Water-Soluble closo-Docecaborate-Containing Pteroyl Derivatives Targeting Folate Receptor-Positive Tumors for Boron Neutron Capture Therapy.
Cells
; 9(7)2020 07 03.
Article
em En
| MEDLINE
| ID: mdl-32635272
ABSTRACT
Water-soluble pteroyl-closo-dodecaborate conjugates (PBCs 1-4), were developed as folate receptor (FRα) targeting boron carriers for boron neutron capture therapy (BNCT). PBCs 1-4 had adequately low cytotoxicity with IC50 values in the range of 1~3 mM toward selected human cancer cells, low enough to use as BNCT boron agents. PBCs 1-3 showed significant cell uptake by FRα positive cells, especially U87MG glioblastoma cells, although the accumulation of PBC 4 was low compared with PBCs 1-3 and L-4-boronophenylalanine (L-BPA). The cellular uptake of PBC 1 and PBC 3 by HeLa cells was arrested by increasing the concentration of folate in the medium, indicating that the major uptake mechanisms of PBC 1-3 are primarily through FRα receptor-mediated endocytosis.
Palavras-chave
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Compostos de Boro
/
Terapia por Captura de Nêutron de Boro
/
Receptores de Folato com Âncoras de GPI
/
Nanoconjugados
/
Ácido Fólico
/
Neoplasias
Idioma:
En
Ano de publicação:
2020
Tipo de documento:
Article