Patent ID: 6576436
Filing Date: 2003-06-10
Classification: A61K,A61P,C12N,C12Q,C12Y,G01N

Abstract:
A method of inactivating a prenylation enzyme, comprising the step of: contacting a prenylation enzyme, in the presence of at least one of its natural substrates, with an &agr;-dicarbonyl compound having a formula:Aâ€”Lâ€”Dâ€”R (Formula III) wherein A is an anionic group selected from the group consisting of carboxylate, sulfate, sulfonate, sulfinate, phosphate, phosphonate, thiophosphate, pyrophosphate, enolate, sulfonamide, sulfone, and tetrazole, or a group that forms an anionic group selected from the group consisting of carboxylate, sulfate, sulfonate, sulfinate, phosphate, phosphonate, thiophosphate, pyrophosphate, enolate, sulfonamide, sulfone, and tetrazole at physiological pH;wherein L is selected from the group consisting of alkyl, alkenyl, alkynyl, and aryl; wherein R is selected from the group consisting of hydrogen, alkyl, alkenyl, alkynyl, and aryl; and wherein D is a dicarbonyl functional group or a masked form of said group, whereby the activity of the prenylation enzyme is reduced by at least 50%.