基于小分子肽的放射性药物
Peptide as carrier for diagnosis and treatment
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摘要: 由于肽分子小,标记物显示了良好的药代动力学性质,如迅速的靶器官摄取、快速的血液清除,为药物进入体内能早期获得显像提供了可能。目前面临的挑战是既要获得高比放的放射性标记的生物活性物质而又不能损伤肽的生物活性。分子生物工程技术已能合成各种生物活性的小分子肽,在它们的分子结构中可引入螯合基团而又不影响它们与受体结合的特性,因而获得高比活度的产品。本文扼要综述了目前基于小分子肽的受体靶向的放射性药物的研究与临床应用情况,主要包括标记的小分子肽的基本特性,及其在血栓、炎症/感染、肿瘤的诊断和治疗方面的应用。Abstract: Due to their small size,peptide molecules exhibit farourablepharmacokinetic characterstics,such as rapid uptake by target tissue and rapid blook clearance,which potentiallyallowes images to be acquired earlier following the administration of a radiolabeled peptide radiopharmaceutical.The challenge is to label bioactive peptide with radioisotop with high specific activity without impairing the biological properties of the peptides.Molecular engineering technique now permits synthesis of a wide range of biologically active peptides that carry chelating groups in their structure without their receptor binding properties,thus permitting a high specific activity product.This article briefly summarized current experiments and clinicalapplication of the radiopharmaceuticals based on small receptor-binding peptides.The basic characteristics and the application of diagnosis and therapy with thrombus,infection/inflammation,and tumors are mainly reviewed.
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Key words:
- small peptides /
- radiopharmaceutical /
- imaging agents /
- therapeutic agent
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