4-4-difluoro-4-bora-3a-4a-diaza-s-indacene and arginyl-glycyl-aspartic-acid

Labeling agents with radioisotopes or fluorescent dyes are useful for investigating the biodistributions of biologically active proteins and peptides. Compared with molecular imaging with a single modality, dual imaging probes provide complementary information for each modality. The development of a dual radioisotope/fluorescence agent for protein labeling would thus be valuable for both preclinical and clinical applications. In this study, we designed and synthesized a radioiodinated BODIPY derivative (BODIPY-ML) with a maleimide group as a thiol-labeling agent. In the presence of N-chlorosuccinimide and 1% acetic acid, [

Topics: Boron Compounds; Chemistry Techniques, Synthetic; Halogenation; Iodine Radioisotopes; Isotope Labeling; Oligopeptides; Radiochemistry; Sulfhydryl Compounds

In molecular imaging research, the development of multimodal imaging probes has recently attracted much attention. In the present study, we prepared radioiodinated BODIPY and applied it as a nuclear and optical dual functional labeling agent for proteins and peptides. We designed and synthesized [

Topics: Animals; Boron Compounds; Cell Line, Tumor; Humans; Iodine Radioisotopes; Male; Mice; Neoplasms, Experimental; Oligopeptides; Radiopharmaceuticals; Succinimides; Tomography, Emission-Computed, Single-Photon; Trastuzumab

We report the direct conversion of fluorescent probes to PET/fluorescent probes after efficient [(19)F]/[(18)F] exchange at the BODIPY motif. The radiolabeling of a NIR BODIPY dye was also established, which was conjugated with the RGD peptide for PET/fluorescence imaging of integrin expression in vivo.

Topics: Animals; Boron Compounds; Fluorescent Dyes; Mice; Oligopeptides; Positron-Emission Tomography

Near-infrared emissive BODIPY polymeric dye bearing cancer-homing cyclic arginine-glycine-aspartic acid (RGD) peptide residues (polymer B) was prepared by post-polymerization functionalization of BODIPY polymeric dye bearing bromo groups through tetra(ethylene glycol) tethered spacers (polymer A) with thiol-functionalized RGD cancer-homing peptide through thioether bonds under a mild basic condition. Polymer B possesses excellent water solubility, good photostability, biocompatibility and resistance to nonspecific interactions to normal endothelial cells, and can efficiently detect breast tumor cells through specific cooperative binding of cancer-homing RGD peptides to αvβ3 integrins of cancer cells while its parent polymer A without RGD residues fails to target cancer cells.

Topics: Boron Compounds; Breast; Breast Neoplasms; Cell Line, Tumor; Female; Fluorescent Dyes; Humans; Integrin alphaVbeta3; Oligopeptides; Optical Imaging; Polymers; Solubility; Water