Glycosphingolipids (GSLs) are major amphiphilic glycolipids present on the surface of living cell membranes. They have important biological functions, including maintaining plasma membrane stability, regulating signal transduction, and mediating cell recognition and adhesion. Specific GSLs and related enzymes are abnormally expressed in many cancer diseases and affect the malignant characteristics of tumors. The regulatory roles of GSLs in signaling pathways suggest that they are involved in tumor pathogenesis. GSLs have therefore been widely studied as diagnostic markers of cancer diseases and important targets of immunotherapy. This review describes the tumor-related biological functions of GSLs and systematically introduces recent progress in using diverse GSLs and related enzymes to diagnose and treat tumor diseases. Development of drugs and biomarkers for personalized cancer therapy based on GSL structure is also discussed. These advances, combined with recent progress in the preparation of GSLs derivatives through synthetic biology technologies, suggest a strong future for the use of customized GSL libraries in treating human diseases.

鞘糖脂 (GSL) 是存在于活细胞膜表面的主要两亲性糖脂。它们具有重要的生物学功能，包括维持质膜稳定性、调节信号转导以及介导细胞识别和粘附。特定的GSLs及相关酶在许多癌症疾病中异常表达并影响肿瘤的恶性特征。GSL 在信号通路中的调节作用表明它们参与肿瘤发病机制。因此，GSL 作为癌症疾病的诊断标志物和免疫治疗的重要靶点已被广泛研究。本文综述了GSLs与肿瘤相关的生物学功能，系统介绍了利用多种GSLs及相关酶诊断和治疗肿瘤疾病的最新进展。还讨论了基于 GSL 结构的个性化癌症治疗药物和生物标志物的开发。这些进展，加上通过合成生物学技术制备 GSL 衍生物的最新进展，表明使用定制 GSL 文库治疗人类疾病有着广阔的前景。