Synthesis, biological evaluation, and docking studies of PAR2-AP-derived pseudopeptides as inhibitors of kallikrein 5 and 6

Autor(es):Mostrar menos -

Severino, Beatrice ^[1] ; Fiorino, Ferdinando ^[1] ; Corvino, Angela ^[1] ; Caliendo, Giuseppe ^[1] ; Santagada, Vincenzo ^[1] ; Assis, Diego Magno ^[2] ; Oliveira, Juliana R. ^[2] ; Juliano, Luiz ^[2] ; Manganelli, Serena ^[3] ; Benfenati, Emilio ^[3] ; Frecentese, Francesco ^[1] ; Perissutti, Elisa ^[1] ; Juliano, Maria Aparecida ^[2]

Afiliação do(s) autor(es)

^[1] Univ Naples Federico II, Dipartimento Farm, I-80131 Naples - Italy

^[2] Univ Fed Sao Paulo, Escola Paulista Med, Dept Biofis, BR-04044020 Sao Paulo - Brazil

^[3] Ist Ric Farmacol Mario Negri, IRCCS, I-20156 Milan - Italy

• Tipo de documento: Artigo Científico
• Fonte: Biological Chemistry; v. 396, n. 1, p. 45-52, JAN 2015.
• Citações Web of Science: 3

Resumo

A series of protease activated receptor 2 activating peptide (PAR2-AP) derivatives (1-15) were designed and synthesized. The obtained compounds were tested on a panel of human kallikreins (hKLK1, hKLK2, hKLK5, hKLK6, and hKLK7) and were found completely inactive toward hKLK1, hKLK2, and hKLK7. Aiming to investigate the mode of interaction between the most interesting compounds and the selected hKLKs, docking studies were performed. The described compounds distinguish the different human tissue kallikreins with compounds 1 and 5 as the best hKLK5 and hKLK6 inhibitors, respectively. (AU)

• Processo FAPESP: 12/50191-4 - Síntese, estudo cinético e aplicações de substratos e inibidores de enzimas proteolíticas
• Beneficiário: Maria Aparecida Juliano
• Modalidade de apoio: Auxílio à Pesquisa - Temático