Metabolic glycoengineering with unnatural sugars provides a powerful tool to label cell membranes with chemical tags for subsequent targeted conjugation of molecular cargos via efficient chemistries. This technology has been widely explored for cancer labelling and targeting. However, as this metabolic labelling process can occur in both cancerous and normal cells, cancer-selective labelling needs to be achieved to develop cancer-targeted therapies. Unnatural sugars can be either rationally designed to enable preferential labelling of cancer cells, or specifically delivered to cancerous tissues. In this Review Article, we will discuss the progress to date in design and delivery of unnatural sugars for metabolic labelling of tumour cells and subsequent development of tumour-targeted therapy. Metabolic cell labelling for cancer immunotherapy will also be discussed. Finally, we will provide a perspective on future directions of metabolic labelling of cancer and immune cells for the development of potent, clinically translatable cancer therapies.

用非天然糖进行代谢糖工程提供了一种强大的工具，可以用化学标签标记细胞膜，以便随后通过有效的化学方法进行分子货物的靶向结合。该技术已被广泛用于癌症标记和靶向。然而，由于这种代谢标记过程可以发生在癌细胞和正常细胞中，因此需要实现癌症选择性标记以开发癌症靶向疗法。非天然糖可以经过合理设计以优先标记癌细胞，或专门输送到癌组织。在这篇综述文章中，我们将讨论迄今为止在用于肿瘤细胞代谢标记的非天然糖的设计和递送以及肿瘤靶向治疗的后续发展方面的进展。还将讨论用于癌症免疫治疗的代谢细胞标记。最后，我们将为癌症和免疫细胞的代谢标记的未来方向提供一个视角，以开发有效的、临床可转化的癌症疗法。