Among glycan-binding proteins, galectins, β-galactoside-binding lectins, exhibit relevant biological roles and are implicated in many diseases, such as cancer and inflammation. Their involvement in crucial pathologies makes them interesting targets for drug discovery. In this review, we gather the last approaches toward the specific design of glycomimetics as potential drugs against galectins. Different approaches, either using specific glycomimetic molecules decorated with key functional groups or employing multivalent presentations of lactose and N-acetyl lactosamine analogs, have provided promising results for binding and modulating different galectins. The review highlights the results obtained with these approximations, from the employment of S-glycosyl compounds to peptidomimetics and multivalent glycopolymers, mostly employed to recognize and/or detect hGal-1 and hGal-3.

在聚糖结合蛋白中，半乳凝素，β-半乳糖苷结合凝集素显示出相关的生物学作用，并且与许多疾病有关，例如癌症和炎症。他们参与关键的病理学使得他们成为药物发现的有趣目标。在这篇综述中，我们收集了针对糖模拟物作为抗半乳凝素的潜在药物进行具体设计的最新方法。通过使用装饰有关键功能基团的特定糖模拟分子或采用乳糖和N-乙酰基乳糖胺类似物的多价表示法，不同方法为结合和调节不同半乳糖凝集素提供了有希望的结果。该评论重点介绍了从这些近似值获得的结果，从使用S-糖基化合物到拟肽和多价糖聚合物，HGal-1和 HGal-3。