Synthesis of dehydrodipeptide esters and their evaluation as inhibitors of cathepsin C

The procedures for the synthesis of esters of dehydropeptides containing C-terminal (Z)-dehydrophenylalanine and dehydroalanine have been elaborated. These esters appeared to be moderate or weak inhibitors of cathepsin C, with some of them exhibiting slow-binding behavior. As shown by molecular mode...

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Detalles Bibliográficos
Autores principales: Makowski, Maciej, Lenartowicz, Paweł, Oszywa, Bartosz, Jewgiński, Michał, Pawełczak, Małgorzata, Kafarski, Paweł
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Springer US 2015
Materias:
Original Research
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4500854/
https://www.ncbi.nlm.nih.gov/pubmed/26190908
http://dx.doi.org/10.1007/s00044-015-1366-0
Descripción
Sumario:The procedures for the synthesis of esters of dehydropeptides containing C-terminal (Z)-dehydrophenylalanine and dehydroalanine have been elaborated. These esters appeared to be moderate or weak inhibitors of cathepsin C, with some of them exhibiting slow-binding behavior. As shown by molecular modeling, they are rather bound at the surface of the enzyme and are not submersed in its binding cavities. ELECTRONIC SUPPLEMENTARY MATERIAL: The online version of this article (doi:10.1007/s00044-015-1366-0) contains supplementary material, which is available to authorized users.

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