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Fibroblast growth factor receptor 1 (FGFR1) is a receptor tyrosine kinase (RTK) that, together with the extracellular fibroblast growth factors (FGFs), is involved in transmission of signals across the plasma membrane. FGFR1-dependent signaling regulates various biological processes like cell migration, proliferation, and apoptosis. Aberrant activity of this receptor causes many developmental disorders and is detected in numerous cancers. Overexpression of FGFR1 has been observed in various tumor types, like lung, breast, ovarian, prostate, head, and neck cancers. FGFR1 is very efficiently internalized by several endocytic pathways, and thus, its endocytosis can be hijacked for rapid intracellular drug delivery. Importantly, complexes of ligands/targeting molecules with FGFR1 avoid the unfavorable recycling pathway and are predominantly sorted to lysosomes for degradation and cytotoxic drug release. All these features make FGFR1 an attractive molecular target for selective anticancer therapies.