Hou Xi-Xi, Wu Zi-Yuan, Zhan An, Gao En, Mao Long-Fei, Wang Hui-Li, Yang Jian-Xue
Department of Pharmacy, The First Affiliated Hospital, and College of Clinical Medicine of Henan University of Science and Technology, Luoyang, China.
School of Nursing, College of Basic Medicine and Forensic Medicine, Henan University of Science and Technology, Luoyang, China.
Front Chem. 2023 Jun 20;11:1222825. doi: 10.3389/fchem.2023.1222825. eCollection 2023.
Indoleamine 2,3-dioxygenase 1 (IDO1) has attracted much attention in the field of cancer immunotherapy as an immunomodulatory enzyme. To identify potential IDO1 inhibitors, a novel series of compounds with N,N-diphenylurea and triazole structures were synthesized. The designed compounds underwent organic synthesis, and subsequent enzymatic activity experiments targeting IDO1 confirmed their activity at the molecular level. These experiments provided validation for the efficacy of the designed compounds in inhibiting IDO1, compound exhibited an IC value of 1.73 ± 0.97 μM. Further molecular docking study further explained the binding mode and reaction potential of compound with IDO1. Our research has resulted in a series of novel IDO1 inhibitors, which is beneficial to the development of drugs targeting IDO1 in numerous cancer diseases.
吲哚胺2,3-双加氧酶1（IDO1）作为一种免疫调节酶，在癌症免疫治疗领域备受关注。为了鉴定潜在的IDO1抑制剂，合成了一系列具有N,N-二苯基脲和三唑结构的新型化合物。所设计的化合物经过有机合成，随后针对IDO1的酶活性实验在分子水平上证实了它们的活性。这些实验验证了所设计化合物抑制IDO1的功效，化合物表现出的IC值为1.73±0.97μM。进一步的分子对接研究进一步解释了该化合物与IDO1的结合模式和反应潜力。我们的研究产生了一系列新型IDO1抑制剂，这有利于针对多种癌症疾病开发靶向IDO1的药物。
