State Key Laboratory of Drug Research & Center for Pharmaceutics, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 501 Haike Road, Shanghai 201203, China.
Chem Soc Rev. 2018 May 21;47(10):3490-3529. doi: 10.1039/c7cs00793k.
Pathological changes in a diseased site are often accompanied by abnormal activities of various biomolecules in and around the involved cells. Identifying the location and expression levels of these biomolecules could enable early-stage diagnosis of the related disease, the design of an appropriate treatment strategy, and the accurate assessment of the treatment outcomes. Over the past two decades, a great diversity of peptide-based nanoprobes (PBNs) have been developed, aiming to improve the in vitro and in vivo performances of water-soluble molecular probes through engineering of their primary chemical structures as well as the physicochemical properties of their resultant assemblies. In this review, we introduce strategies and approaches adopted for the identification of functional peptides in the context of molecular imaging and disease diagnostics, and then focus our discussion on the design and construction of PBNs capable of navigating through physiological barriers for targeted delivery and improved specificity and sensitivity in recognizing target biomolecules. We highlight the biological and structural roles that low-molecular-weight peptides play in PBN design and provide our perspectives on the future development of PBNs for clinical translation.
病变部位的病理变化通常伴随着相关细胞内外各种生物分子的异常活动。鉴定这些生物分子的位置和表达水平可以实现相关疾病的早期诊断、适当治疗策略的设计以及治疗效果的准确评估。在过去的二十年中，已经开发出了大量基于肽的纳米探针（PBNs），旨在通过对其初级化学结构以及其组装体的物理化学性质进行工程设计，来提高水溶性分子探针的体外和体内性能。在这篇综述中，我们介绍了在分子成像和疾病诊断背景下鉴定功能肽的策略和方法，然后重点讨论了设计和构建能够穿越生理屏障进行靶向递药的 PBNs 的方法，以提高识别靶生物分子的特异性和灵敏度。我们强调了在 PBN 设计中低分子量肽所起的生物学和结构作用，并对 PBN 用于临床转化的未来发展提出了看法。
