Radiolabeled bombesin derivatives for preclinical oncological imaging.
Radiolabeled bombesin derivatives for preclinical oncological imaging.
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DOI：
10.1016/j.biopha.2016.12.083
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发表时间：
2017-03
期刊：
影响因子：
--
通讯作者：
Barros ALB
中科院分区：
文献类型：
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作者：
Ferreira CA;Fuscaldi LL;Townsend DM;Rubello D;Barros ALB
尽管做出了努力，但癌症仍然是全球发病率和死亡率的主要原因之一，根据世界卫生组织的数据，每年约有1400万新病例和820万癌症相关死亡。在减少癌症进展和改善其管理的战略中，实施早期检测技术至关重要。基于几种类型的癌细胞过度表达表面受体的事实，人们开发了肽等小分子配体，以实现早期肿瘤识别。结合PET和SPECT等成像技术，放射性标记肽在核医学中发挥着关键作用。蛙皮素是哺乳动物胃泌素释放肽（GRP）的一种两栖动物同源物，是一种14个氨基酸的肽，已被广泛研究作为GRP阳性肿瘤（如乳腺癌、胰腺癌、肺癌和前列腺癌）的诊断和治疗的靶向配体。在这种情况下，在此我们提供了一个审查报告蛙皮素衍生物的放射性同位素标记的多种诊断目的在临床前设置。此外，由于动物模型是高度相关的评估这种放射性肽的临床翻译的潜力，目前使用的GRP阳性荷瘤动物模型的简要报告进行了描述。
Despite efforts, cancer is still one of the leading causes of morbidity and mortality worldwide, with approximately 14 million new cases and 8.2 million cancer-related deaths each year, according to the World Health Organization. Among the strategies to reduce cancer progression and improving its management, implementing early detection technologies is crucial. Based on the fact that several types of cancer cells overexpress surface receptors, small molecule ligands, such as peptides, have been developed to allow tumor identification at earlier stages. Allied with imaging techniques such as PET and SPECT, radiolabeled peptides play a pivotal role in nuclear medicine. Bombesin, a peptide of 14 amino acids, is an amphibian homolog to the mammalian gastrin-releasing peptide (GRP), that has been extensively studied as a targeting ligand for diagnosis and therapy of GRP positive tumors, such as breast, pancreas, lungs and prostate cancers. In this context, herein we provide a review of reported bombesin derivatives radiolabeled with a multitude of radioactive isotopes for diagnostic purposes in the preclinical setting. Moreover, since animal models are highly relevant for assessing the potential of clinical translation of this radiopeptides, a brief report of the currently used GRP-positive tumor-bearing animal models is described.