Design and synthesis of a novel BODIPY-labeled PSMA inhibitor

Sang Hyun Son, Hongmok Kwon, Hye Hyun Ahn, Hwanhee Nam, Kyul Kim, Sang Jin Nam, Doyoung Choi, Hyunsoo Ha, Il Minn, Youngjoo Byun

Research output: Contribution to journalArticlepeer-review

Abstract

Prostate-specific membrane antigen (PSMA) is a zinc-bound metalloprotease which is highly expressed in metastatic prostate cancer. It has been considered an excellent target protein for prostate cancer imaging and targeted therapy because it is a membrane protein and its active site is located in the extracellular region. We successfully synthesized and evaluated a novel PSMA ligand conjugated with BODIPY650/665. Compound 1 showed strong PSMA-inhibitory activity and selective uptake into PSMA-expressing tumors. Compound 1 has the potential to be utilized as a near infrared (NIR) optical imaging probe targeting PSMA-expressing cancers.

Original languageEnglish (US)
Article number126894
JournalBioorganic and Medicinal Chemistry Letters
Volume30
Issue number3
DOIs
StatePublished - Feb 1 2020

Keywords

  • BODIPY
  • Optical imaging
  • PSMA
  • Prostate cancer

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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