6533b861fe1ef96bd12c44f1

RESEARCH PRODUCT

Synthesis of Hybrid Tripeptide Peptidomimetics Containing Dehydroamino Acid and Aminophosphonic Acid in the Chain and Evaluation of Their Activity toward Cathepsin C

Michał Paweł JewgińskiMaciej MakowskiMałgorzata PawełczakWaldemar GoldemanAlicja Trojanowska‐laskowskaPaweł KafarskiRafał Latajka

subject

phosphonopeptidesmolecular modelingMolecular ConformationBioengineeringGeneral ChemistryGeneral MedicineBiochemistryCathepsin Cdehydropeptidesstructure-activity relationinhibitorsMolecular MedicinePeptidomimeticsDPPIPeptidesMolecular Biology

description

Synthesis of a new group of hybrid phosphonodehydropeptides composed of glycyl-(Z)-dehydrophenylalanine and structurally variable aminophosphonates alongside with investigations of their activity towards cathepsin C are presented. Obtained results suggest that the introduction of (Z)- dehydrophenylalanine residue into the short phosphonopeptide chain does induce the ordered conformation. Investigated peptides appeared to act as weak or moderate inhibitors of cathepsin C.

https://doi.org/10.1002/cbdv.202101019