Tclin ERBB3 Receptor tyrosine-protein kinase erbB-3

Protein Summary

Description

Tyrosine-protein kinase that plays an essential role as cell surface receptor for neuregulins. Binds to neuregulin-1 (NRG1) and is activated by it; ligand-binding increases phosphorylation on tyrosine residues and promotes its association with the p85 subunit of phosphatidylinositol 3-kinase (PubMed:20682778). May also be activated by CSPG5 (PubMed:15358134). This gene encodes a member of the epidermal growth factor receptor (EGFR) family of receptor tyrosine kinases. This membrane-bound protein has a neuregulin binding domain but not an active kinase domain. It therefore can bind this ligand but not convey the signal into the cell through protein phosphorylation. However, it does form heterodimers with other EGF receptor family members which do have kinase activity. Heterodimerization leads to the activation of pathways which lead to cell proliferation or differentiation. Amplification of this gene and/or overexpression of its protein have been reported in numerous cancers, including prostate, bladder, and breast tumors. Alternate transcriptional splice variants encoding different isoforms have been characterized. One isoform lacks the intermembrane region and is secreted outside the cell. This form acts to modulate the activity of the membrane-bound form. Additional splice variants have also been reported, but they have not been thoroughly characterized. [provided by RefSeq, Jul 2008]

Uniprot Accession IDs

• P21860
• A8K6L6
• B4DIK7
• B4DV32
• E9PDT8
• Q9BUD7

Gene Name

• ERBB3

Ensembl ID

• ENST00000267101
• ENSP00000267101
• ENSG00000065361
• ENST00000411731
• ENSP00000415753
• ENST00000415288
• ENSP00000408340
• ENST00000551242
• ENSP00000447510

Symbol

• HER3
• HER3
• FERLK
• LCCS2
• ErbB-3
• c-erbB3
• erbB3-S
• MDA-BF-1
• c-erbB-3
• p180-ErbB3
• p45-sErbB3
• p85-sErbB3

Knowledge Table

Most Knowledge About	Knowledge Value (0 to 1 scale)
molecular function	1
protein domain	0.99
transcription factor perturbation	0.98
hub protein	0.97
kinase perturbation	0.95

Protein Classes

DTO Classes

Protein / Kinase / Protein Kinase / Tk Group / Egfr Family / Receptor Tyrosine-protein Kinase Erbb-3

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: 1145.12   (req: < 5)

Gene RIFs: 411   (req: <= 3)

Antibodies: 2081   (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: 1145.12   (req: >= 5)

Gene RIFs: 411   (req: > 3)

Antibodies: 2081   (req: > 50)

- OR - satisfy the following criterion:

Gene Ontology Terms: 42

Tchem

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

Active Ligands: 21

Tclin

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

Active Drugs: 6