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基于肽的放射性药物和细胞毒性缀合物:对抗癌症的潜在工具。

Peptide-based radiopharmaceuticals and cytotoxic conjugates: potential tools against cancer.

作者信息

Okarvi S M

机构信息

Cyclotron and Radiopharmaceuticals Department, King Faisal Specialist Hospital and Research Centre, Riyadh, Saudi Arabia.

出版信息

Cancer Treat Rev. 2008 Feb;34(1):13-26. doi: 10.1016/j.ctrv.2007.07.017. Epub 2007 Sep 17.

DOI:10.1016/j.ctrv.2007.07.017
PMID:17870245
Abstract

A hope for the diagnosis and treatment of cancer is the development of new tumor-specific peptide-based radiopharmaceuticals. The overexpression of many peptide receptors on human tumors makes such receptors an attractive potential target for diagnostic imaging and radiotherapy with specifically designed radiolabeled peptides. The use of solid-phase peptide synthesis, and the availability of a wide range of bifunctional chelating agents for the convenient radiolabeling of bioactive peptides with different radionuclides have produced a wide variety of medicinally useful peptide radiopharmaceuticals. A few of these peptides, such as somatostatin, bombesin, cholecystokinin/gastrin, neurotensin and vasoactive intestinal peptide are currently under investigation for their possible clinical applications in nuclear oncology. This article presents the recent development in radiolabeled small peptides, with major emphasis on somatostatin and bombesin analogs.

摘要

癌症诊断与治疗的一个希望是开发新型基于肿瘤特异性肽的放射性药物。人类肿瘤上许多肽受体的过度表达使得这些受体成为使用专门设计的放射性标记肽进行诊断成像和放射治疗的有吸引力的潜在靶点。固相肽合成的应用以及多种双功能螯合剂的可得性,便于用不同放射性核素对生物活性肽进行放射性标记,从而产生了各种各样具有药用价值的肽放射性药物。其中一些肽,如生长抑素、蛙皮素、胆囊收缩素/胃泌素、神经降压素和血管活性肠肽,目前正在研究它们在核肿瘤学中的可能临床应用。本文介绍了放射性标记小肽的最新进展,主要重点是生长抑素和蛙皮素类似物。

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