FGR
FGR (Tyrosine-protein kinase Fgr) is a protein kinase, an enzyme that switches other proteins on by adding phosphate groups. The public catalogues list it as a drug target, and an approved or late-stage drug is recorded against it. Tied to Leukaemia, Myeloproliferative neoplasms, Non-Hodgkin lymphoma and 2 more.
Overview
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.
Open Targets scores its association with cancer at 0.61 (direct and indirect evidence; datatypes literature 0.79, animal model 0.49, genetic association 0.00, clinical 0.96).
- Target · the protein and the cell it sits on
- Drug · antibody, small molecule, cell or radioligand
- Effect · signal, damage or kill
In plain words · FGR (Tyrosine-protein kinase Fgr) is a protein kinase, an enzyme that switches other proteins on by adding phosphate groups. The public catalogues list it as a drug target, and an approved or late-stage drug is recorded against it. Tied to Leukaemia, Myeloproliferative neoplasms, Non-Hodgkin lymphoma and 2 more.
- 1 · What it is
FGR (Tyrosine-protein kinase Fgr) is a protein kinase, an enzyme that switches other proteins on by adding phosphate groups. The public catalogues list it as a drug target, and an approved or late-stage drug is recorded against it. Tied to Leukaemia, Myeloproliferative neoplasms, Non-Hodgkin lymphoma and 2 more.
- 2 · What goes wrong in cancer
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.
- 3 · How drugs use it
No product in this corpus aims at FGR yet. Kinases are switched on by binding ATP inside the cell, so most drugs are small molecules shaped to plug that ATP pocket.
External identifiers
Sources: HGNC HGNC:3697 (approved symbol, name, aliases, locus and cross-references (hgnc_complete_set.txt)); UniProt P09769 (protein name, function text, keywords and locations (REST API)); Open Targets ENSG00000000938 (association with cancer (MONDO_0004992) 0.61; per-cancer scores at or above 0.5: acute lymphoblastic leukaemia 0.55, non-Hodgkin lymphoma 0.55, chronic myelogenous leukaemia, BCR-ABL1 positive 0.58, myeloproliferative neoplasm 0.60, leukaemia 0.61 (GraphQL API, CC0))
Biology
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 reorganisation, cell spreading and adhesion. Depending on the context, activates or inhibits cellular responses. Functions as a negative regulator of ITGB2 signalling, phagocytosis and SYK activity in monocytes. Location: Cell membrane; Cell projection, ruffle membrane; Cytoplasm, cytosol; Cytoplasm, cytoskeleton (UniProt). Locus 1p35.3 (HGNC).
- Leukaemia: Open Targets association 0.61 with leukaemia (MONDO_0005059)
- Myeloproliferative neoplasms: Open Targets association 0.60 with myeloproliferative neoplasm (MONDO_0020076)
- Non-Hodgkin lymphoma: Open Targets association 0.55 with non-Hodgkin lymphoma (MONDO_0018908)
- Chronic myeloid leukaemia: Open Targets association 0.58 with chronic myelogenous leukaemia, BCR-ABL1 positive (MONDO_0011996)
- Acute lymphoblastic leukaemia: Open Targets association 0.55 with acute lymphoblastic leukaemia (MONDO_0004967)
Notes
top- Written by scripts/fetch-cancer-genes.ts from CIViC, Open Targets, IntOGen, HGNC and UniProt; the function text is UniProt's, condensed and in UK spelling. Roles: Open Targets known-drug datatype score 0.97. Evidence tier "approved-drug" is the strongest of those signals.
- Prevalence not recorded: none of the sources gives a positivity rate.
Latest papers
topQuery for this target: (TITLE:"FGR" OR ABSTRACT:"FGR" OR TITLE:"FGR proto-oncogene, Src family tyrosine kinase" OR ABSTRACT:"FGR proto-oncogene, Src family tyrosine kinase" OR TITLE:"Tyrosine-protein kinase Fgr" OR ABSTRACT:"Tyrosine-protein kinase Fgr" OR TITLE:"c-fgr" OR ABSTRACT:"c-fgr" OR TITLE:"p55c-fgr" OR ABSTRACT:"p55c-fgr" OR TITLE:"SRC2" OR ABSTRACT:"SRC2") AND (cancer OR tumor OR tumour OR oncology OR carcinoma OR lymphoma OR leukemia OR leukaemia OR myeloma OR sarcoma OR melanoma OR glioma). Results are unfiltered search hits about FGR, not a curated reading list.
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