Indoleamine 2, 3-dioxygenase 1 (IDO1) is the only rate-limiting enzyme outside the liver that catalyzes the oxidation and cracking of indole rings in the tryptophan along the kynurenine pathway (KP). The overactivation of IDO1 is closely related to the pathogenesis of various human immune and neurological diseases. As an important target for the treatment of many human serious diseases, including malignant tumors, the development of IDO1 inhibitors is of great practical significance. In this work, the structure and function of IDO1 both are summarized from the aspects of the signal pathway, catalytic mechanism, structural biology, and so on. Moreover, the current development status of IDO1 inhibitors is also systematically reviewed, which provides assistance for anti-cancer drug design based on the structure of receptors.

中文翻译：

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吲哚胺2, 3-双加氧酶1及其抑制剂的结构和功能研究进展。

吲哚胺 2, 3-双加氧酶 1 (IDO1) 是肝脏外唯一的限速酶，可沿犬尿氨酸途径 (KP) 催化色氨酸中吲哚环的氧化和裂解。IDO1的过度激活与多种人体免疫和神经系统疾病的发病机制密切相关。作为治疗包括恶性肿瘤在内的许多人类严重疾病的重要靶点，IDO1抑制剂的开发具有重要的现实意义。本文从信号通路、催化机制、结构生物学等方面对IDO1的结构和功能进行了综述。此外，还系统回顾了IDO1抑制剂的发展现状，为基于受体结构的抗癌药物设计提供了帮助。