Department of Medicinal Chemistry, Drug Discovery and Development, Virginia Commonwealth University, Richmond, VA 23219, USA.
Institute for Structural Biology, Drug Discovery and Development, Virginia Commonwealth University, Richmond, VA 23219, USA.
Int J Mol Sci. 2019 Apr 22;20(8):1963. doi: 10.3390/ijms20081963.
Glycosaminoglycans (GAGs) are a class of biomolecules expressed virtually on all mammalian cells and usually covalently attached to proteins, forming proteoglycans. They are present not only on the cell surface, but also in the intracellular milieu and extracellular matrix. GAGs interact with multiple ligands, both soluble and insoluble, and modulate an important role in various physiological and pathological processes including cancer, bacterial and viral infections, inflammation, Alzheimer's disease, and many more. Considering their involvement in multiple diseases, their use in the development of drugs has been of significant interest in both academia and industry. Many GAG-based drugs are being developed with encouraging results in animal models and clinical trials, showcasing their potential for development as therapeutics. In this review, the role GAGs play in both the development and inhibition of cancer and inflammation is presented. Further, advancements in the development of GAGs and their mimetics as anti-cancer and anti-inflammatory agents are discussed.
糖胺聚糖（GAGs）是一类几乎存在于所有哺乳动物细胞中的生物分子，通常与蛋白质共价结合，形成蛋白聚糖。它们不仅存在于细胞表面，还存在于细胞内环境和细胞外基质中。GAGs 与多种可溶性和不溶性配体相互作用，并在包括癌症、细菌和病毒感染、炎症、阿尔茨海默病等在内的多种生理和病理过程中发挥重要作用。鉴于它们在多种疾病中的参与，它们在药物开发中的应用在学术界和工业界都引起了极大的兴趣。许多基于 GAG 的药物在动物模型和临床试验中取得了令人鼓舞的结果，展示了它们作为治疗剂的开发潜力。在这篇综述中，介绍了 GAG 在癌症和炎症的发展和抑制中的作用。此外，还讨论了 GAG 及其类似物作为抗癌和抗炎药物的开发进展。
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