Search results for "FGFR"
showing 4 items of 24 documents
Design of copper(II) complexes as potential anticancer prodrugs
The fibroblast growth factor receptors (FGFR) are tyrosine kinases that are present in many types of endothelial and tumor cells and play an important role in cell growth, survival, and migration as well as in maintaining tumor angiogenesis (1). FGFR genetic alterations are frequently observed in cancer, suggesting that FGFR inhibition may be a promising therapy in patients harboring these lesions (2). In particular, molecules with structural properties similar to Ponatinib, a known inhibitor of FGFR, that shows a selective interaction for the ATP binding site of the isoform 4 of these receptors (FGFR4), are being considered. Molecular modeling studies have been conducted to design novel po…
Interactions between cholinergic and fibroblast growth factor receptors in brain trophism and plasticity
2014
Acetylcholine, acting on both nicotinic receptors (nAChRs) and muscarinic receptors (mAChRs), plays a role in the regulation of synaptic plasticity, being involved in the regulation of cellular processes and cognitive functions, such as learning, memory and attention. Recently, G protein coupled receptors (GPCRs), including mAChRs, have been reported to transactivate tyrosine-kinase receptors (RTK), such as epidermal growth factor receptor (EGFR), and initiate their intracellular signaling. In this minireview we have first analysed the RTK transactivation mechanisms, involving cholinergic receptors, and thereafter the interplay between AChR and neurotrophic factor systems built up by FGF2 a…
Serotonin receptor agonist treatment induces transactivation of fibroblast growth factor receptor-1 (FGFR1) tyrosine kinase in the rat hippocampal ne…
2010
Over the past decade, many examples of activation of receptor tyrosine kinases in response to G-protein coupled receptor signaling have been reported, indicating that there are alternative modes of receptor tyrosine kinase activation (transactivation) in the absence of neurotrophic factor binding. In the present work, we aimed to examine if 5-HT receptor subtype activation may induce fibroblast growth factor receptor-1 (FGFR1) phosphorylation through transactivation of tyrosine kinase. The study has been performed in young adult rats treated with the selective 5-HT1A receptor agonist 8-OHDPAT at the dose of 0.4 mg/kg/i.p.. FGFR1 phosphorylation was evaluated by immunoprecipitation and weste…
Papel de IRS2 en la reparación del daño hepático y cáncer
2019
La resistencia a insulina es una característica típica de la diabetes tipo 2 y la obesidad, patologías vinculadas a un alto riesgo del desarrollo de enfermedades crónicas hepáticas y hepatocarcinoma. Sin embargo, se desconoce el papel que la resistencia a insulina pueda ejercer durante el daño hepático crónico y durante la hepatocarcinogénesis, por lo que se ha abordado esta cuestión a través del estudio del substrato receptor de insulina 2 (IRS2), principal promotor de la señalización de insulina en el hígado. La experimentación llevada a cabo durante este proyecto muestra que la deleción del gen Irs2 en el modelo murino Irs2-/- impide la inducción de Fgf7 en células estromales durante el …