Design and synthesis of a novel BODIPY-labeled PSMA inhibitor.

Bioorg Med Chem Lett

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:

Published: February 2020

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 BODIPY. 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.

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Source
http://dx.doi.org/10.1016/j.bmcl.2019.126894DOI Listing

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