Making way for suppressing the FGF19/FGFR4 axis in cancer

FGF19 is a noncanonical FGF ligand that can control a broad spectrum of physiological responses, which include bile acid homeostasis, liver metabolism and glucose uptake. Many of these responses are mediated by FGF19 binding to its FGFR4/β-klotho receptor complex and controlling activation of an arr...

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Bibliographic Details
Published in:Future medicinal chemistry 2018-10, Vol.10 (20), p.2457-2470
Main Authors: Prieto-Dominguez, Nestor, Shull, Austin Y, Teng, Yong
Format: Article
Language:English
Subjects:
Animals
anticancer
Antineoplastic Agents - metabolism
Bile Acids and Salts - metabolism
Carcinogenesis - metabolism
Cell Line, Tumor
Cell Proliferation - drug effects
Cell Survival - drug effects
FGF19
FGFR4
Fibroblast Growth Factors - genetics
Fibroblast Growth Factors - metabolism
Humans
inhibitors
Membrane Proteins - metabolism
Molecular Targeted Therapy - methods
oncogenic role
Protein Binding
Receptor, Fibroblast Growth Factor, Type 4 - metabolism
Signal Transduction
signaling transduction
treatment regimens
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Summary:FGF19 is a noncanonical FGF ligand that can control a broad spectrum of physiological responses, which include bile acid homeostasis, liver metabolism and glucose uptake. Many of these responses are mediated by FGF19 binding to its FGFR4/β-klotho receptor complex and controlling activation of an array of intracellular signaling events. Overactivation of the FGF19/FGFR4 axis has been implicated in tumorigenic formation, progression and metastasis, and inhibitors of this axis have recently been developed for single agent use or in combination with other anticancer drugs. Considering the critical role of this receptor complex in cancer, this review focuses on recent developments and applications of FGF19/FGFR4-targeted therapeutics.
ISSN:1756-8919
1756-8927
DOI:10.4155/fmc-2018-0099