Curtin Health Innovation Research Institute, Western Australian Biomedical Research Institute, School of Biomedical Sciences, Curtin University, Perth, WA 6845, Australia.
Drug Discov Today. 2010 Dec;15(23-24):1058-69. doi: 10.1016/j.drudis.2010.10.009. Epub 2010 Oct 23.
Glycosaminoglycans (GAGs) are an untapped source of novel chemical entities and, therefore, offer exciting new opportunities for the development of novel drug molecules because of their unique physical and biological properties. Advances in the functional understanding of GAG-protein interactions are enabling the development of GAG mimetics for use as anti-angiogenic, anti-metastatic, anti-inflammatory, anticoagulant and anti-thrombotic agents. Many anti-thrombotic molecules, such as Fondaparinux and Idraparinux, have been successful in clinical trials, and a new generation of heparin mimetic oligosaccharides and small molecules are currently in different stages of clinical development. In particular, the recent increased activity in the development of new mimetics by altering the composition of sulphated GAGs is very encouraging. This article reviews structurally defined heparin-mimetic oligosaccharides and small molecules currently in development or clinical trials.
糖胺聚糖（GAGs）是新型化学实体的未开发来源，因此，由于其独特的物理和生物学特性，为新型药物分子的开发提供了令人兴奋的新机会。GAG-蛋白相互作用功能理解的进步使 GAG 类似物的开发成为可能，可将其用作抗血管生成、抗转移、抗炎、抗凝和抗血栓形成剂。许多抗血栓形成分子，如磺达肝素和依达肝素，在临床试验中取得了成功，新一代肝素类似物寡糖和小分子目前处于不同的临床开发阶段。特别是，最近通过改变硫酸化 GAG 的组成来开发新型类似物的活动增加，这非常令人鼓舞。本文综述了目前正在开发或临床试验中的结构明确的肝素类似物寡糖和小分子。
