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Synthesis and in vitro evaluation of a PDT active BODIPY-NLS conjugate.
Verwilst, Peter; David, Charlotte C; Leen, Volker; Hofkens, Johan; de Witte, Peter A M; De Borggraeve, Wim M.
Afiliação
  • Verwilst P; Division of Molecular Design and Synthesis, Department of Chemistry, University of Leuven, Celestijnenlaan 200F, P.O. Box 2404, 3001 Heverlee, Belgium.
Bioorg Med Chem Lett ; 23(11): 3204-7, 2013 Jun 01.
Article em En | MEDLINE | ID: mdl-23639541
ABSTRACT
Two new photosensitizers based on the BODIPY scaffold have been synthesized, of which one bears an NLS peptide, which is linked to the BODIPY's core using the copper catalysed azide-alkyne click reaction. The phototoxicities of these BODIPY based photosensitizers have been determined, as well as their dark toxicities. Although the conjugation of a single NLS peptide to the BODIPY did not lead to any observable nuclear localization, the photosensitizer did exhibit a superior photoxicity. Cellular co-localization experiments revealed a localization of both dyes in the lysosomes, as well as a partial localization within the ER (for the peptide-bearing BODIPY).
Assuntos

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Compostos de Boro / Fármacos Fotossensibilizantes / Sinais de Localização Nuclear Limite: Humans Idioma: En Revista: Bioorg Med Chem Lett Assunto da revista: BIOQUIMICA / QUIMICA Ano de publicação: 2013 Tipo de documento: Article País de afiliação: Bélgica

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Compostos de Boro / Fármacos Fotossensibilizantes / Sinais de Localização Nuclear Limite: Humans Idioma: En Revista: Bioorg Med Chem Lett Assunto da revista: BIOQUIMICA / QUIMICA Ano de publicação: 2013 Tipo de documento: Article País de afiliação: Bélgica