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Design and synthesis of a novel BODIPY-labeled PSMA inhibitor.
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2019-12-18 , 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 3 , Youngjoo Byun 4
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2019-12-18 , 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 3 , Youngjoo Byun 4
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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.
中文翻译：
一种新型BODIPY标记的PSMA抑制剂的设计与合成。
前列腺特异性膜抗原（PSMA）是与锌结合的金属蛋白酶，在转移性前列腺癌中高度表达。它被认为是前列腺癌成像和靶向治疗的优秀靶蛋白，因为它是一种膜蛋白，其活性位点位于细胞外区域。我们成功地合成和评估了与BODIPY650 / 665共轭的新型PSMA配体。化合物1表现出强大的PSMA抑制活性，并选择性地被表达PSMA的肿瘤吸收。化合物1有潜力用作靶向表达PSMA的癌症的近红外（NIR）光学成像探针。
更新日期：2019-12-18
中文翻译：
一种新型BODIPY标记的PSMA抑制剂的设计与合成。
前列腺特异性膜抗原（PSMA）是与锌结合的金属蛋白酶，在转移性前列腺癌中高度表达。它被认为是前列腺癌成像和靶向治疗的优秀靶蛋白，因为它是一种膜蛋白，其活性位点位于细胞外区域。我们成功地合成和评估了与BODIPY650 / 665共轭的新型PSMA配体。化合物1表现出强大的PSMA抑制活性，并选择性地被表达PSMA的肿瘤吸收。化合物1有潜力用作靶向表达PSMA的癌症的近红外（NIR）光学成像探针。
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