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dc.contributor.author Assis, Diego Magno
dc.contributor.author Zalazar, Lucia
dc.contributor.author Juliano, María Aparecida
dc.contributor.author de Castro, Rosana Esther
dc.contributor.author Cesari, Andreina
dc.date.available 2017-02-20T21:17:38Z
dc.date.issued 2013-04
dc.identifier.citation Assis, Diego Magno; Zalazar, Lucia; Juliano, María Aparecida; de Castro, Rosana Esther; Cesari, Andreina; Novel inhibitory activity for serine protease inhibitor Kazal type-3 (Spink3) on human recombinant kallikreins; Bentham Science Publishers; Protein And Peptide Letters; 20; 10; 4-2013; 1098-1107
dc.identifier.issn 0929-8665
dc.identifier.uri http://hdl.handle.net/11336/13203
dc.description.abstract Kallikrein-related peptidases (KLKs) are trypsin-like and chymotrypsin-like serine proteases which are expressed in several tissues. Their activity is tightly controlled by inhibitors including members of the serine protease Kazal-type (SPINK) family. These enzymes are promising targets for the treatment of skin desquamation, inflammation and cancer. Spink3 or caltrin I is expressed in mouse pancreas and males accessory glands and the resulting mature protein has been associated with different activities such as an inhibitor of trypsin and acrosin activity, calcium transport inhibitor in sperm and inhibitor of cell proliferation during embryogenesis. In this study, we produced a soluble recombinant Spink3 from mouse seminal vesicle (rmSpink3) that inhibited the activity of human KLKs. Using FRET substrates, rmSpink3 exhibited a potent inhibitory activity against human KLK2, KLK3, KLK5 (Ki ranging from 260 to 1500 nM), and to a lesser extent against KLK6, KLK1 and KLK7 (Ki around 3000 nM). As shown by mass spectrometry analysis of rmSpink3 incubated with trypsin, the inhibitor was not truncated by the target enzyme. Based on the in silico analysis of the expression of Spink3/SPINK1 and KLKs it is speculated that some KLKs may be natural targets of Spink3/SPINK1, however experimental confirmation using both proteins from mouse or human origin is needed. This work shows that rmSpink3 is a potent inhibitor of various human KLK members suggesting the potential of this molecule in the diagnosis/prevention of several human diseases.
dc.format application/pdf
dc.language.iso eng
dc.publisher Bentham Science Publishers
dc.rights info:eu-repo/semantics/restrictedAccess
dc.rights.uri https://creativecommons.org/licenses/by-nc-sa/2.5/ar/
dc.subject Spink3
dc.subject kallikreins
dc.subject pharmaceutical application
dc.subject protease inhibitor
dc.subject.classification Bioquímica y Biología Molecular
dc.subject.classification Ciencias Biológicas
dc.subject.classification CIENCIAS NATURALES Y EXACTAS
dc.title Novel inhibitory activity for serine protease inhibitor Kazal type-3 (Spink3) on human recombinant kallikreins
dc.type info:eu-repo/semantics/article
dc.type info:ar-repo/semantics/artículo
dc.type info:eu-repo/semantics/publishedVersion
dc.date.updated 2017-02-10T18:12:33Z
dc.identifier.eissn 1875-5303
dc.journal.volume 20
dc.journal.number 10
dc.journal.pagination 1098-1107
dc.journal.pais Estados Unidos
dc.description.fil Fil: Assis, Diego Magno. Universidade Federal de São Paulo; Brasil
dc.description.fil Fil: Zalazar, Lucia. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Mar del Plata. Instituto de Investigaciones Biológicas; Argentina
dc.description.fil Fil: Juliano, María Aparecida. Universidade Federal de São Paulo; Brasil
dc.description.fil Fil: de Castro, Rosana Esther. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Mar del Plata. Instituto de Investigaciones Biológicas; Argentina
dc.description.fil Fil: Cesari, Andreina. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Mar del Plata. Instituto de Investigaciones Biológicas; Argentina
dc.journal.title Protein And Peptide Letters
dc.relation.alternativeid info:eu-repo/semantics/altIdentifier/url/http://www.eurekaselect.com/114224/article
dc.relation.alternativeid info:eu-repo/semantics/altIdentifier/url/http://dx.doi.org/10.2174/0929866511320100003


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info:eu-repo/semantics/restrictedAccess Excepto donde se diga explícitamente, este item se publica bajo la siguiente descripción: Creative Commons Attribution-NonCommercial-ShareAlike 2.5 Unported (CC BY-NC-SA 2.5)