Top ▲

pyruvate dehydrogenase kinase 3

Click here for help

Target not currently curated in GtoImmuPdb

Target id: 2143

Nomenclature: pyruvate dehydrogenase kinase 3

Abbreviated Name: PDHK3

Family: PDHK family

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 406 Xp22.11 PDK3 pyruvate dehydrogenase kinase 3
Mouse - 415 X C3 Pdk3 pyruvate dehydrogenase kinase, isoenzyme 3
Rat - 415 X q22 Pdk3 pyruvate dehydrogenase kinase 3
Previous and Unofficial Names Click here for help
pyruvate dehydrogenase kinase, isozyme 3 | pyruvate dehydrogenase kinase
Database Links Click here for help
Alphafold Q15120 (Hs), Q922H2 (Mm)
BRENDA 2.7.11.2
CATH/Gene3D 1.20.140.20, 3.30.565.10
ChEMBL Target CHEMBL3893 (Hs)
Ensembl Gene ENSG00000067992 (Hs), ENSMUSG00000035232 (Mm), ENSRNOG00000012513 (Rn)
Entrez Gene 5165 (Hs), 236900 (Mm), 296849 (Rn)
Human Protein Atlas ENSG00000067992 (Hs)
KEGG Enzyme 2.7.11.2
KEGG Gene hsa:5165 (Hs), mmu:236900 (Mm), rno:296849 (Rn)
OMIM 602526 (Hs)
Orphanet ORPHA356172 (Hs)
Pharos Q15120 (Hs)
RefSeq Nucleotide NM_001142386 (Hs), NM_145630 (Mm), NM_001106581 (Rn)
RefSeq Protein NP_001135858 (Hs), NP_663605 (Mm), NP_001100051 (Rn)
UniProtKB Q15120 (Hs), Q922H2 (Mm)
Wikipedia PDK3 (Hs)
Selected 3D Structures Click here for help
Image of receptor 3D structure from RCSB PDB
Description:  Crystal structure of the PDK3-L2 complex
PDB Id:  1Y8O
Ligand:  ADP   This ligand is endogenous
Resolution:  2.48Å
Species:  Human
References:  1
Enzyme Reaction Click here for help
EC Number: 2.7.11.2

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 7.4 pIC50 2
⤷ pIC50 7.4 (IC50 4x10-8 M) [2]
Description: In vitro functional assay
Clinically-Relevant Mutations and Pathophysiology Click here for help
Disease:  Charcot-Marie-Tooth disease, X-linked dominant, 6
Synonyms: X-linked Charcot-Marie-Tooth disease type 6 [Orphanet: ORPHA352675]
OMIM: 300905
Orphanet: ORPHA352675

References

Show »

1. Kato M, Chuang JL, Tso SC, Wynn RM, Chuang DT. (2005) Crystal structure of pyruvate dehydrogenase kinase 3 bound to lipoyl domain 2 of human pyruvate dehydrogenase complex. EMBO J, 24 (10): 1763-74. [PMID:15861126]

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]

How to cite this page

PDHK family: pyruvate dehydrogenase kinase 3. Last modified on 03/11/2016. Accessed on 19/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetoimmunopharmacology.org/GRAC/ObjectDisplayForward?objectId=2143.