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Development of mutant serpins for inhibition of human tissue kallikreins

Abstract

The human tissue kallikreins (KLKs) are a group of 15 serine proteases distributed over a wide range of tissues. 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. This protease is routinely used in the detection and monitoring of prostate cancer. Thus, in this project, our goal is to obtain specific serpins for KLKs, mainly PSA. This can represent a new indirect method for the detection of these enzymes in cancer tissue. The serpins are irreversible proteic inhibitors for serine proteases, and hence only interact with the active enzyme. Thus, it is possible to develop a more efficient method for detection of kallikreins (PSA mainly), since the traditional method, which uses ELISA, can not differentiate between the active PSA and the PSA with no proteolytic activity. (AU)

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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)
BARROS, THALITA G.; SANTOS, JORGE A. N.; DE SOUZA, BRUNO E. G.; SODERO, ANA CAROLINA R.; DE SOUZA, ALESSANDRA M. T.; DA SILVA, DAYANE P.; RODRIGUES, CARLOS RANGEL; PINHEIRO, SERGIO; DIAS, LUIZA R. S.; ABRAHIM-VIEIRA, BARBARA; et al. Discovery of a new isomannide-based peptidomimetic synthetized by Ugi multicomponent reaction as human tissue kallikrein 1 inhibitor. Bioorganic & Medicinal Chemistry Letters, v. 27, n. 2, p. 314-318, . (13/10548-3)
SANTOS, JORGE A. N.; KONDO, MARCIA Y.; FREITAS, RENATO F.; DOS SANTOS, MARCELO H.; RAMALHO, TEODORICO C.; ASSIS, DIEGO M.; JULIANO, LUIZ; JULIANO, MARIA A.; PUZER, LUCIANO. The natural flavone fukugetin as a mixed-type inhibitor for human tissue kallikreins. Bioorganic & Medicinal Chemistry Letters, v. 26, n. 5, p. 1485-1489, . (13/10548-3)

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Filed patent(s) as a result of this research project

COMPOSTOS INIBIDORES SELETIVOS DA CALICREÍNA TECIDUAL HUMANA 1 (KLK1), COMPOSIÇÃO, PROCESSO E USOS BR1020140272720 - Instituto Federal de Educação, Ciência e Tecnologia do Sul de Minas Gerais (IFSULDEMINAS) ; Universidade Federal do ABC (UFABC) ; Universidade federal Fluminense (UFF) . Estela Maris Freitas Muri ; Thalita Gonçalves Barros ; Luciano Puzer ; Jorge Alexandre Nogueira Santos ; Sérgio Pinheiro - October 2014, 31