Hetero-bivalent Imaging Agents for Simultaneous Targeting Prostate-Specific Membrane Antigen (PSMA) and Hepsin
Annual rept. 1 Sep 2011-31 Aug 2012
KOREA UNIV YEONGI-GUN (KOREA) RESEARCH AND BUSINESS FOUNDATION
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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 radionuclidesoptical dyes and evaluated in vivo in Year 3.
- Anatomy and Physiology
- Medicine and Medical Research