Department of Nuclear Medicine and Molecular Imaging, University of Groningen, University Medical Center Groningen, Groningen, The Netherlands.
Curr Pharm Des. 2013;19(18):3329-41. doi: 10.2174/1381612811319180015.
Prostate cancer is a critical public health problem in USA and Europe. New non-invasive imaging methods are urgently needed, due to the low accuracy and specificity of current screen methods and the desire of localizing primary prostate cancer and bone metastasis. Positron Emission Tomography (PET) and Single Photon Emission Computed Tomography (SPECT) are the non-invasive and sensitive imaging methods which have been widely used for diagnosing diseases in the clinic. Lack of suitable radiotracers is the major issue for nuclear imaging of prostate cancer, although radiolabeled bombesin (BN) peptides targeting the Gastrin-Releasing Peptide Receptor (GRPR) on tumor cells are widely investigated. In this review we discuss the recent trends in the development of GRPR-targeted radiopharmaceuticals based on BN analogs with regard to their potential for imaging and therapy of GRPR-expressing malignancies. Following a brief introduction of GRPR and bombesin peptides, we summarize the properties of prostate cancer specific radiolabeled bombesins. New bombesin tracers published in the last five years are reviewed and compared according to their novelties in biomolecules, radionuclides, labeling methods, bifunctional chelators and linkers. Hot topics such as multimerization, application of agonists and antagonists are highlighted in the review. Lastly, a few clinical trials of cancer nuclear imaging with radiolabeled bombesin have been discussed.
前列腺癌是美国和欧洲的一个重大公共卫生问题。由于当前筛查方法的准确性和特异性较低，以及定位前列腺癌原发灶和骨转移的需求，迫切需要新的非侵入性成像方法。正电子发射断层扫描（PET）和单光子发射计算机断层扫描（SPECT）是用于临床诊断疾病的非侵入性和敏感的成像方法。尽管放射性标记的蛙皮素（BN）肽靶向肿瘤细胞上的胃泌素释放肽受体（GRPR）已被广泛研究，但缺乏合适的放射性示踪剂是前列腺癌核成像的主要问题。在这篇综述中，我们讨论了基于 BN 类似物的 GRPR 靶向放射性药物的最新发展趋势，以及它们在成像和治疗 GRPR 表达恶性肿瘤方面的潜力。在简要介绍 GRPR 和蛙皮素肽之后，我们总结了前列腺癌特异性放射性标记蛙皮素的特性。根据生物分子、放射性核素、标记方法、双功能螯合剂和连接物的新颖性，对过去五年发表的新的蛙皮素示踪剂进行了综述和比较。本文强调了多聚化、激动剂和拮抗剂的应用等热门话题。最后，讨论了一些使用放射性标记蛙皮素进行癌症核成像的临床试验。
