Tchem PDK1 [Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 1, mitochondrial

Protein Classes

PANTHER Classes

Protein / Transferase / Kinase / Protein Kinase / [Pyruvate Dehydrogenase (Acetyl-transferring)] Kinase Isozyme 1, Mitochondrial

DTO Classes

Protein / Kinase / Protein Kinase / Atypical Group / Pdhk Family / [Pyruvate Dehydrogenase (Acetyl-transferring)] Kinase Isozyme 1, Mitochondrial

Protein Summary

Description

Kinase that plays a key role in regulation of glucose and fatty acid metabolism and homeostasis via phosphorylation of the pyruvate dehydrogenase subunits PDHA1 and PDHA2. This inhibits pyruvate dehydrogenase activity, and thereby regulates metabolite flux through the tricarboxylic acid cycle, down-regulates aerobic respiration and inhibits the formation of acetyl-coenzyme A from pyruvate. Plays an important role in cellular responses to hypoxia and is important for cell proliferation under hypoxia. Protects cells against apoptosis in response to hypoxia and oxidative stress. Pyruvate dehydrogenase (PDH) is a mitochondrial multienzyme complex that catalyzes the oxidative decarboxylation of pyruvate and is one of the major enzymes responsible for the regulation of homeostasis of carbohydrate fuels in mammals. The enzymatic activity is regulated by a phosphorylation/dephosphorylation cycle. Phosphorylation of PDH by a specific pyruvate dehydrogenase kinase (PDK) results in inactivation. Multiple alternatively spliced transcript variants have been found for this gene. [provided by RefSeq, Jun 2013]

Uniprot Accession IDs

• Q15118
• B2R6T1
• B7Z937
• D3DPD8
• E9PD65
• Q308M4

Gene Name

• PDK1

Ensembl ID

• ENST00000282077
• ENSP00000282077
• ENSG00000152256
• ENST00000392571
• ENSP00000376352
• ENST00000410055
• ENSP00000386985

Symbol

• PDHK1

Knowledge Table

Most Knowledge About	Knowledge Value (0 to 1 scale)
transcription factor perturbation	0.98
PubMedID	0.94
kinase perturbation	0.91
molecular function	0.91
transcription factor binding site profile	0.88

IDG Partner Tools

GlyGen

IDG Development Level Summary

Tdark

These are targets about which virtually nothing is known. They do not have known drug or small molecule activities
- AND - satisfy two or more of the following criteria:

Pubmed score: 129.06   (req: < 5)

Gene RIFs: 36   (req: <= 3)

Antibodies: 636   (req: <= 50)

Tbio

These targets do not have known drug or small molecule activities
- AND - satisfy two or more of the following criteria:

Pubmed score: 129.06   (req: >= 5)

Gene RIFs: 36   (req: > 3)

Antibodies: 636   (req: > 50)

- OR - satisfy the following criterion:

Gene Ontology Terms: 9

Tchem

Target has at least one ChEMBL compound with an activity cutoff of < 30 nM - AND - satisfies the preceding conditions

Active Ligands: 102

Tclin

Target has at least one approved drug - AND - satisfies the preceding conditions

Active Drug: 0

Active Ligands (102)

Explore Active Ligands

1 – 10 of 102

CHEMBL495727

PDK1Tchem Kinase

IC50: 8

CHEMBL2347053

PDK1Tchem Kinase

IC50: 8.08

CHEMBL3673096

PDK1Tchem Kinase

IC50: 8.33

CHEMBL3727577

PDK1Tchem Kinase

IC50: 8

CHEMBL3673097

PDK1Tchem Kinase

IC50: 8.46

CHEMBL3730418

PDK1Tchem Kinase

IC50: 8

CHEMBL3730260

PDK1Tchem Kinase

IC50: 8

CHEMBL3733299

PDK1Tchem Kinase

IC50: 8

CHEMBL3732487

PDK1Tchem Kinase

IC50: 8

CHEMBL3730383

PDK1Tchem Kinase

IC50: 8

Protein Data Bank (3)

1 – 3 of 3

PDB Structure Id	Ligand	Method	Resolution (Å)	M.W. (kDa)	Pub Year	Title

PDB Structure Id	M.W.	Resolution	Pub Year

Pathways (173)

Reactome (8)

KEGG (3)

PathwayCommons (2)

WikiPathways (160)

Metabolism (R-HSA-1430728)

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5

1 – 5 of 8

Data Source	Name	Explore in Pharos	Explore in Source
Reactome	Metabolism	2112 targets	R-HSA-1430728
Reactome	Pyruvate metabolism	31 targets	R-HSA-70268
Reactome	Pyruvate metabolism and Citric Acid (TCA) cycle	55 targets	R-HSA-71406
Reactome	Regulation of pyruvate dehydrogenase (PDH) complex	16 targets	R-HSA-204174
Reactome	Signal Transduction	2704 targets	R-HSA-162582

Name	Explore in Pharos	Explore in Source
Metabolism	2112 targets	R-HSA-1430728
Pyruvate metabolism	31 targets	R-HSA-70268
Pyruvate metabolism and Citric Acid (TCA) cycle	55 targets	R-HSA-71406
Regulation of pyruvate dehydrogenase (PDH) complex	16 targets	R-HSA-204174
Signal Transduction	2704 targets	R-HSA-162582

Gene Ontology Terms (14)

Functions (3)

Components (5)

Processes (6)

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Items per page:

10

1 – 3 of 3

GO Term	Evidence	Assigned by
protein kinase activity	Inferred from Direct Assay (IDA)	UniProtKB
pyruvate dehydrogenase (acetyl-transferring) kinase activity	Inferred from Direct Assay (IDA)	UniProtKB
ATP binding	Inferred from Electronic Annotation (IEA)	UniProtKB-KW

Protein-Protein Interactions (125)

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1 – 10 of 125

• See Interactions on String-DB

PDK3

Tchem

Family: Kinase

Novelty: 0.05009442

p_int: 1

Score: 0.839

Data Source: BioPlex,STRINGDB

PDK2

Tchem

Family: Kinase

Novelty: 0.01502257

p_int: 0.999999962

p_ni: 3.8e-8

Score: 0.91

Data Source: BioPlex,STRINGDB

FOXD4

Tbio

Family: TF

Novelty: 0.11166611

p_int: 0.999998293

p_ni: 0.000001707

Score: 0.647

Data Source: BioPlex,STRINGDB

PDK4

Tchem

Family: Kinase

Novelty: 0.00410067

p_int: 0.999664796

p_ni: 0.000335204

Score: 0.828

Data Source: BioPlex,STRINGDB

CRBN

Tclin

Novelty: 0.00385433

p_int: 0.998900553

p_ni: 0.001077012

p_wrong: 0.000022435

Score: 0.234

Data Source: BioPlex,STRINGDB

NDUFS7

Tclin

Family: Enzyme

Novelty: 0.01562198

p_int: 0.987629181

p_ni: 0.01236723

p_wrong: 0.00000359

Data Source: BioPlex

ACAD9

Tbio

Family: Enzyme

Novelty: 0.03238308

p_int: 0.987560964

p_ni: 0.012438911

p_wrong: 1.25e-7

Score: 0.507

Data Source: BioPlex,STRINGDB

SLC18A1

Tchem

Family: Transporter

Novelty: 0.01135292

p_int: 0.982652996

p_ni: 0.017345208

p_wrong: 0.000001796

Data Source: BioPlex

PDHB

Tbio

Family: Enzyme

Novelty: 0.01018086

p_int: 0.982590067

p_ni: 0.017409933

Score: 0.988

Data Source: BioPlex,Reactome,STRINGDB

APLNR

Tchem

Family: GPCR

Novelty: 0.00224203

p_int: 0.981154959

p_ni: 0.018845041

Data Source: BioPlex

Publication Statistics

PubMed Score  129.06

PubMed score by year

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PubTator Score  421.82

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Amino Acid Sequence

Residue Counts

Protein Sequence

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UniProt Keyword Find Similar Targets

3D-structure
Alternative splicing
ATP-binding
Carbohydrate metabolism
Complete proteome
Glucose metabolism
Kinase
Mitochondrion
Nucleotide-binding
Phosphoprotein

MGI Phenotype Find Similar Targets

endocrine/exocrine gland phenotype
reproductive system phenotype