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Development of Inhibitors for Human Tissue Kallikreins

Grant number: 16/21441-3
Support type:Regular Research Grants
Duration: December 01, 2017 - November 30, 2019
Field of knowledge:Biological Sciences - Biochemistry - Chemistry of Macromolecules
Principal Investigator:Luciano Puzer
Grantee:Luciano Puzer
Home Institution: Centro de Ciências Naturais e Humanas (CCNH). Universidade Federal do ABC (UFABC). Ministério da Educação (Brasil). Santo André , SP, Brazil

Abstract

Protease inhibitors can directly or indirectly affect the active proteolytic enzyme, limiting or eliminating their ability to catalyze the cleavage of peptide bonds. These molecules may also act selectively or specifically, endogenously controlling various physiological processes. In recent years our group has been working on developing inhibitors for proteases, particularly against human tissue kallikreins (KLKs), which comprise a family of 15 serine proteases distributed in various tissues of the human body. They appear involved in several pathological events and therefore it is believed that specific inhibitors to these enzymes may represent new therapeutic procedures for certain pathologies. The KLKs also appear differentially expressed in cancer, and for this reason they are pointed as potential biomarkers for this kind of pathology. The most representative case is the human tissue kallikrein 3 (KLK3), which is also called PSA. Thus in this project we are proposing new strategies for the development of inhibitors for the KLKs, but that may also be used for any other proteolytic enzyme. Here we will work with three different strategies based in synthetic inhibitors, protein inhibitors, and the recombinant antibodies. (AU)

Scientific publications
(References retrieved automatically from Web of Science and SciELO through information on FAPESP grants and their corresponding numbers as mentioned in the publications by the authors)
LAUREANO, ANA FLAVIA S.; ZANI, MARCELO B.; SANT'ANA, AQUILES M.; TOGNATO, RAFAEL C.; LOMBELLO, CHRISTIANE B.; DO NASCIMENTO, MONICA HELENA M.; HELMSING, SASKIA; FUEHNER, VIOLA; HUST, MICHAEL; PUZER, LUCIANO. Generation of recombinant antibodies against human tissue kallikrein 7 to treat skin diseases. Bioorganic & Medicinal Chemistry Letters, v. 30, n. 23 DEC 1 2020. Web of Science Citations: 0.
DE SOUZA, ACACIO S.; PACHECO, BARBARA D. C.; PINHEIRO, SERGIO; MURI, ESTELA M. F.; DIAS, LUIZA R. S.; LIMA, CAMILO H. S.; GARRETT, RAFAEL; DE MORAES, MARIANA B. M.; DE SOUZA, BRUNO E. G.; PUZER, LUCIANO. 3-Acyltetramic acids as a novel class of inhibitors for human kallikreins 5 and 7. Bioorganic & Medicinal Chemistry Letters, v. 29, n. 9, p. 1094-1098, MAY 1 2019. Web of Science Citations: 0.

Please report errors in scientific publications list by writing to: cdi@fapesp.br.