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. 2020 Feb 1;30(3):126894.
doi: 10.1016/j.bmcl.2019.126894. Epub 2019 Dec 18.

Design and synthesis of a novel BODIPY-labeled PSMA inhibitor

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

Design and synthesis of a novel BODIPY-labeled PSMA inhibitor

Sang-Hyun Son et al. Bioorg Med Chem Lett. .

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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