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Image-Guided Surgery: Are We Getting the Most Out of Small-Molecule Prostate-Specific-Membrane-Antigen-Targeted Tracers?
Bioconjugate Chemistry ( IF 4.7 ) Pub Date : 2020-01-06 , DOI: 10.1021/acs.bioconjchem.9b00758
Albertus Wijnand Hensbergen 1 , Danny M van Willigen 1 , Florian van Beurden 1, 2 , Pim J van Leeuwen 2 , Tessa Buckle 1, 2 , Margret Schottelius 3 , Tobias Maurer 4 , Hans-Jürgen Wester 5 , Fijs W B van Leeuwen 1, 2
Affiliation  

Expressed on virtually all prostate cancers and their metastases, the transmembrane protein prostate-specific membrane antigen (PSMA) provides a valuable target for the imaging of prostate cancer. Not only does PSMA provide a target for noninvasive diagnostic imaging, e.g., PSMA-positron emission tomography (PSMA-PET), it can also be used to guide surgical resections of PSMA-positive lesions. The latter characteristic has led to the development of a plethora of PSMA-targeted tracers, i.e., radiolabeled, fluorescent, or hybrid. With image-guided surgery applications in mind, this review discusses these compounds based on clinical need. Here, the focus is on the chemical aspects (e.g., imaging label, spacer moiety, and targeting vector) and their impact on in vitro and in vivo tracer characteristics (e.g., affinity, tumor uptake, and clearance pattern).

中文翻译:

图像引导手术:我们是否充分利用小分子前列腺特异性膜抗原靶向示踪剂?

跨膜蛋白前列腺特异性膜抗原 (PSMA) 几乎在所有前列腺癌及其转移灶上表达,为前列腺癌成像提供了有价值的靶标。PSMA 不仅为无创诊断成像(例如 PSMA-正电子发射断层扫描 (PSMA-PET))提供了靶标,还可以用于指导 PSMA 阳性病变的手术切除。后一个特征导致了大量 PSMA 靶向示踪剂的开发,即放射性标记的、荧光的或混合的。考虑到图像引导手术的应用,本综述根据临床需求讨论了这些化合物。这里,重点是化学方面(例如,成像标记、间隔部分和靶向载体)及其对体外和体内示踪剂特征(例如,亲和力、肿瘤摄取和清除模式)的影响。
更新日期:2020-01-07
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