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基于金属的前列腺特异性膜抗原放射性配体

Metal-Based PSMA Radioligands.

作者信息

Gourni Eleni, Henriksen Gjermund

机构信息

Institute of Basic Medical Sciences, University of Oslo, Oslo 0372, Norway.

Norwegian Medical Cyclotron Centre Ltd., P.O. Box 4950 Nydalen, Oslo 0424, Norway.

出版信息

Molecules. 2017 Mar 24;22(4):523. doi: 10.3390/molecules22040523.

DOI:10.3390/molecules22040523
PMID:28338640
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6154343/
Abstract

Prostate cancer is one of the most common malignancies for which great progress has been made in identifying appropriate molecular targets that would enable efficient in vivo targeting for imaging and therapy. The type II integral membrane protein, prostate specific membrane antigen (PSMA) is overexpressed on prostate cancer cells in proportion to the stage and grade of the tumor progression, especially in androgen-independent, advanced and metastatic disease, rendering it a promising diagnostic and/or therapeutic target. From the perspective of nuclear medicine, PSMA-based radioligands may significantly impact the management of patients who suffer from prostate cancer. For that purpose, chelating-based PSMA-specific ligands have been labeled with various diagnostic and/or therapeutic radiometals for single-photon-emission tomography (SPECT), positron-emission-tomography (PET), radionuclide targeted therapy as well as intraoperative applications. This review focuses on the development and further applications of metal-based PSMA radioligands.

摘要

前列腺癌是最常见的恶性肿瘤之一，在确定合适的分子靶点方面已取得了巨大进展，这些靶点能够实现体内高效靶向成像和治疗。II型整合膜蛋白前列腺特异性膜抗原（PSMA）在前列腺癌细胞上的表达与肿瘤进展的阶段和分级成正比，尤其是在雄激素非依赖性、晚期和转移性疾病中，这使其成为一个有前景的诊断和/或治疗靶点。从核医学的角度来看，基于PSMA的放射性配体可能会显著影响前列腺癌患者的管理。为此，基于螯合的PSMA特异性配体已用各种诊断和/或治疗放射性金属进行标记，用于单光子发射断层扫描（SPECT）、正电子发射断层扫描（PET）、放射性核素靶向治疗以及术中应用。本综述重点关注基于金属的PSMA放射性配体的开发和进一步应用。

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