Repozytorium publikacji - Politechnika Gdańska

A series of compounds containing either non-proteinogenic beta-/gamma-amino acids or N-substituted beta-alanine residues (beta-peptoid units) in P-1 specificity position were synthesized based on the structure of sunflower trypsin inhibitor 1 (SFTI-1). The compounds were synthesized on a solid support; the N-substituted beta-alanines (beta Nhlys and beta Nhphe) were introduced into a peptidomimetic chain via a two-step approach using acryloyl chloride and an appropriate primary amine. The inhibitory activities were characterized in vitro against bovine alpha-chymotrypsin or bovine beta-trypsin. Three analogues displayed activity comparable to fully proteinogenic counterparts-monocyclic SFTI-1 and [Phe(5)] SFTI-1. Moreover, all active peptidomimetics were resistant toward proteolytic degradation, even after 24-h incubation at room temperature. (C) 2012 Wiley Periodicals, Inc

Autorzy

• D. Debowski,
• R. Łukajtis,
• M. Filipowicz,
• P. Strzelecka,
• M. Wysocka,
• A. Łęgowska,
• A. Lesner,
• K. Rolka,
• Rafał Łukajtis link otwiera się w nowej karcie ,
• Adam Lesner link otwiera się w nowej karcie