期刊
PEPTIDE SCIENCE
卷 112, 期 4, 页码 -出版社
WILEY
DOI: 10.1002/pep2.24159
关键词
H1-relaxin B chain; microwave-assisted click reaction; on-resin CuAAC; stapled peptides
资金
- Fondazione Ricerca Relaxina Firenze [05/2017]
- Ente Cassa di Risparmio di Firenze [2018/0306]
The development of conformationally constrained analogues of bioactive peptides is a relevant goal in peptide medicinal chemistry. Among the several classes of conformationally constrained peptides, the so-called stapled peptides, which bear a side-chain-to-side-chain bridge, are particularly interesting since they offer the possibility to stabilize specific conformational elements, such as a-helices or beta-turns. We describe an efficient and reproducible microwave-assisted strategy to prepare side-chain-to-side-chain clicked peptides, performing the copper-catalyzed azide-alkyne cycloaddition on solid phase, using as a model peptide a portion of the H1-relaxin B chain, which contains the binding cassette motif of this important bioactive peptide. All the relevant parameters, that is, resin, solvent, catalytic system, microwave energy and reaction time were optimized using a systematic one-factor-at-a-time (OFAT) approach. This method will be useful for the preparation of libraries of conformationally constrained relaxin analogues.
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