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

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
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
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
RefSeq Nucleotide
RefSeq Protein
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

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


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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 30/09/2020. IUPHAR/BPS Guide to PHARMACOLOGY,