Chittasupho Chuda
Department of Pharmaceutical Technology, Faculty of Pharmacy, Srinakharinwirot University, 63 Mu 7 Rangsit-Nakhonnayok Road, Ongkharak, Nakhonnayok, 26120, Thailand.
Ther Deliv. 2012 Oct;3(10):1171-87. doi: 10.4155/tde.12.99.
Multivalent interactions of biological molecules play an important role in many biochemical events. A multivalent ligand comprises of multiple copies of ligands conjugated to scaffolds, allowing the simultaneous binding of multivalent ligands to multiple binding sites or receptors. Many research groups have successfully designed and synthesized multivalent ligands to increase the binding affinity, avidity and specificity of the ligand to the receptor. A multimeric ligand is a promising option for the specific treatment of diseases. In this review, the factors affecting multivalent interactions, including the size and shape of the ligand, geometry and an arrangement of ligands on the scaffold, linker length, thermodynamic, and kinetics of the interactions are discussed. Examples of the multivalent ligand applications for therapeutic delivery are also summarized.
生物分子的多价相互作用在许多生化事件中起着重要作用。多价配体由与支架缀合的多个配体拷贝组成，允许多价配体同时与多个结合位点或受体结合。许多研究小组已成功设计并合成了多价配体，以提高配体与受体的结合亲和力、亲合力和特异性。多聚体配体是疾病特异性治疗的一个有前景的选择。在这篇综述中，讨论了影响多价相互作用的因素，包括配体的大小和形状、支架上配体的几何形状和排列、连接子长度、相互作用的热力学和动力学。还总结了多价配体在治疗递送中的应用实例。
