Compounds for inhibition of protein methylation

C - Chemistry – Metallurgy – 07 – K

Patent

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Details

C07K 14/47 (2006.01) A61K 31/00 (2006.01) A61K 38/17 (2006.01) C07C 59/60 (2006.01) C07C 317/44 (2006.01) C07C 317/50 (2006.01) C07C 323/00 (2006.01) C07C 323/03 (2006.01) C07C 323/52 (2006.01) C07C 323/54 (2006.01) C07C 323/59 (2006.01) C07C 323/60 (2006.01) C07C 323/61 (2006.01) C07C 327/58 (2006.01) C07C 391/00 (2006.01) C07F 9/38 (2006.01) C07F 9/40 (2006.01) C07K 1/113 (2006.01)

Patent

CA 2107790

2107790 9218465 PCTABS00016 The invention features a compound of the formula W-Y-Q-Z or W-Y-Zwherein W is a farnesyl group, a geranylgeranyl group, a substituted farnesyl group or a substituted geranylgeranyl group; Y is (1); Q is (2), wherein n = 1, 2, 3, 4, 5, or 6; each of T1' ... Tn' and T1" ... Tn" is independently: Fl, Br, -NHCOCH3, -NH2, a peptide, an alkane group, an alkene group, a polyethyleneglycol group, a saturated fatty acid, an unsaturated fatty acid, a monosaccharide, or a disaccharide; and Z is -COOH or salts or esters thereof, -CONH2, -NO2, -PO3 or salts or esters thereof, -C N, or -SO3 or salts or esters thereof, provided that when W is farnesyl, Y is -S-, n = 2, and either T2' or T2" is -NHCOCH3, then Z is not -COOH. The compounds of the invention are capable of interfering with enzymatic methylation of a peptide having the carboxyl-terminal motif -CAAX wherein C = cysteine, A = aliphatic amino acid, and X = any amino acid.

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