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Farnesyl: proteintransferase inhibitors as agents to inhibit tumor growth
Author(s) -
Omer Ch. A.,
Anthony N. J.,
BuserDoepner C. A.,
Burkhardt A. L.,
Desolms S. J.,
Dinsmore Ch. J.,
Gibbs J. B.,
Hartman G. D.,
Koblan K. S.,
Lobell R. B.,
Oliff A.,
Williams T. M.,
Kohl N. E.
Publication year - 1997
Publication title -
biofactors
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.204
H-Index - 94
eISSN - 1872-8081
pISSN - 0951-6433
DOI - 10.1002/biof.5520060306
Subject(s) - pharmacology , chemistry , medicine
Ras, a signal‐transducing protein involved in mediating growth factor‐stimulated proliferation, is mutationally activated in over 30% of human tumors. To be functional Ras must bind to the inner surface of the plasma membrane, with post‐translational lipid modifications being necessary for this localization. The essential, first modification of Ras is farnesylation catalyzed by the enzyme farnesyl: proteintransferase (FPTase). Inhibitors of FPTase (FTIs) are currently being tested to determine if they are capable of tumor growth inhibition. Here we describe our efforts, along with those of other groups, in testing the biological and biochemical effects of FTIs.