Hetero-bivalent Imaging Agents for Simultaneous Targeting Prostate-Specific Membrane Antigen (PSMA) and Hepsin
Abstract
The hypothesis of the original proposal was to improve the sensitivity and accuracy of prostate cancer diagnosis by targeting simultaneously PSMA and hepsin, which are highly expressed in advanced and metastatic prostate cancer. In Year 2, we successfully established the solid-phase synthetic strategy of PSMA-hepsin peptide conjugates and synthesized key intermediates to conjugate with imaging probes including optical dyes and radionuclides. The synthesized dual-targeting conjugates consist of PSMA-binding ligand (Lys-urea-Glu) and hepsin-binding ligands derived from the IPLLVVPLGGSSK peptide and indole-5-caboximidamide. In silico docking studies of compound library with human hepsin identified potential hits which can be utilized as hepsin-binding scaffolds. The synthesized conjugates will be labeled with radionuclides/optical dyes and evaluated in vivo in Year 3.
Document Details
- Document Type
- Technical Report
- Publication Date
- Sep 01, 2012
- Accession Number
- ADA568064
Entities
People
- Youngjoo Byun
Organizations
- Korea University