Biophysical and pharmacological characterization of a full-length synthetic analog of the antitumor polypeptide crotamine

Página do item simplificado
dc.contributor.authorPorta, Lucas de Carvalho [UNIFESP]
dc.contributor.authorFadel, Valmir
dc.contributor.authorCampeiro, Joana D'Arc [UNIFESP]
dc.contributor.authorGodinho, Rosely Oliveira [UNIFESP]
dc.contributor.authorHayashi, Mirian Akemi Furuie [UNIFESP]
dc.contributor.authorOliveira, Eduardo Brandt
dc.contributor.authorLatteshttp://lattes.cnpq.br/5559309395232147pt_BR
dc.coverageBerlin
dc.date.accessioned2021-10-29T14:49:48Z
dc.date.available2021-10-29T14:49:48Z
dc.date.issued2020-09-07
dc.description.abstractCrotamine is a polypeptide isolated from the venom of a South American rattlesnake. Among the properties and biological activities of crotamine, the most extraordinary is its ability to enter cells with unique selective affinity and cytotoxic activity against actively proliferating cells, such as tumor cells. This peptide is also a cargo carrier, and anticipating commercial application of this native polypeptide as a potential theranostic compound against cancer, we performed here a side-by-side characterization of a chemically synthesized full-length crotamine compared with its native counterpart. The structural, biophysical, and pharmacological properties were evaluated. Comparative NMR studies showed structural conservation of synthetic crotamine. Moreover, similarly to native crotamine, the synthetic polypeptide was also capable of inhibiting tumor growth in vivo, increasing the survival of mice bearing subcutaneous tumor. We also confirmed the ability of synthetic crotamine to transfect and transport DNA into eukaryotic cells, in addition to the importance of proteoglycans on cell surface for its internalization. This work opens new opportunities for future evaluation of chimeric and/or point-mutated analogs of this snake polypeptide, aiming for improving crotamine properties and applications, as well as possibly diminishing its potential toxic effects.pt_BR
dc.format.extentp. 1561-1571
dc.identifierhttps://doi.org/10.1007/s00109-020-01975-y
dc.identifier.citationJournal of Molecular Medicine, Berlin, v. 98, n. 11, p. 1561-1571, Nov. 2020.
dc.identifier.issn1432-1440
dc.identifier.urihttps://hdl.handle.net/11600/62157
dc.languageengpt_BR
dc.publisherSpringerpt_BR
dc.relation.ispartofJournal of Molecular Medicinept_BR
dc.rightsinfo:eu-repo/semantics/restrictedAccesspt_BR
dc.subjectCrotaminept_BR
dc.subjectCPPpt_BR
dc.subjectProteoglycanspt_BR
dc.subjectStructural NMRpt_BR
dc.subjectMelanoma tumorpt_BR
dc.subjectHind limb paralysispt_BR
dc.subjectSkeletal muscle contractionpt_BR
dc.titleBiophysical and pharmacological characterization of a full-length synthetic analog of the antitumor polypeptide crotaminept_BR
dc.typeinfo:eu-repo/semantics/articlept_BR
unifesp.campusEscola Paulista de Medicina (EPM)pt_BR
unifesp.departamentoFarmacologiapt_BR
unifesp.graduateProgramFarmacologiapt_BR
unifesp.knowledgeAreaOutrapt_BR
Arquivos
Pacote Original
Agora exibindo 1 - 1 de 1
Imagem de Miniatura
Nome:
CarvalhoPorta2020_Article_BiophysicalAndPharmacologicalC.pdf
Tamanho:
2.26 MB
Formato:
Adobe Portable Document Format
Descrição:
Baixar
Licença do Pacote
Agora exibindo 1 - 1 de 1
Imagem de Miniatura
Nome:
license.txt
Tamanho:
5.72 KB
Formato:
Item-specific license agreed upon to submission
Descrição:
Baixar
Coleções
EPM - Artigos