MERTK
MERTK (Tyrosine-protein kinase Mer) 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 a biomarker, and clinical evidence ties its variants to diagnosis, prognosis or drug response. Tied to Melanoma.
Overview
Receptor tyrosine kinase that transduces signals from the extracellular matrix into the cytoplasm by binding to several ligands including LGALS3, TUB, TULP1 or GAS6. Regulates many physiological processes including cell survival, migration, differentiation, and phagocytosis of apoptotic cells (efferocytosis). Ligand binding at the cell surface induces autophosphorylation of MERTK on its intracellular domain that provides docking sites for downstream signalling molecules.
CIViC holds 1 clinical evidence item and 0 assertions across 1 variant, naming UNC1062.
- Target · the protein and the cell it sits on
- Drug · antibody, small molecule, cell or radioligand
- Effect · signal, damage or kill
In plain words · MERTK (Tyrosine-protein kinase Mer) 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 a biomarker, and clinical evidence ties its variants to diagnosis, prognosis or drug response. Tied to Melanoma.
- 1 · What it is
MERTK (Tyrosine-protein kinase Mer) 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 a biomarker, and clinical evidence ties its variants to diagnosis, prognosis or drug response. Tied to Melanoma.
- 2 · What goes wrong in cancer
Receptor tyrosine kinase that transduces signals from the extracellular matrix into the cytoplasm by binding to several ligands including LGALS3, TUB, TULP1 or GAS6.
- 3 · How drugs use it
No product in this corpus aims at MERTK 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:7027 (approved symbol, name, aliases, locus and cross-references (hgnc_complete_set.txt)); UniProt Q12866 (protein name, function text, keywords and locations (REST API)); CIViC gene MERTK (1 evidence items, 0 assertions, 1 variants; diseases: Melanoma (GraphQL API, CC0))
Biology
Receptor tyrosine kinase that transduces signals from the extracellular matrix into the cytoplasm by binding to several ligands including LGALS3, TUB, TULP1 or GAS6. Regulates many physiological processes including cell survival, migration, differentiation, and phagocytosis of apoptotic cells (efferocytosis). Ligand binding at the cell surface induces autophosphorylation of MERTK on its intracellular domain that provides docking sites for downstream signalling molecules. Following activation by ligand, interacts with GRB2 or PLCG2 and induces phosphorylation of MAPK1, MAPK2, FAK/PTK2 or RAC1. MERTK signalling plays a role in various processes such as macrophage clearance of apoptotic cells, platelet aggregation, cytoskeleton reorganisation and engulfment. Functions in the retinal pigment epithelium (RPE) as a regulator of rod outer segments fragments phagocytosis. Location: Cell membrane (UniProt). Locus 2q13 (HGNC).
- Melanoma: CIViC evidence names this disease
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: CIViC lists 1 therapies; CIViC holds 1 clinical evidence items on its variants. Evidence tier "clinical-evidence" is the strongest of those signals.
- Prevalence not recorded: none of the sources gives a positivity rate.
Latest papers
topQuery for this target: (TITLE:"MERTK" OR ABSTRACT:"MERTK" OR TITLE:"MER proto-oncogene, tyrosine kinase" OR ABSTRACT:"MER proto-oncogene, tyrosine kinase" OR TITLE:"Tyrosine-protein kinase Mer" OR ABSTRACT:"Tyrosine-protein kinase Mer" OR TITLE:"mer" OR ABSTRACT:"mer" OR TITLE:"RP38" OR ABSTRACT:"RP38" OR TITLE:"c-Eyk" OR ABSTRACT:"c-Eyk") 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 MERTK, not a curated reading list.