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Beschreibung

Tyrosine-protein kinase Mer (UniProt: Q12866, also known as EC:2.7.10.1, Proto-oncogene c-Mer, Receptor tyrosine kinase MerTK) is encoded by the MERTK (also known as MER) gene (Gene ID: 10461) in human. MerTK is a single-pass type I membrane glycoprotein that is synthesized with a signal peptide (aa 1-20), which is subsequently cleaved off to generate the mature form that contains an extracellular domain (aa 21-505), a transmembrane domain (aa 506-526), and a cytoplasmic domain (aa 27-999). Its protein kinase domain is localized to amino acids 587-858. MerTK is highly expressed in testis, ovary, prostate, lung, and kidney tissue. Its expression is not observed in normal B- and T-cells but is expressed in several neoplastic B- and T-cell lines. Overexpression of MerTK has also been reported in non-small cell lung cancer (NSCLC). It is involved in the regulation of cell survival, migration, differentiation, and phagocytosis of apoptotic cells. It transduces signals from the extracellular matrix into the cytoplasm by binding to several ligands, including galectin-3, Tubby protein, Tubby-related protein 1, and GAS6, a member of the Axl subfamily of receptor protein-tyrosine kinases. Ligand binding at the cell surface induces autophosphorylation of MerTK on its intracellular domain that provides docking sites for downstream signaling molecules. Its autophosphorylation on tyrosines 749, 753, and 754 in the activation loop imparts full activity. It is also autophosphorylated on tyrosine 872 that leads to recruitment of downstream partners of the signaling cascade such as phospholipase C ?2. Clone Mer590 is shown to rapidly reduce total and surface expression of MerTK and prevents its phosphorylation and downstream signaling. It is also shown to enhance carboplatin induced apoptosis in Colo699 cells and diminish glioblastoma cell migration in vitro. (Ref.: Cummings, CT., et al. (2014). Oncotarget, 5(21), 10434-45, Rogers, AEJ., et al. (2012). Oncogene. 31(38): 4171 4181).