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(Referência obtida automaticamente do Web of Science, por meio da informação sobre o financiamento pela FAPESP e o número do processo correspondente, incluída na publicação pelos autores.)

Deferasirox-TAT(47-57) peptide conjugate as a water soluble, bifunctional iron chelator with potential use in neuromedicine

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Autor(es):
Goswami, Dibakar [1, 2] ; Vitorino, Hector A. [1] ; Alta, Roxana Y. P. [1] ; Silvestre, Daniel M. [1] ; Nomura, Cassiana S. [1] ; Teresa Machini, M. [3] ; Esposito, Breno P. [1]
Número total de Autores: 7
Afiliação do(s) autor(es):
[1] Univ Sao Paulo, Dept Quim Fundamental, BR-05508000 Sao Paulo - Brazil
[2] Bhabha Atom Res Ctr, Div Bioorgan, Bombay 400085, Maharashtra - India
[3] Univ Sao Paulo, Inst Quim, Dept Bioquim, BR-05508000 Sao Paulo - Brazil
Número total de Afiliações: 3
Tipo de documento: Artigo Científico
Fonte: BIOMETALS; v. 28, n. 5, p. 869-877, OCT 2015.
Citações Web of Science: 4
Resumo

Deferasirox (DFX), an orally active and clinically approved iron chelator, is being used extensively for the treatment of iron overload. However, its water insolubility makes it cumbersome for practical use. In addition to this, the low efficacy of DFX to remove brain iron prompted us to synthesize and evaluate a DFX-TAT(47-57) peptide conjugate for its iron chelation properties and permeability across RBE4 cell line, an in vitro model of the blood-brain barrier. The water-soluble conjugate was able to remove labile iron from buffered solution as well as from iron overloaded sera, and the permeability of DFX-TAT(47-57) conjugate into RBE4 cells was not affected compared to parent deferasirox. The iron bound conjugate was also able to translocate through the cell membrane. (AU)

Processo FAPESP: 11/18958-0 - Conjugados quelante-peptídeo permeáveis à barreira hematoencefálica como protetores contra toxicidade induzida por ferro
Beneficiário:Dibakar Goswami
Modalidade de apoio: Bolsas no Brasil - Pós-Doutorado