Tchem FGR Tyrosine-protein kinase Fgr

Protein Summary

Description

Non-receptor tyrosine-protein kinase that transmits signals from cell surface receptors devoid of kinase activity and contributes to the regulation of immune responses, including neutrophil, monocyte, macrophage and mast cell functions, cytoskeleton remodeling in response to extracellular stimuli, phagocytosis, cell adhesion and migration. Promotes mast cell degranulation, release of inflammatory cytokines and IgE-mediated anaphylaxis. Acts downstream of receptors that bind the Fc region of immunoglobulins, such as MS4A2/FCER1B, FCGR2A and/or FCGR2B. Acts downstream of ITGB1 and ITGB2, and regulates actin cytoskeleton reorganization, cell spreading and adhesion. Depending on the context, activates or inhibits cellular responses. Functions as negative regulator of ITGB2 signaling, phagocytosis and SYK activity in monocytes. Required for normal ITGB1 and ITGB2 signaling, normal cell spreading and adhesion in neutrophils and macrophages. Functions as positive regulator of cell migration and regulates cytoskeleton reorganization via RAC1 activation. Phosphorylates SYK (in vitro) and promotes SYK-dependent activation of AKT1 and MAP kinase signaling. Phosphorylates PLD2 in antigen-stimulated mast cells, leading to PLD2 activation and the production of the signaling molecules lysophosphatidic acid and diacylglycerol. Promotes activation of PIK3R1. Phosphorylates FASLG, and thereby regulates its ubiquitination and subsequent internalization. Phosphorylates ABL1. Promotes phosphorylation of CBL, CTTN, PIK3R1, PTK2/FAK1, PTK2B/PYK2 and VAV2. Phosphorylates HCLS1 that has already been phosphorylated by SYK, but not unphosphorylated HCLS1. This gene is a member of the Src family of protein tyrosine kinases (PTKs). The encoded protein contains N-terminal sites for myristylation and palmitylation, a PTK domain, and SH2 and SH3 domains which are involved in mediating protein-protein interactions with phosphotyrosine-containing and proline-rich motifs, respectively. The protein localizes to plasma membrane ruffles, and functions as a negative regulator of cell migration and adhesion triggered by the beta-2 integrin signal transduction pathway. Infection with Epstein-Barr virus results in the overexpression of this gene. Multiple alternatively spliced variants, encoding the same protein, have been identified. [provided by RefSeq, Jul 2008]

Uniprot Accession IDs

• P09769
• D3DPL7
• Q9UIQ3

Gene Name

• FGR

Ensembl ID

• ENST00000374003
• ENSP00000363115
• ENSG00000000938
• ENST00000374004
• ENSP00000363116
• ENST00000374005
• ENSP00000363117
• ENST00000399173
• ENSP00000382126

Symbol

• SRC2
• SRC2
• c-fgr
• c-src2
• p55-Fgr
• p58-Fgr
• p55c-fgr
• p58c-fgr

Knowledge Table

Most Knowledge About	Knowledge Value (0 to 1 scale)
biological process	0.99
molecular function	0.99
protein domain	0.99
PubMedID	0.91
drug perturbation	0.87

Protein Classes

DTO Classes

Protein / Kinase / Protein Kinase / Tk Group / Src Family / Tyrosine-protein Kinase Fgr

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: 514.77   (req: < 5)

Gene RIFs: 14   (req: <= 3)

Antibodies: 513   (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: 514.77   (req: >= 5)

Gene RIFs: 14   (req: > 3)

Antibodies: 513   (req: > 50)

- OR - satisfy the following criterion:

Gene Ontology Terms: 30

Tchem

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

Active Ligands: 17

Tclin

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

Active Drugs: 3