Benzodiazepine peptidomimetics: potent inhibitors of Ras farnesylation in animal cells.

@article{James1993BenzodiazepinePP,
  title={Benzodiazepine peptidomimetics: potent inhibitors of Ras farnesylation in animal cells.},
  author={Glyn James and Joseph L Goldstein and Michael Scott Brown and Thomas E. Rawson and Th. Somers and Robert S. McDowell and Craig W. Crowley and B K Lucas and Arthur D. Levinson and James C. Marsters},
  journal={Science},
  year={1993},
  volume={260 5116},
  pages={
          1937-42
        }
}
Oncogenic Ras proteins transform animal cells to a malignant phenotype only when modified by farnesyl residues attached to cysteines near their carboxyl termini. The farnesyltransferase that catalyzes this reaction recognizes tetrapeptides of the sequence CAAX, where C is cysteine, A is an aliphatic amino acid, and X is a carboxyl-terminal methionine or serine. Replacement of the two aliphatic residues with a benzodiazepine-based mimic of a peptide turn generated potent inhibitors of… CONTINUE READING
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