title: Synthesis and in vitro evaluation of a PDT active BODIPY-NLS conjugate.
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).
authors: Division of Molecular Design and Synthesis, Department of Chemistry, University of Leuven, Celestijnenlaan 200F, P.O. Box 2404, 3001 Heverlee, Belgium.
authors: Peter
authors: P
authors: Verwilst
authors: Charlotte C
authors: CC
authors: David
authors: Volker
authors: V
authors: Leen
authors: Johan
authors: J
authors: Hofkens
authors: Peter A M
authors: PA
authors: de Witte
authors: Wim M
authors: WM
authors: De Borggraeve
mesh_terms: D001896:Boron Compounds / Q000737:chemistry*; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D004353:Drug Evaluation, Preclinical; D006801:Humans; D008856:Microscopy, Fluorescence; D019913:Nuclear Localization Signals / Q000737:chemistry*; D010778:Photochemotherapy; D017319:Photosensitizing Agents / Q000138:chemical synthesis* / Q000627:therapeutic use / Q000633:toxicity; D001749:Urinary Bladder Neoplasms / Q000188:drug therapy
chemical_list: C095489:4,4-difluoro-4-bora-3a,4a-diaza-s-indacene; D001896:Boron Compounds; D019913:Nuclear Localization Signals; D017319:Photosensitizing Agents