Chapter Nineteen - Mer Receptor Tyrosine Kinase: Therapeutic Opportunities in Oncology, Virology, and Cardiovascular Indications

• Autores: Xiaodong Wang, Stephen Frye
• Localización: Annual reports in medicinal chemistry, ISSN 0065-7743, Vol 49, 2014, págs. 301-314
• Idioma: inglés
• Texto completo no disponible (Saber más ...)
• Resumen

  • Abstract Mer is a member of the TAM (Tyro3, Axl, and Mer) receptor tyrosine kinase subfamily with growth arrest specific-6 as one of its endogenous ligands. Elevated Mer activation has been strongly associated with poor prognosis and enhanced survival signaling in many human cancers. The normal biological role of Mer in regulating ingestion of apoptotic material by macrophages and epithelial cells, and the latter stages of platelet aggregation, presents therapeutic opportunities beyond oncology for a Mer-directed tyrosine kinase inhibitor. The activity of highly potent small molecule Mer inhibitors in: (1) animal models of Mer driven tumors, (2) tumors lacking Mer but sensitive to a Mer antagonist's immune stimulatory effects, (3) acute models of coagulation, and (4) enveloped virus infections will be reviewed and discussed.