Article
Identification of a farnesol analog as a Ras function inhibitor using both an in vivo Ras activation sensor and a phenotypic screening approach.
Molecular and cellular biochemistry - 1 Feb 2014
Srinivasan Kamalakkannan, Subramanian Thangaiah, Spielmann H Peter, Janetopoulos Chris
Abstract excerpt
Mutations in Ras isoforms such as K-Ras, N-Ras, and H-Ras contribute to roughly 85, 15, and 1% of human cancers, respectively. Proper membrane targeting of these Ras isoforms, a prerequisite for Ras activity, requires farnesylation or geranylgeranylation at the C-terminal CAAX box. We devised an in vivo screening strategy based on monitoring Ras activation and phenotypic physiological outputs for assaying...
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