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Synthesis of 3-Amino-l-CarboxymethyI-Benzodiazepine (BZA) Peptidomimetics

2025-03-27 生物化学 加入收藏
Replacement of key structural or binding elements of a peptide lead with nonpept

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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