Abstract
Replacement of key structural or binding elements of a peptide lead with nonpeptide components can improve affinity and metabolic stability (1–5). Such a strategy was successfully applied to the generation of potent, cell-permeable inhibitors of Ras famesyltransferase (FTase) (6,7). The central pair of amino acids in the CAAX tetrapeptide was replaced with the nonpeptide scaffold 3-methylamino-1-carboxymethyl-2,3-dihydro-5-phenyl-1H-1,4-benzodiazepin-2-one, (N-Me)BZA, shown below.
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© 1999 Humana Press Inc., Totowa, NJ
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Marsters, J.C., Rawson, T.E. (1999). Synthesis of 3-Amino-l-CarboxymethyI-Benzodiazepine (BZA) Peptidomimetics. In: Kazmierski, W.M. (eds) Peptidomimetics Protocols. Methods in Molecular Medicine™, vol 23. Humana Press. https://doi.org/10.1385/0-89603-517-4:385
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DOI: https://doi.org/10.1385/0-89603-517-4:385
Publisher Name: Humana Press
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