSeq Protein
SynPHARM
UniProtKB
Wikipedia
Selected 3D Structures
Image of receptor 3D structure from RCSB PDB
Description:  Structure of pyruvate dehydrogenase kinase isoform 1 in complex with glucose-lowering drug AZD7545.
PDB Id:  2Q8G
Ligand:  AZD7545
Resolution:  1.9Å
Species:  Human
References:  1

Download all structure-activity data for this target as a CSV file

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 7.5 pIC50 2
pIC50 7.5 (IC50 3.5x10-8 M) [2]
Description: In vitro functional assay
AZD7545 Hs Inhibition 7.4 pIC50 3
pIC50 7.4 (IC50 3.68x10-8 M) [3]
Description: In a biochemical enzyme assay

References

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1. Kato M, Li J, Chuang JL, Chuang DT. (2007) Distinct Structural Mechanisms for Inhibition of Pyruvate Dehydrogenase Kinase Isoforms by AZD7545, Dichloroacetate, and Radicicol. Structure, 15: 992-1004. [PMID:17683942]

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 1. Last modified on 07/11/2016. Accessed on 15/09/2019. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2915.