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Trends Mol Med DOI:10.1016/j.molmed.2011.01.012

Targeting mutant fibroblast growth factor receptors in cancer.

Publication TypeJournal Article
Year of Publication2011
AuthorsGreulich, H, Pollock, PM
JournalTrends Mol Med
Date Published2011 May
KeywordsClinical Trials as Topic, Humans, Molecular Targeted Therapy, Mutation, Neoplasms, Protein Kinase Inhibitors, Receptors, Fibroblast Growth Factor

Fibroblast growth factor receptors (FGFRs) play diverse roles in the control of cell proliferation, cell differentiation, angiogenesis and development. Activating the mutations of FGFRs in the germline has long been known to cause a variety of skeletal developmental disorders, but it is only recently that a similar spectrum of somatic FGFR mutations has been associated with human cancers. Many of these somatic mutations are gain-of-function and oncogenic and create dependencies in tumor cell lines harboring such mutations. A combination of knockdown studies and pharmaceutical inhibition in preclinical models has further substantiated genomically altered FGFR as a therapeutic target in cancer, and the oncology community is responding with clinical trials evaluating multikinase inhibitors with anti-FGFR activity and a new generation of specific pan-FGFR inhibitors.


Alternate JournalTrends Mol Med
PubMed ID21367659
PubMed Central IDPMC3809064
Grant ListP50 CA134254 / CA / NCI NIH HHS / United States