Design and synthesis of a novel BODIPY-labeled PSMA inhibitor |
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| Institution: | 1. Department of Chemistry, Stony Brook University, Stony Brook, NY, United States;2. Institute of Chemical Biology and Drug Discovery, Stony Brook University, Stony Brook, NY, United States |
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| 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. |
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| Keywords: | Prostate cancer PSMA BODIPY Optical imaging |
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