Peptide heterodimers for molecular imaging.
Peptide heterodimers for molecular imaging.
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DOI：
10.1007/s00726-010-0546-y
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发表时间：
2011-11
期刊：
影响因子：
3.5
通讯作者：
Chen, Xiaoyuan
中科院分区：
文献类型：
--
作者：
Yan, Yongjun;Chen, Xiaoyuan
基于肽的分子成像探针的一个主要问题是它们相对较低的肿瘤亲和力和较短的保留时间。为了提高肽的结合亲和力，引入了多价方法。传统上，这种方法涉及使用肽同二聚体或同聚体，其中相同类型的肽配体与合适的连接体构建。近年来，利用多肽异二聚体作为靶向多受体过表达肿瘤细胞的新方法已成为一种很有前景的方法。与亲本肽单体相比，已观察到与肽异源二聚体的显著亲和增强。在肽异二聚体中，能够靶向两种不同受体的两种不同肽配体是共价连接的。肽异二聚体的结合方式可以是单价的，也可以是二价的，这取决于两个配体能否同时结合。随着局部配体浓度的增加和结合动力学的改善，在单价和二价结合模式下的结合都增强了，而多价效应在二价结合模式中也起着重要作用。由于许多肿瘤过表达多种受体，未来有望开发更多基于多肽异二聚体的分子成像探针。本文综述了多肽同二聚体和异二聚体在分子成像中的应用，重点介绍了多肽异二聚体。
One main issue with peptide-based molecular imaging probes is their relatively low tumor affinity and short retention time. To improve peptide binding affinity, multivalency approach has been introduced. Traditionally, this approach involves the use of peptide homodimers or homomultimers in which peptide ligands of the same type are constructed with suitable linkers. Recently, a new approach using peptide heterodimers has emerged as a promising method for targeting multi-receptor over-expressed tumor cells. Significant affinity enhancements have been observed with peptide heterodimers compared with their parent peptide monomers. In a peptide hetero-dimer, two different peptide ligands capable of targeting two different receptors are covalently linked. The binding modes of peptide heterodimers can be monovalent or bivalent depending on whether simultaneous binding of two ligands can be achieved. Increased local ligand concentration and improved binding kinetics contribute to enhanced binding in both monovalent- and bivalent binding modes, while multivalency effect also plays an important role in bivalent binding mode. As many tumors overexpress multiple receptors, more peptide heterodimer-based molecular imaging probes are expected to be developed in future. This review article will discuss the peptide homodimers and heterodimers for molecular imaging with special emphasis on peptide heterodimers.
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影响因子：
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