Targeting the Fibroblast Growth Factor Receptors for the Treatment of Cancer
Steven M. Lemieux,
M. Kyle Hadden.
Receptor tyrosine kinases (RTKs) are transmembrane proteins that play a critical role in stimulating signal transduction
cascades to influence cell proliferation, growth, and differentiation and they have also been shown to promote angiogenesis when they
are up-regulated or mutated. For this reason, their dysfunction has been implicated in the development of human cancer. Over the past
decade, much attention has been devoted to developing inhibitors and antibodies against several classes of RTKs, including vascular
endothelial growth factor receptors (VEGFRs), epidermal growth factor receptors (EGFRs), and platelet-derived growth factor receptors
(PDGFRs). More recently, interest in the fibroblast growth factor receptor (FGFR) class of RTKs as a drug target for the treatment of
cancer has emerged. Signaling through FGFRs is critical for normal cellular function and their dysregulation has been linked to various
malignancies such as breast and prostate cancer. This review will focus on the current state of both small molecules and antibodies as
FGFR inhibitors to provide insight into their development and future potential as anti-cancer agents.
Keywords: Antibodies, ATP Binding Site, Cancer, Fibroblast Growth Factor Receptor, Indolinone, Pyrido[2, 3-d]pyrimidine, Small Molecules,
Tyrosine Kinase Inhibitor.
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