Tumour-associated macrophages (TAMs) that present abundantly in the tumour microenvironment (TME) exhibit a protumour property, such as promoting genetic instability, tumour metastasis and immunosuppression. Macrophage-targeted therapeutic approaches hence have been applied and shown their significances in the process of tumour immune treatment, including blocking TAM recruitment, depleting or transforming TAMs that already exist in the tumour site. Here, we summarized the functional regulation of TAMs in the respects of hypoxia environment, metabolism in the tumour microenvironment and the transcription factors involved. We reviewed the strategies for transforming TAMs, including immune stimuli targeting TAMs, inhibitors against TAMs, pathogen or irradiation stimulation on TAMs, and the application of natural compounds in TAMs. Furthermore, we also discussed the macrophage-targeted therapies in the clinical studies. Taken together, this review tries to shed light on the TAM regulation and the main strategies of TAM reprogramming for an enhanced immune surveillance.

大量存在于肿瘤微环境 (TME) 中的肿瘤相关巨噬细胞 (TAM) 表现出促肿瘤特性，例如促进遗传不稳定性、肿瘤转移和免疫抑制。因此，巨噬细胞靶向治疗方法已被应用并显示其在肿瘤免疫治疗过程中的重要性，包括阻断 TAM 募集、消耗或转化肿瘤部位已存在的 TAM。在这里，我们总结了TAMs在缺氧环境、肿瘤微环境中的代谢和所涉及的转录因子方面的功能调节。我们回顾了转化 TAM 的策略，包括针对 TAM 的免疫刺激、针对 TAM 的抑制剂、病原体或对 TAM 的辐射刺激，以及天然化合物在 TAM 中的应用。此外，我们还讨论了临床研究中的巨噬细胞靶向疗法。总之，这篇综述试图阐明 TAM 调节和 TAM 重编程以增强免疫监视的主要策略。