[HTML][HTML] Pharmacologically targeting the myristoylation of the scaffold protein FRS2α inhibits FGF/FGFR-mediated oncogenic signaling and tumor progression
Fibroblast growth factor (FGF)/FGF receptor (FGFR) signaling facilitates tumor initiation and
progression. Although currently approved inhibitors of FGFR kinase have shown therapeutic
benefit in clinical trials, overexpression or mutations of FGFRs eventually confer drug
resistance and thereby abrogate the desired activity of kinase inhibitors in many cancer
types. In this study, we report that loss of myristoylation of fibroblast growth factor receptor
substrate 2 (FRS2α), a scaffold protein essential for FGFR signaling, inhibits FGF/FGFR …
progression. Although currently approved inhibitors of FGFR kinase have shown therapeutic
benefit in clinical trials, overexpression or mutations of FGFRs eventually confer drug
resistance and thereby abrogate the desired activity of kinase inhibitors in many cancer
types. In this study, we report that loss of myristoylation of fibroblast growth factor receptor
substrate 2 (FRS2α), a scaffold protein essential for FGFR signaling, inhibits FGF/FGFR …