2. Academic Validation
  3. Design and synthesis of a novel BODIPY-labeled PSMA inhibitor

Design and synthesis of a novel BODIPY-labeled PSMA inhibitor

  • Bioorg Med Chem Lett. 2020 Feb 1;30(3):126894. doi: 10.1016/j.bmcl.2019.126894.
Sang-Hyun Son 1,  Hongmok Kwon 1,  Hye-Hyun Ahn 2,  Hwanhee Nam 3,  Kyul Kim 1,  SangJin Nam 1,  Doyoung Choi 1,  Hyunsoo Ha 1,  Il Minn 4,  Youngjoo Byun 5
Affiliations

Affiliations

  • 1 College of Pharmacy, Korea University, 2511 Sejong-ro, Sejong 30019, Republic of Korea.
  • 2 Russell H. Morgan Department of Radiology and Radiological Science, Johns Hopkins University, Baltimore, MD 21287, United States.
  • 3 Russell H. Morgan Department of Radiology and Radiological Science, Johns Hopkins University, Baltimore, MD 21287, United States; Institute for NanoBioTechnology, Johns Hopkins University, Baltimore, MD 21287, United States.
  • 4 Russell H. Morgan Department of Radiology and Radiological Science, Johns Hopkins University, Baltimore, MD 21287, United States; Institute for NanoBioTechnology, Johns Hopkins University, Baltimore, MD 21287, United States. Electronic address: iminn1@jhmi.edu.
  • 5 College of Pharmacy, Korea University, 2511 Sejong-ro, Sejong 30019, Republic of Korea; Biomedical Research Center, Korea University Guro Hospital, 148 Gurodong-ro, Guro-gu, Seoul 08308, Republic of Korea. Electronic address: yjbyun1@korea.ac.kr.
PMID: 31874825 DOI: 10.1016/j.bmcl.2019.126894
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.

Keywords

BODIPY; Optical imaging; PSMA; Prostate cancer.

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