Dijkraaf I, Wester H J
Department of Nuclear Medicine, Technische Universität München, Ismaninger Strasse 22, 81675 München, Germany.
Handb Exp Pharmacol. 2008(185 Pt 2):61-92. doi: 10.1007/978-3-540-77496-9_4.
Due to their favorable properties and pharmacokinetics, peptides are often regarded as "agents of choice" for imaging and radiotherapy. Chemical strategies have been developed that allow their site specific labeling with various radionuclides for PET and SPECT, without compromising their biological integrity. Together with the overexpression of a wide range of peptide receptors and binding sites on tumor cells or matrix components, this class of compounds offers multiple imaging applications. Furthermore, radiolabeled peptides have great potential as carrier molecules for site-specific delivery of other signalling units, such as fluorescent moieties, cyctotoxic compounds or metals for magnetic resonance imaging. In addition, great efforts have been made to exploit the favorable characteristics of peptides for the development of larger constructs, such as multimeric ligands, polymer-peptide conjugates and "peptide-coated" liposomes and nanoparticles. Some peptides have already entered clinical routine application; some are currently being evaluated in clinical studies. However, a variety of peptides is still "waiting" to enter the imaging arena. This chapter presents a brief overview of the highly active field of peptide radiopharmaceuticals and the future potential of multimeric and polymeric peptide constructs.
由于其良好的性质和药代动力学，肽类常常被视为成像和放射治疗的“首选药物”。已经开发出化学策略，能够在不损害其生物学完整性的情况下，用各种放射性核素对其进行位点特异性标记，用于正电子发射断层扫描（PET）和单光子发射计算机断层扫描（SPECT）。再加上肿瘤细胞或基质成分上广泛存在的多种肽受体和结合位点的过表达，这类化合物提供了多种成像应用。此外，放射性标记的肽作为载体分子，具有极大的潜力用于其他信号单元的位点特异性递送，如荧光部分、细胞毒性化合物或用于磁共振成像的金属。此外，人们还付出了巨大努力，利用肽的有利特性来开发更大的构建体，如多聚体配体、聚合物 - 肽缀合物以及“肽包被”的脂质体和纳米颗粒。一些肽已经进入临床常规应用；一些目前正在临床研究中进行评估。然而，仍有多种肽“等待”进入成像领域。本章简要概述了肽类放射性药物这一高度活跃的领域以及多聚体和聚合物肽构建体的未来潜力。
