c-mer proto-oncogene tyrosine kinase (MERTK) (MERTK)

c-mer proto-oncogene tyrosine kinase (MERTK) is a member of the TAM (Tyro3, Axl, Mer) family of receptor tyrosine kinases (UniProt P51813). It plays a critical role in efferocytosis, the process by which phagocytes remove apoptotic cells, thereby maintaining tissue homeostasis and preventing chronic inflammation (Lemke, 2013, Nature Reviews Immunology). In the tumor microenvironment, MERTK is often overexpressed on both tumor cells and tumor-associated macrophages, where it promotes cell survival, migration, and an immunosuppressive environment that facilitates tumor escape (Graham et al., 2014, Nature Reviews Cancer). Mutations in the MERTK gene are notably associated with retinitis pigmentosa due to the failure of retinal pigment epithelial cells to phagocytose photoreceptor outer segments (Gal et al., 2000, Nature Genetics). Therapeutic strategies primarily focus on small molecule inhibitors like Sitravatinib and MRX-2843 to block MERTK signaling in oncology (ClinicalTrials.gov NCT02219711, NCT03510169). However, therapeutic development faces challenges such as potential retinal toxicity due to MERTK's essential role in the eye. The target name provided, MERTK mRNA, is considered incorrect as the therapeutic target is the protein product rather than the messenger RNA transcript itself.

Other names

MERTyro12c-EykSTK kinaseProto-oncogene c-MerReceptor tyrosine kinase Mer

Inhibition of the intracellular tyrosine kinase domain to block downstream signaling pathways such as PI3K/AKT, MAPK/ERK, and STAT, thereby reducing cell survival and restoring anti-tumor immune responses.