PD-L1在肿瘤细胞表面过度表达并与PD-1结合，导致肿瘤免疫逃逸。针对 PD-1/PD-L1 通路的治疗策略包括阻断结合。免疫检查点抑制剂对肿瘤的疗效有限，因为 PD-L1 也存在于细胞质中。 PD-L1 翻译后修饰 (PTM) 揭示了许多致癌机制，并确定了潜在的治疗靶点。因此，小分子抑制剂可以阻断关键的致癌信号通路，使其成为潜在的治疗选择。为了更好地开发小分子抑制剂，我们总结了PD-L1的PTM。本文讨论了小分子抑制剂在癌变过程中的调控机制，并探讨了其潜在应用，提出了一种基于PD-L1 PTM的肿瘤免疫治疗新方法。

PD-L1 is overexpressed on the surface of tumor cells and binds to PD-1, resulting in tumor immune escape. Therapeutic strategies to target the PD-1/PD-L1 pathway involve blocking the binding. Immune checkpoint inhibitors have limited efficacy against tumors because PD-L1 is also present in the cytoplasm. PD-L1 of post-translational modifications (PTMs) have uncovered numerous mechanisms contributing to carcinogenesis and have identified potential therapeutic targets. Therefore, small molecule inhibitors can block crucial carcinogenic signaling pathways, making them a potential therapeutic option. To better develop small molecule inhibitors, we have summarized the PTMs of PD-L1. This review discusses the regulatory mechanisms of small molecule inhibitors in carcinogenesis and explore their potential applications, proposing a novel approach for tumor immunotherapy based on PD-L1 PTM.