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Nat Rev Cancer. 2010 Dec;10(12):842-57. doi: 10.1038/nrc2960. Epub 2010 Nov 24.

Ras superfamily GEFs and GAPs: validated and tractable targets for cancer therapy?

Author information

1
University of North Carolina at Chapel Hill, Lineberger Comprehensive Cancer Center, Department of Pharmacology, Chapel Hill, North Carolina 27599, USA.

Abstract

There is now considerable and increasing evidence for a causal role for aberrant activity of the Ras superfamily of small GTPases in human cancers. These GTPases function as GDP-GTP-regulated binary switches that control many fundamental cellular processes. A common mechanism of GTPase deregulation in cancer is the deregulated expression and/or activity of their regulatory proteins, guanine nucleotide exchange factors (GEFs) that promote formation of the active GTP-bound state and GTPase-activating proteins (GAPs) that return the GTPase to its GDP-bound inactive state. In this Review, we assess the association of GEFs and GAPs with cancer and their druggability for cancer therapeutics.

PMID:
21102635
PMCID:
PMC3124093
DOI:
10.1038/nrc2960
[Indexed for MEDLINE]
Free PMC Article

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