Department of Chemistry & Biochemistry, San Diego State University, San Diego, CA 92182, USA.
Curr Med Chem. 2012;19(20):3255-65. doi: 10.2174/092986712801215856.
Due to the growing toolkit of targeted contrast agents, molecular imaging continues to play a prominent role in the clinical care of cancer. Peptide-based imaging approaches are of particular significance due to their favorable pharmacokinetic properties, established manufacturing infrastructure, and documented clinical success in whole-body imaging. A logical extension of molecular imaging with peptides is to improve surgical outcomes in cancer through highly sensitive and specific probes which can be used intraoperatively. Advances in fluorescent imaging have resulted in various peptide labeling strategies with intraoperative indications. In this review, we focused on the evolving design of peptide imaging agents starting with the clinically used somatostatin targeting peptides. We then review the current synthetic approaches used for dual-labeled agent development and offer perspectives on optimal protection schemes that can be used for multimodal probe development.
由于靶向对比剂的工具包不断增加，分子成像在癌症的临床治疗中继续发挥突出作用。基于肽的成像方法具有重要意义，因为它们具有良好的药代动力学特性、成熟的制造基础设施以及在全身成像方面的临床成功记录。肽的分子成像的一个合乎逻辑的延伸是通过高度敏感和特异的探针来改善癌症的手术结果，这些探针可以在手术中使用。荧光成像的进步已经产生了各种具有术中适应证的肽标记策略。在本综述中，我们从临床应用的生长抑素靶向肽开始，重点介绍了肽成像剂的不断发展的设计。然后，我们回顾了目前用于双标记剂开发的合成方法，并对可用于多模式探针开发的最佳保护方案提出了看法。
