Design and synthesis of a novel BODIPY-labeled PSMA inhibitor

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

doi:10.1016/j.bmcl.2019.126894

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Design and synthesis of a novel BODIPY-labeled PSMA inhibitor

Son, Sang-Hyun;
Kwon, Hongmok;
Ahn, Hye-Hyun;
Nam, Hwanhee;
Kim, Kyul;
... Byun, Youngjoo;
외 4명

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초록

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.

키워드

Prostate cancer; PSMA; BODIPY; Optical imaging; MEMBRANE ANTIGEN; FLUORESCENT-PROBE; PROSTATE-CANCER; PRECLINICAL EVALUATION; BIOLOGICAL EVALUATION; DERIVATIVES; DYES; GLUTATHIONE; EXPRESSION; AGENTS

제목: Design and synthesis of a novel BODIPY-labeled PSMA inhibitor

저자: Son, Sang-Hyun; Kwon, Hongmok; Ahn, Hye-Hyun; Nam, Hwanhee; Kim, Kyul; Nam, SangJin; Choi, Doyoung; Ha, Hyunsoo; Minn, Il; Byun, Youngjoo

DOI: 10.1016/j.bmcl.2019.126894

발행일: 2020-02-01

유형: Article

저널명: Bioorganic & Medicinal Chemistry Letters

권: 30

호: 3