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Trends Mol Med. 2011 May;17(5):283-92. doi: 10.1016/j.molmed.2011.01.012. Epub 2011 Mar 1.

Targeting mutant fibroblast growth factor receptors in cancer.

Author information

1
Dana-Farber Cancer Institute, Boston, MA 02115, USA. heidig@broadinstitute.org

Abstract

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.

PMID:
21367659
PMCID:
PMC3809064
DOI:
10.1016/j.molmed.2011.01.012
[Indexed for MEDLINE]
Free PMC Article

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