Pseudopeptide inhibitors of Ras farnesyl-protein transferase.

  title={Pseudopeptide inhibitors of Ras farnesyl-protein transferase.},
  author={Samuel Graham and S. Jane Desolms and Elizabeth A. Giuliani and Nancy E. Kohl and Scott D. Mosser and Allen I. Oliff and David L. Pompliano and Elaine Rands and Michael J. Breslin and A A Deana},
  journal={Journal of medicinal chemistry},
  volume={37 6},
Inhibitors of Ras farnesyl-protein transferase are described. These are reduced pseudopeptides related to the C-terminal tetrapeptide of the Ras protein that signals farnesylation. Deletion of the carbonyl groups between the first two residues of the tetrapeptides either preserves or improves activity, depending on the peptide sequence. The most potent in vitro enzyme inhibitor described (IC50 = 5 nM) is Cys [psi CH2NH]Ile[psi CH2NH]Phe-Met (3). To obtain compounds able to suppress Ras… CONTINUE READING

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