Solid-Phase Synthesis of NMe-IB-01212, a Highly N-Methylated Cyclic Peptide
✍ Scribed by Marcucci, Eleonora; Tulla-Puche, Judit; Albericio, Fernando
- Book ID
- 111929561
- Publisher
- American Chemical Society
- Year
- 2011
- Tongue
- English
- Weight
- 379 KB
- Volume
- 14
- Category
- Article
- ISSN
- 1523-7060
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## Abstract Structural modification of the peptide backbone via __N__‐methylation is a powerful tool to modulate the pharmacokinetic profile and biological activity of peptides. Here we describe a rapid and highly efficient microwave(MW)‐assisted Fmoc/tBu solid‐phase method to prepare short chain _
We synthesized a 18 residues cyclic ppcicle correqonding to a loop involved in tk cumremimetic action of a snake toxic pmtein. This peptide. whii ccnn~les with Ihe native toxin for the binding lo the nicolinic ucetylcholii mzeptor, inclti the Bturn inducing Pro-AW moiety. Gibe peptide wax pqxued and