Tchem MERTK Tyrosine-protein kinase Mer

Protein Summary

Description

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 signaling molecules. Following activation by ligand, interacts with GRB2 or PLCG2 and induces phosphorylation of MAPK1, MAPK2, FAK/PTK2 or RAC1. MERTK signaling plays a role in various processes such as macrophage clearance of apoptotic cells, platelet aggregation, cytoskeleton reorganization and engulfment. Functions in the retinal pigment epithelium (RPE) as a regulator of rod outer segments fragments phagocytosis. Plays also an important role in inhibition of Toll-like receptors (TLRs)-mediated innate immune response by activating STAT1, which selectively induces production of suppressors of cytokine signaling SOCS1 and SOCS3. This gene is a member of the MER/AXL/TYRO3 receptor kinase family and encodes a transmembrane protein with two fibronectin type-III domains, two Ig-like C2-type (immunoglobulin-like) domains, and one tyrosine kinase domain. Mutations in this gene have been associated with disruption of the retinal pigment epithelium (RPE) phagocytosis pathway and onset of autosomal recessive retinitis pigmentosa (RP). [provided by RefSeq, Jul 2008]

Uniprot Accession IDs

• Q12866
• Q9HBB4

Gene Name

• MERTK

Ensembl ID

• ENST00000295408
• ENSP00000295408
• ENSG00000153208
• ENST00000421804
• ENSP00000389152

Symbol

• MER
• MER
• RP38
• c-Eyk
• c-mer
• Tyro12

Knowledge Table

Most Knowledge About	Knowledge Value (0 to 1 scale)
protein domain	1
molecular function	0.98
kinase perturbation	0.88
small molecule	0.85
biological process	0.84

Protein Classes

DTO Classes

Protein / Kinase / Protein Kinase / Tk Group / Axl Family / Tyrosine-protein Kinase Mer

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: 420.71   (req: < 5)

Gene RIFs: 148   (req: <= 3)

Antibodies: 780   (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: 420.71   (req: >= 5)

Gene RIFs: 148   (req: > 3)

Antibodies: 780   (req: > 50)

- OR - satisfy the following criterion:

Gene Ontology Terms: 28

Tchem

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

Active Ligands: 200

Tclin

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

Active Drugs: 4