N-Methylation of peptides is a strategy for enhancement of their peptidase resistance. Methylated residues are widely present in natural products such as dactinomycin and cyclosporine, which are used as chemotherapy agents. In recent years, numerous projects have included methylation of peptide backbone in the process of optimization of peptide therapeutics. The use of N-methyl amino acids in peptide synthesis has been recently optimized in several works enabling the routine use of Fmoc-/Boc-building blocks in parallel synthesis of cyclic peptides.
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