Mechanism
c-Kit (CD117); also PDGFR, Lck, FAK, FGFR3, CSF1R
Assets acting on this target.
- Class
- Multi-target tyrosine kinase inhibitor (mast cell/kinase inhibitor)
- Pathway
- Mast cell activation / receptor tyrosine kinase signaling
c-Kit (CD117) is a receptor tyrosine kinase that, when activated by its ligand stem cell factor, drives the growth, survival, and activation of mast cells, along with several other cell types including hematopoietic progenitors and melanocytes. Because mast cells are central to allergic and inflammatory responses, and because uncontrolled c-Kit signaling can also drive tumor growth, inhibiting this receptor is a strategy used both in inflammatory/autoimmune conditions and in certain cancers. This mechanism describes a multi-target kinase inhibitor that blocks c-Kit alongside several related enzymes: PDGFR, another growth-factor receptor with overlapping roles in tumor and stromal biology; Lck, a signaling kinase in T lymphocytes; FAK, involved in cell adhesion and migration; FGFR3, a growth-factor receptor implicated in some cancers; and CSF1R, which governs macrophage development. By simultaneously dampening several of these pathways, such an inhibitor can suppress mast cell activation while also curbing T-cell and macrophage contributions to disease, an approach relevant to mast cell disorders, certain fibrotic and autoimmune diseases, and kinase-driven tumors. The broad target profile is intended to address diseases where multiple immune and stromal cell types, not just mast cells alone, sustain pathology.
Explore this mechanism at different depths
Research adds deeper and simplified explanation variants while preserving the same scientific register and source caveats.
1 of 1 assets