Synthesis, Characterization, and Evaluation of Near-IR Boron Dipyrromethene Bioconjugates for Labeling of Adenocarcinomas by Selectively Targeting the Epidermal Growth Factor Receptor.

ABSTRACT: A series of five boron dipyrromethene (BODIPY) bioconjugates containing an epidermal growth factor receptor (EGFR)-targeted pegylated LARLLT peptide and/or a glucose or biotin ethylene diamine group were synthesized, and the binding capability of the new conjugates to the extracellular domain of EGFR was investigated using molecular modeling, surface plasmon resonance, fluorescence microscopy, competitive binding assays, and animal studies. The BODIPY conjugates with a LARLLT peptide were found to bind specifically to EGFR, whereas those lacking the peptide bound weakly and nonspecifically. All BODIPY conjugates showed low cytotoxicity (IC₅₀ > 94 μM) in HT-29 cells, both in the dark and upon light activation (1.5 J/cm²). Studies of nude mice bearing subcutaneous human

SUBMITTER: Kaufman NEM 

PROVIDER: S-EPMC6693348 | biostudies-literature | 2019 Apr

REPOSITORIES: biostudies-literature