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

Research output: Contribution to journalArticle

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 languageEnglish
Pages (from-to)45-52
Number of pages8
JournalBiological Chemistry
Volume396
Issue number1
DOIs
Publication statusPublished - 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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  • Cite this

    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