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Development of inhibitors for human tissue kallikreins 5 and 7 (KLK5 and KLK7)

Grant number: 11/51297-8
Support type:Regular Research Grants
Duration: February 01, 2012 - September 30, 2013
Field of knowledge:Biological Sciences - Biochemistry - Enzymology
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


Human kallikreins 5 (KLK5) and 7 (KLK7) are members of the human tissue kallikreins, comprising 15 kallikrein like serine peptidases (KLKs). KLK5 is found in many tissues, including breast, central nervous system, prostate, testis and trachea; and KLK7 was reported to be present at esophagus, kidney, liver and salivary gland. Moreover, both enzymes appear to be most abundantly expressed in human skin, where an important role in the skin desquamation process has been reported. In the extracellular space, KLK5 and KLK7 are believed to contribute to desquamation by hydrolyzing proteins composing intercellular adhesion structures called corneodesmosomes. Thus, the development of inhibitor for KLK5 and KLK7 can contribute not only to elucidate its physiological and pathological mechanisms but also as an archetype of new drugs whose hinder such complications caused by KLK5 and KLK7 uncontrolled activity. Thus, in this project, we will strive in the search for inhibitors for KLK5 and KLK7 using synthetic molecules and protein inhibitors. The molecules are peptidomimetic based compounds and bacterial serpins. (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)
OLIVEIRA, JOCELIA P. C.; FREITAS, RENATO F.; DE MELO, LEANDRO SILVA; BARROS, THALITA G.; SANTOS, JORGE A. N.; JULIANO, MARIA A.; PINHEIRO, SERGIO; BLABER, MICHAEL; JULIANO, LUIZ; MURI, ESTELA M. F.; PUZER, LUCIANO. Isomannide-Based Peptidomimetics as Inhibitors for Human Tissue Kallikreins 5 and 7. ACS Medicinal Chemistry Letters, v. 5, n. 2, p. 128-132, FEB 2014. Web of Science Citations: 20.
DE SOUZA, LUCAS R.; MELO, POLLYANA M.; PASCHOALIN, THAYSA; CARMONA, ADRIANA K.; KONDO, MARCIA; HIRATA, IZAURA Y.; BLABER, MICHAEL; TERSARIOL, IVARNE; TAKATSUKA, JOYCE; JULIANO, MARIA A.; JULIANO, LUIZ; GOMES, ROSELI A.; PUZER, LUCIANO. Human tissue kallikreins 3 and 5 can act as plasminogen activator releasing active plasmin. Biochemical and Biophysical Research Communications, v. 433, n. 3, p. 333-337, APR 12 2013. Web of Science Citations: 6.
FREITAS, RENATO F.; TEIXEIRA, THIAGO S. P.; BARROS, THALITA G.; SANTOS, JORGE A. N.; KONDO, MARCIA Y.; JULIANO, MARIA A.; JULIANO, LUIZ; BLABER, MICHAEL; ANTUNES, OCTAVIO A. C.; ABRAHAO, JR., ODONIRIO; PINHEIRO, SERGIO; MURI, ESTELA M. F.; PUZER, LUCIANO. Isomannide derivatives as new class of inhibitors for human kallikrein 7. Bioorganic & Medicinal Chemistry Letters, v. 22, n. 19, p. 6072-6075, OCT 1 2012. Web of Science Citations: 16.

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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