Heterobivalent Imaging Agents for Simultaneous Targeting Prostate-Specific Membrane Antigen (PSMA) and Hepsin

Abstract

The purpose of this work is to prepare and evaluate heterobivalent conjugates of PSMA/hepsin-binding ligands labeled with optical dyes or radionuclides. The sensitivity and accuracy of prostate cancer diagnosis can be improved by dual-targeting of PSMA and hepsin which are highly overexpressed in advanced and metastatic prostate cancer. In this final year, we prepared several heterobivalent PSMA-hepsin conjugates labeled with optical dyes such as Cy7 and SulfoCy7. One of them, designated as KB304, exhibited selective uptake in the PSMA/hepsin-expressing cell lines compared to control cells. In vivo optical imaging study confirmed the accumulation of KB304 in PSMA-HPN-dual-expressing tumors as compared to PC3/ML tumors which express low level of PSMA and hepsin. From these results, we can conclude that KB304 can be utilized as a potential lead compound for optimizing PSMA-hepsin heterobivalent conjugates.

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Document Details

Document Type
Technical Report
Publication Date
Nov 01, 2014
Accession Number
ADA613790

Entities

People

  • Youngjoo Byun

Organizations

  • Korea University

Tags

DTIC Thesaurus Topics

  • Amines
  • Amino Acids
  • Cell Line
  • Cells
  • Detection
  • Detectors
  • Formic Acid
  • Glutamic Acid
  • Hydrophilic Properties
  • Imaging Techniques
  • Mass Spectrometry
  • Nanoparticles
  • Neoplasms
  • Prostate
  • Prostate Cancer
  • Spectra
  • Targeting

Readers

  • Data Mining and Knowledge Discovery.
  • Oncology (Cancer Research).