Inhibition of farnesyl transferases from malignant and non-malignant cultured human lymphocytes by prenyl substrate analogues.
Cytosolic prenyl transferases from two human lymphoid tissue-derived cell lines, IM-9 and Molt-4 cells, are shown to isoprenylate recombinant p21H-ras. Isoprenylation was inhibited by an N-acetylated pentapeptide (N-Ac-Lys-Cys-Val-Leu-Ser), c,t-farnesyl diphosphate, c,t,t-geranylgeranyl diphosphate, t,t,t-geranylgeranyl diphosphate and a photolabile farnesyl diphosphate analogue. c,t-Farnesyl and t,t,t-geranylgeranyl monophosphates were also effective inhibitors of the Molt-4 enzyme but not the IM-9 enzyme.
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Department of Biochemistry and Molecular Biology, J. Hillis Miller Health Center, University of Florida, Gainesville 32610.
Allen
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D019883:Alkyl and Aryl Transferases; D000595:Amino Acid Sequence; D006801:Humans; D007938:Leukemia / Q000201:enzymology*; D008969:Molecular Sequence Data; D011106:Polyisoprenyl Phosphates / Q000494:pharmacology*; D016283:Proto-Oncogene Proteins p21(ras) / Q000378:metabolism; D012717:Sesquiterpenes; D014166:Transferases / Q000037:antagonists & inhibitors*; D014407:Tumor Cells, Cultured
D011106:Polyisoprenyl Phosphates; D012717:Sesquiterpenes; C004808:farnesyl pyrophosphate; D014166:Transferases; D019883:Alkyl and Aryl Transferases; C064911:p21(ras) farnesyl-protein transferase; C501009:HRAS protein, human; D016283:Proto-Oncogene Proteins p21(ras); C002963:geranylgeranyl pyrophosphate