半乳糖凝集素是一类内源性糖蛋白，能与糖元结合，在广泛的生理和病理过程中起着重要作用。这些蛋白质作为一个群体，使用细胞外和细胞内机制，以及依赖和不依赖糖元的途径，重编程许多细胞类型的命运和功能。由于半乳糖凝集素在组织纤维化和癌症中的多功能作用，它们被认为是这些疾病的潜在治疗靶点。在本文中，我们重点探讨了半乳糖凝集素在肿瘤进展和纤维化疾病中的治疗相关性，特别是GAL1、GAL3和GAL9。我们考虑了一系列针对半乳糖凝集素的策略，包括小分子碳水化合物抑制剂、天然多糖及其衍生物、肽、肽类似物和生物制剂（特别是中和单克隆抗体和截短的半乳糖凝集素），并讨论它们在纤维化和癌症临床前模型中的作用机制、选择性和治疗潜力。我们还回顾了旨在评估半乳糖凝集素抑制剂在原因不明的肺纤维化、非酒精性脂肪肝和癌症患者中的疗效的临床试验结果。糖生物学研究的快速推进，加上缓解纤维化炎症和克服抗癌治疗抵抗的药物迫切需求，将加速抗半乳糖凝集素治疗药物进入临床实践。© 2023 Springer Nature Limited。

Galectins are a family of endogenous glycan-binding proteins that have crucial roles in a broad range of physiological and pathological processes. As a group, these proteins use both extracellular and intracellular mechanisms as well as glycan-dependent and independent pathways to reprogramme the fate and function of numerous cell types. Given their multifunctional roles in both tissue fibrosis and cancer, galectins have been identified as potential therapeutic targets for these disorders. Here, we focus on the therapeutic relevance of galectins, particularly galectin 1 (GAL1), GAL3 and GAL9 to tumour progression and fibrotic diseases. We consider an array of galectin-targeted strategies, including small-molecule carbohydrate inhibitors, natural polysaccharides and their derivatives, peptides, peptidomimetics and biological agents (notably, neutralizing monoclonal antibodies and truncated galectins) and discuss their mechanisms of action, selectivity and therapeutic potential in preclinical models of fibrosis and cancer. We also review the results of clinical trials that aim to evaluate the efficacy of galectin inhibitors in patients with idiopathic pulmonary fibrosis, nonalcoholic steatohepatitis and cancer. The rapid pace of glycobiology research, combined with the acute need for drugs to alleviate fibrotic inflammation and overcome resistance to anticancer therapies, will accelerate the translation of anti-galectin therapeutics into clinical practice.© 2023. Springer Nature Limited.