Tchem PKM Pyruvate kinase PKM

Protein Summary

Description

Glycolytic enzyme that catalyzes the transfer of a phosphoryl group from phosphoenolpyruvate (PEP) to ADP, generating ATP. Stimulates POU5F1-mediated transcriptional activation. Plays a general role in caspase independent cell death of tumor cells. The ratio between the highly active tetrameric form and nearly inactive dimeric form determines whether glucose carbons are channeled to biosynthetic processes or used for glycolytic ATP production. The transition between the 2 forms contributes to the control of glycolysis and is important for tumor cell proliferation and survival. This gene encodes a protein involved in glycolysis. The encoded protein is a pyruvate kinase that catalyzes the transfer of a phosphoryl group from phosphoenolpyruvate to ADP, generating ATP and pyruvate. This protein has been shown to interact with thyroid hormone and may mediate cellular metabolic effects induced by thyroid hormones. This protein has been found to bind Opa protein, a bacterial outer membrane protein involved in gonococcal adherence to and invasion of human cells, suggesting a role of this protein in bacterial pathogenesis. Several alternatively spliced transcript variants encoding a few distinct isoforms have been reported. [provided by RefSeq, May 2011]

Uniprot Accession IDs

• P14618
• A6NFK3
• B2R5N8
• B3KRY0
• B4DFX8
• B4DUU6
• P14786
• Q53GK4
• Q96E76
• Q9BWB5
• Q9UCV6
• Q9UPF2

Gene Name

• PKM

Ensembl ID

• ENST00000319622
• ENSP00000320171
• ENSG00000067225
• ENST00000335181
• ENSP00000334983
• ENST00000449901
• ENSP00000403365
• ENST00000565154
• ENSP00000455901
• ENST00000565184
• ENSP00000455736
• ENST00000568459
• ENSP00000456970

Symbol

• OIP3
• PK2
• PK3
• PKM2
• PK3
• TCB
• OIP3
• PKM2
• CTHBP
• THBP1
• HEL-S-30

Knowledge Table

Most Knowledge About	Knowledge Value (0 to 1 scale)
interacting protein	1
viral protein	1
virus	1
molecular function	0.99
protein complex	0.98

Protein Classes

DTO Classes

Protein / Kinase / Non-protein Kinase / Other Small Molecule Kinase / Pyruvate Kinase Pkm

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: 1543.92   (req: < 5)

Gene RIFs: 281   (req: <= 3)

Antibodies: 1066   (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: 1543.92   (req: >= 5)

Gene RIFs: 281   (req: > 3)

Antibodies: 1066   (req: > 50)

- OR - satisfy the following criterion:

Gene Ontology Terms: 25

Tchem

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

Active Ligands: 16

Tclin

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

Active Drug: 0

Protein Sequence and Structure

Residue Counts

Protein Sequence

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Expression Data (0 Tissues)

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No expression data found

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Target Illumination GWAS Analytics (TIGA)

TIGA scores and ranks GWAS discovered associations according to the quantity and quality of the evidence supporting the association.

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GENEVA

GENEVA (GENe Expression Variance Analysis) allows you to identify RNA-sequencing datasets from the Gene Expression Omnibus (GEO) that contain conditions modulating a gene or a gene signature.

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GlyGen

GlyGen is a data integration and dissemination project for carbohydrate and glycoconjugate related data.

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ARCHS4

ARCHS4 provides access to gene-function predictions based on RNA-seq co-expression, and gene expression levels across cell and tissues.

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Approved Drugs (0)

No approved drugs found

Active Ligands (16)

Explore Active Ligands

1 – 10 of 16

CHEMBL4071498

PKMTchem Kinase

pAC50 : 8.49

Micheliolide

PKMTchem Kinase

pEC50 : 8.22

CHEMBL1084899

PKMTchem Kinase

pAC50 : 7.96

CHEMBL3104587

PKMTchem Kinase

pAC50 : 7.96

CHEMBL4070458

PKMTchem Kinase

pAC50 : 7.85

CHEMBL4466655

PKMTchem Kinase

pAC50 : 7.82

CHEMBL1085647

PKMTchem Kinase

pAC50 : 7.8

CHEMBL3335791

PKMTchem Kinase

pAC50 : 7.77

CHEMBL1086349

PKMTchem Kinase

pAC50 : 7.75

CHEMBL2385099

PKMTchem Kinase

pEC50 : 7.66

Protein-Protein Interactions (496)

Explore Interacting Targets

1 – 10 of 496

• See Interactions on String-DB

GREM2

Tbio

Novelty:  0.01839564

p_int:  0.874895559

p_ni:  0.125104441

Data Source:  BioPlex

FAM24B

Tdark

Novelty:  1.04675689

p_int:  0.874627622

p_ni:  0.125372378

Data Source:  BioPlex

CYP1A1

Tchem

Novelty:  0.0002404

p_int:  0.767213419

p_ni:  0.232786581

Score:  0.364

Data Source:  BioPlex,STRINGDB

SNRNP27

Tbio

Novelty:  0.0175187

p_int:  0.766843414

p_ni:  0.233156586

Data Source:  BioPlex

DDX19B

Tbio

Family:  Enzyme

Novelty:  0.0504568

p_int:  0.765904555

p_ni:  0.234095445

Score:  0.19

Data Source:  BioPlex,STRINGDB

PAPLN

Tbio

Novelty:  0.06871524

p_int:  0.756537652

p_ni:  0.243462348

Score:  0.19

Data Source:  BioPlex,STRINGDB

SEMA4C

Tbio

Novelty:  0.01237067

p_int:  0.752493335

p_ni:  0.247506665

Data Source:  BioPlex

ENO1

Tchem

Family:  Enzyme

Novelty:  0.00109178

Score:  0.993

Data Source:  STRINGDB

ENO3

Tbio

Family:  Enzyme

Novelty:  0.00322051

Score:  0.989

Data Source:  STRINGDB

GPI

Tbio

Family:  Enzyme

Novelty:  0.00095404

Score:  0.987

Data Source:  STRINGDB

Nearest Tclin Targets (7)

Explore Nearest Tclin Targets

Upstream (7)

1 – 5 of 7

GUCY1B1

Tclin

Family:  Enzyme

KEGG Distance:  1

Common Pathways:  2

1: Metabolic pathways

2: Purine metabolism

NPR1

Tclin

Family:  Kinase

KEGG Distance:  1

Common Pathways:  2

1: Metabolic pathways

2: Purine metabolism

RRM2

Tclin

Family:  Enzyme

KEGG Distance:  1

Common Pathways:  2

1: Metabolic pathways

2: Purine metabolism

GUCY1A1

Tclin

Family:  Enzyme

KEGG Distance:  1

Common Pathways:  2

1: Metabolic pathways

2: Purine metabolism

GUCY2C

Tclin

Family:  Kinase

KEGG Distance:  1

Common Pathways:  2

1: Metabolic pathways

2: Purine metabolism

Pathways (32)

Reactome (7)

KEGG (11)

PathwayCommons (8)

UniProt (1)

WikiPathways (5)

Glucose metabolism (R-HSA-70326)

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5

1 – 5 of 7

Data Source	Name	Explore in Pharos	Explore in Source
Reactome	Glucose metabolism	92 targets	R-HSA-70326
Reactome	Glycolysis	72 targets	R-HSA-70171
Reactome	Immune System	2246 targets	R-HSA-168256
Reactome	Innate Immune System	1188 targets	R-HSA-168249
Reactome	Metabolism	2112 targets	R-HSA-1430728

Name	Explore in Pharos	Explore in Source
Glucose metabolism	92 targets	R-HSA-70326
Glycolysis	72 targets	R-HSA-70171
Immune System	2246 targets	R-HSA-168256
Innate Immune System	1188 targets	R-HSA-168249
Metabolism	2112 targets	R-HSA-1430728

Viral Interactions (0)

No viral interactions found

Gene Ontology Terms (39)

Functions (11)

Components (14)

Processes (14)

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Items per page:

10

1 – 10 of 11

GO Term	Evidence	Assigned by
pyruvate kinase activity	Inferred from Direct Assay (IDA)	CACAO
cadherin binding	Inferred from High Throughput Direct Assay (HDA)	BHF-UCL
MHC class II protein complex binding	Inferred from High Throughput Direct Assay (HDA)	UniProtKB
RNA binding	Inferred from High Throughput Direct Assay (HDA)	UniProtKB
ADP binding	Inferred from Electronic Annotation (IEA)	Ensembl
ATP binding	Inferred from Electronic Annotation (IEA)	UniProtKB-KW
identical protein binding	Inferred from Electronic Annotation (IEA)	Ensembl
kinase activity	Inferred from Electronic Annotation (IEA)	UniProtKB-KW
magnesium ion binding	Inferred from Electronic Annotation (IEA)	InterPro
potassium ion binding	Inferred from Electronic Annotation (IEA)	InterPro

Disease Associations ()

No disease associations found

GWAS Traits (2)

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5

1 – 2 of 2

GWAS Trait	EFO ID	Study Count	SNP Count	Beta Count	Odds Ratio	Evidence (Mean Rank Score)	Provenance
aspartate aminotransferase measurement	EFO_0004736	1	1	0	5.9	30.2
serum alanine aminotransferase measurement	EFO_0004735	1	1	0	5.5	1.5

• Explore on Target Illumination GWAS Analytics (TIGA)

Items per page:

5

1 – 2 of 2

GWAS Trait	EFO ID	Beta Count	Odds Ratio	Evidence (Mean Rank Score)	Provenance
aspartate aminotransferase measurement	EFO_0004736	0	5.9	30.2
serum alanine aminotransferase measurement	EFO_0004735	0	5.5	1.5

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UniProt Keyword Find Similar Targets

No Header	No Header
3D-structure
Acetylation
Allosteric enzyme
Alternative splicing
ATP-binding
Complete proteome
Cytoplasm
Direct protein sequencing
Glycolysis
Hydroxylation

GWAS Trait Find Similar Targets

No Header	No Header
aspartate aminotransferase measurement
serum alanine aminotransferase measurement

MGI Phenotype Find Similar Targets

No Header	No Header
mortality/aging

IDG Resources

No IDG generated resources found

Orthologs (10)

1 – 5 of 10

Species	Name	Source ID	Gene ID	OMA	EggNOG	Inparanoid
Chimp	pyruvate kinase M1/2	VGNC:49018	748700
Macaque	pyruvate kinase M1/2		697742
Mouse	pyruvate kinase, muscle	MGI:97591	18746
Rat	pyruvate kinase M1/2	RGD:3337	25630
Dog	pyruvate kinase M1/2		403874

Species	Name	OMA	EggNOG	Inparanoid
Chimp	pyruvate kinase M1/2
Macaque	pyruvate kinase M1/2
Mouse	pyruvate kinase, muscle
Rat	pyruvate kinase M1/2
Dog	pyruvate kinase M1/2

Publication Statistics

PubMed Score 1543.92

PubMed score by year

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PubTator Score 558.71

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Patents

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Related Publications

Text Mined References (340)

GeneRif Annotations (281)

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PMID	Year	Title