title: Synthesis, biological evaluation, and docking studies of PAR2-AP-derived pseudopeptides as inhibitors of kallikrein 5 and 6.
abstract: 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.
authors.forename: Beatrice
authors.initials: B
authors.lastname: Severino
authors.forename: Ferdinando
authors.initials: F
authors.lastname: Fiorino
authors.forename: Angela
authors.initials: A
authors.lastname: Corvino
authors.forename: Giuseppe
authors.initials: G
authors.lastname: Caliendo
authors.forename: Vincenzo
authors.initials: V
authors.lastname: Santagada
authors.forename: Diego Magno
authors.initials: DM
authors.lastname: Assis
authors.forename: Juliana R
authors.initials: JR
authors.lastname: Oliveira
authors.forename: Luiz
authors.initials: L
authors.lastname: Juliano
authors.forename: Serena
authors.initials: S
authors.lastname: Manganelli
authors.forename: Emilio
authors.initials: E
authors.lastname: Benfenati
authors.forename: Francesco
authors.initials: F
authors.lastname: Frecentese
authors.forename: Elisa
authors.initials: E
authors.lastname: Perissutti
authors.forename: Maria Aparecida
authors.initials: MA
authors.lastname: Juliano
mesh_terms: D006801:Humans; D007610:Kallikreins / Q000037:antagonists & inhibitors*; D008958:Models, Molecular; D044464:Receptor, PAR-2 / Q000096:biosynthesis* / Q000235:genetics
chemical_list: D044464:Receptor, PAR-2; D007610:Kallikreins