Targeting mutant fibroblast growth factor receptors in cancer.

Trends Mol Med
Authors
Keywords
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.

Year of Publication
2011
Journal
Trends Mol Med
Volume
17
Issue
5
Pages
283-92
Date Published
2011 May
ISSN
1471-499X
URL
DOI
10.1016/j.molmed.2011.01.012
PubMed ID
21367659
PubMed Central ID
PMC3809064
Links
Grant list
P50 CA134254 / CA / NCI NIH HHS / United States