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pyruvate dehydrogenase kinase 1

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Target not currently curated in GtoImmuPdb

Target id: 2915

Nomenclature: pyruvate dehydrogenase kinase 1

Family: PDHK family

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 436 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 Click here for help
pyruvate dehydrogenase kinase, isoenzyme 1 | pyruvate dehydrogenase kinase
Database Links Click here for help
Alphafold Q15118 (Hs), Q8BFP9 (Mm)
CATH/Gene3D 1.20.140.20, 3.30.565.10
ChEMBL Target CHEMBL4766 (Hs)
Ensembl Gene ENSG00000152256 (Hs), ENSMUSG00000006494 (Mm), ENSRNOG00000001517 (Rn)
Entrez Gene 5163 (Hs), 228026 (Mm), 116551 (Rn)
Human Protein Atlas ENSG00000152256 (Hs)
KEGG Gene hsa:5163 (Hs), mmu:228026 (Mm), rno:116551 (Rn)
Pharos Q15118 (Hs)
RefSeq Nucleotide NM_001278549 (Hs), NM_172665 (Mm), NM_053826 (Rn)
RefSeq Protein NP_001265478 (Hs), NP_766253 (Mm), NP_446278 (Rn)
SynPHARM 83947 (in complex with AZD7545)
UniProtKB Q15118 (Hs), Q8BFP9 (Mm)
Wikipedia PDK1 (Hs)
Selected 3D Structures Click here for help
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 go icon to follow link

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 7.5 pIC50 2
⤷ pIC50 7.5 (IC50 3.5x10-8 M) [2]
Description: In vitro functional assay
AZD7545 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure 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 20/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2915.