State Key Laboratory of Genetic Engineering, Department of Biochemistry, School of Life Sciences, Fudan University, Songhu Road 2005, Shanghai 200438, China.
Shanghai Key Lab of Chemical Assessment and Sustainability, School of Chemical Science and Engineering, Tongji University, 1239 Siping Road, 200092 Shanghai, China.
Bioorg Chem. 2020 Nov;104:104348. doi: 10.1016/j.bioorg.2020.104348. Epub 2020 Oct 8.
Inhibitors of indoleamine 2,3-dioxygenase 1 (IDO1) and tryptophan 2,3-dioxygenase (TDO) are potential drugs for the treatment of tumor and neurological diseases. A variety of bioassays have been developed to evaluate IDO1/TDO (IDO1 and/or TDO) inhibitors, with uncertainty regarding how the differences in the assay methods or protocols may influence the assay outcomes. The enzymatic assays of IDO1/TDO are usually performed with NFK assay and Kyn adduct assay while the cellular assays of IDO1 are carried out with Hela assay and HEK293 assay. The present study focused on the comparison of the most common bioassays of IDO1/TDO. In addition, the effects of major factors of bioassays such as reaction time and culture medium on the assay outcomes were evaluated. The study will provide reference for the researchers to select IDO1/TDO inhibitors with bioassays, and promote the development of IDO1/TDO inhibitors.
吲哚胺 2,3-双加氧酶 1（IDO1）和色氨酸 2,3-双加氧酶（TDO）抑制剂是治疗肿瘤和神经疾病的潜在药物。已经开发了多种生物测定法来评估 IDO1/TDO（IDO1 和/或 TDO）抑制剂，但对于测定方法或方案的差异如何影响测定结果存在不确定性。IDO1/TDO 的酶促测定通常使用 NFK 测定法和 Kyn 加合物测定法进行，而 IDO1 的细胞测定则使用 Hela 测定法和 HEK293 测定法进行。本研究重点比较了 IDO1/TDO 的最常见生物测定法。此外，还评估了生物测定中主要因素（如反应时间和培养基）对测定结果的影响。该研究将为研究人员选择具有生物测定法的 IDO1/TDO 抑制剂提供参考，并促进 IDO1/TDO 抑制剂的发展。
Bioorg Med Chem. 2019-2-8
J Biomol Screen. 2014-10
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