The utility of radiolabeled PSMA ligands for tumor imaging,Chemical Biology & Drug Design

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The utility of radiolabeled PSMA ligands for tumor imaging
Chemical Biology & Drug Design ( IF 3.2 ) Pub Date : 2021-09-02 , DOI: 10.1111/cbdd.13946
Pejman Shahrokhi ₁ , Arezou Masteri Farahani ₁ , Mohammad Tamaddondar ₂ , Farzaneh Rezazadeh ₃

Affiliation

Prostate-specific membrane antigen (PSMA) is a glycosylated type-II transmembrane protein expressed in prostatic tissue and significantly overexpressed in several prostate cancer cells. Despite its name, PSMA has also been reported to be overexpressed in endothelial cells of benign and malignant non-prostate disease. So its clinical use was extended to detection, staging, and therapy of various tumor types. Recently small molecules targeting PSMA have been developed as imaging probes for diagnosis of several malignancies. Preliminary studies are emerging improved diagnostic sensitivity and specificity of PSMA imaging, leading to a change in patient management. In this review, we evaluated the first preclinical and clinical studies on PSMA ligands resulting future perspectives radiolabeled PSMA in staging and molecular characterization, based on histopathologic examinations of PSMA expression.

中文翻译：

放射性标记的 PSMA 配体在肿瘤成像中的应用

前列腺特异性膜抗原 (PSMA) 是一种糖基化的 II 型跨膜蛋白，在前列腺组织中表达并在几种前列腺癌细胞中显着过表达。尽管它的名字，据报道 PSMA 在良性和恶性非前列腺疾病的内皮细胞中过度表达。因此，其临床应用扩展到各种肿瘤类型的检测、分期和治疗。最近，针对 PSMA 的小分子已被开发为用于诊断几种恶性肿瘤的成像探针。初步研究正在提高 PSMA 成像的诊断敏感性和特异性，从而改变患者管理。在这篇综述中，我们评估了 PSMA 配体的首次临床前和临床研究，从而为放射性标记 PSMA 在分期和分子表征方面的未来前景提供了展望，

更新日期：2021-09-02

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