Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Peptide containing doai
Patent
1993-05-18
1997-02-11
Warden, Jill
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Peptide containing doai
562557, 562559, 562445, 530331, 530332, 530323, A61K 3806
Patent
active
056020988
ABSTRACT:
Peptidomimetics of the formula C-AMBA-X where C is cysteine, X is, for example, methionine or phenylalanine and AMBA is a hydrophobic spacer, notably 3-aminomethylbenzoic acid. These compounds are effective inhibitors of p21 ras farnesyltransferase. Other modifications including alternative spacers for AMBA, and replacement of the A.sub.1 A.sub.2 X component of known CA.sub.1 A.sub.2 X tetrapeptides by a non-peptide aryl or heterocyclic component are also disclosed as are various phosphonylated and arylated derivatives of peptides and peptidomimetics. Pro-drugs made by functionalizing terminal amino and carboxylic acid groups of peptides and peptidomimetics are also disclosed. Such functionalized derivatives demonstrate increased cell uptake. Other structural modifications are also referred to.
REFERENCES:
patent: 5043268 (1991-08-01), Stock
patent: 5141851 (1992-08-01), Brown et al.
patent: 5238922 (1993-08-01), Graham et al.
Hancock et al, "A polybasic Domain or Palmitoylation is Required in Addition to the CAAX Motif to Localize p21.sup.ras to the Plasma Membrane", Cell, vol. 63, Oct. 5, 1990, pp. 133-139.
Reiss et al, "Inhibition of Purified p21.sup.ras Farnesyl:Protein Transferase by Cys-AAX Tetrapeptides", Cell, vol. 62, Jul. 13, 1990, pp. 81-88.
Willumsen et al, "The p21 ras C-terminus is required for transformation and membrane association," Nature, vol. 310, Aug. 16, 1984, pp. 583-586.
Hamilton Andrew
Sebti Said
Seong Churl M.
Lukton David
University of Pittsburgh
Warden Jill
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