TY - JOUR
T1 - Synthesis, biological evaluation, and docking studies of PAR2-AP-derived pseudopeptides as inhibitors of kallikrein 5 and 6
AU - Severino, Beatrice
AU - Fiorino, Ferdinando
AU - Corvino, Angela
AU - Caliendo, Giuseppe
AU - Santagada, Vincenzo
AU - Assis, Diego Magno
AU - Oliveira, Juliana R.
AU - Juliano, Luiz
AU - Manganelli, Serena
AU - Benfenati, Emilio
AU - Frecentese, Francesco
AU - Perissutti, Elisa
AU - Juliano, Maria Aparecida
PY - 2015/1/1
Y1 - 2015/1/1
N2 - 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.
AB - 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.
KW - human kallikrein 5
KW - human kallikrein 6
KW - inhibitor
KW - molecular modeling
KW - serine protease
UR - http://www.scopus.com/inward/record.url?scp=84914689095&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=84914689095&partnerID=8YFLogxK
U2 - 10.1515/hsz-2014-0190
DO - 10.1515/hsz-2014-0190
M3 - Article
C2 - 25153237
AN - SCOPUS:84914689095
VL - 396
SP - 45
EP - 52
JO - Biological Chemistry
JF - Biological Chemistry
SN - 1431-6730
IS - 1
ER -