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

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

doi:10.1515/hsz-2014-0190

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

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

Istituto di Ricerche Farmacologiche "Mario Negri"

Research output: Contribution to journal › Article › peer-review

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.

Original language	English
Pages (from-to)	45-52
Number of pages	8
Journal	Biological Chemistry
Volume	396
Issue number	1
DOIs	https://doi.org/10.1515/hsz-2014-0190
Publication status	Published - Jan 1 2015

Keywords

human kallikrein 5
human kallikrein 6
inhibitor
molecular modeling
serine protease

ASJC Scopus subject areas

Biochemistry
Clinical Biochemistry
Molecular Biology
Medicine(all)

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10.1515/hsz-2014-0190

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Severino, B., Fiorino, F., Corvino, A., Caliendo, G., Santagada, V., Assis, D. M., Oliveira, J. R., Juliano, L., Manganelli, S., Benfenati, E., Frecentese, F., Perissutti, E., & Juliano, M. A. (2015). Synthesis, biological evaluation, and docking studies of PAR2-AP-derived pseudopeptides as inhibitors of kallikrein 5 and 6. Biological Chemistry, 396(1), 45-52. https://doi.org/10.1515/hsz-2014-0190

Severino, B, Fiorino, F, Corvino, A, Caliendo, G, Santagada, V, Assis, DM, Oliveira, JR, Juliano, L, Manganelli, S, Benfenati, E, Frecentese, F, Perissutti, E & Juliano, MA 2015, 'Synthesis, biological evaluation, and docking studies of PAR2-AP-derived pseudopeptides as inhibitors of kallikrein 5 and 6', Biological Chemistry, vol. 396, no. 1, pp. 45-52. https://doi.org/10.1515/hsz-2014-0190

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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.",

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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

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

Abstract

Keywords

ASJC Scopus subject areas

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