A number of proteins involved in cell growth control, including members of the Ras family of
GTPases, are modified at their C terminus by a three-step posttranslational process termed
prenylation. The enzyme isoprenylcysteine carboxylmethyl-transferase (Icmt) catalyzes the
last step in this process, and genetic and pharmacological suppression of Icmt activity
significantly impacts on cell growth and oncogenesis. Screening of a diverse chemical
library led to the identification of a specific small molecule inhibitor of Icmt, cysmethynil, that …