Q12866

Background

Protein Name
Tyrosine-protein kinase Mer
Gene Name
MERTK
Organism
Homo sapiens

Annotations

Function
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.

Mapping Statistics

Site Maximum Consensus Site Population Minimum Consensus Site Population Median Consensus Site Population
MPP 37 2 16.0
AAS 20 5 9.0
MT3 19 2 6.0
ATP 17 2 9.0
DFG 10 7 8.5
CMP 21 2 12.0
PMP 3 3 3.0
EDI 10 2 3.0
DRS 13 2 9.0
PDIG 15 10 12.5
PIF 19 3 13.0

Mapping Results

PDB ID Maximum Consensus Site Population
MPP site AAS site MT3 site LBP site ATP site DEF site DFG site CMP site PMP site EDI site DRS site PDIG site PIF site
Total Druggable Structures per Site 7 1 4 0 1 0 0 2 0 0 0 0 2
3TCP 28 20 17 0 10 0 0 17 0 0 9 0 15
3BPR 22 0 12 0 12 0 10 14 0 0 10 0 0
AFQ12866 0 0 0 0 0 0 0 0 0 0 0 0 0
4M3Q 24 5 0 0 11 0 0 0 0 0 13 0 0
2P0C 24 0 18 0 11 0 0 21 3 2 0 13 13
4MHA 25 0 19 0 17 0 0 0 0 0 11 15 3
3BRB 37 0 17 0 9 0 0 5 0 10 2 10 19
4MH7 16 5 5 0 8 0 0 0 0 4 9 12 16