A series of PAR2-AP derivatives (1-15) was designed and synthesized. The obtained compounds were tested on a panel of human kallikreins (hKLK1, hKLK2, hKLK5, hKLK6 and hKLK7) resulting completely inactive towards hKLK1, hKLK2 and hKLK7. Aiming to investigate the mode of interaction between the most interesting compounds and the selected hKLKs, docking studies have been performed. The described compounds distinguish the different human tissue kallikreins with compounds 1 and 5 as the best hKLK5 and hKLK6 inhibitors, respectively.
Synthesis, Biological Evaluation and Docking Studies of PAR2-AP Derived Pseudopeptides as Inhibitors of Kallikrein 5 and 6 / Severino, Beatrice; Fiorino, Ferdinando; Corvino, Angela; Caliendo, Giuseppe; Santagada, Vincenzo; Diego Magno, Assis; Juliana R., Oliveira; Luiz, Juliano; Serena, Manganelli; Emilio, Benfenati; Frecentese, Francesco; Perissutti, Elisa; Maria Aparecida, Juliano. - In: BIOLOGICAL CHEMISTRY. - ISSN 1431-6730. - 396:1(2015), pp. 45-52. [10.1515/hsz-2014-0190]
Synthesis, Biological Evaluation and Docking Studies of PAR2-AP Derived Pseudopeptides as Inhibitors of Kallikrein 5 and 6
SEVERINO, BEATRICE;FIORINO, FERDINANDO;CORVINO, ANGELA;CALIENDO, GIUSEPPE;SANTAGADA, VINCENZO;FRECENTESE, FRANCESCO;PERISSUTTI, ELISA;
2015
Abstract
A series of PAR2-AP derivatives (1-15) was designed and synthesized. The obtained compounds were tested on a panel of human kallikreins (hKLK1, hKLK2, hKLK5, hKLK6 and hKLK7) resulting completely inactive towards hKLK1, hKLK2 and hKLK7. Aiming to investigate the mode of interaction between the most interesting compounds and the selected hKLKs, docking studies have been performed. The described compounds distinguish the different human tissue kallikreins with compounds 1 and 5 as the best hKLK5 and hKLK6 inhibitors, respectively.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
