2. Academic Validation
  3. Establishment of a human indoleamine 2, 3-dioxygenase 2 (hIDO2) bioassay system and discovery of tryptanthrin derivatives as potent hIDO2 inhibitors

Establishment of a human indoleamine 2, 3-dioxygenase 2 (hIDO2) bioassay system and discovery of tryptanthrin derivatives as potent hIDO2 inhibitors

  • Eur J Med Chem. 2016 Nov 10;123:171-179. doi: 10.1016/j.ejmech.2016.07.013.
Juanjuan Li 1,  Yang Li 1,  Dan Yang 1,  Nan Hu 1,  Zhanling Guo 1,  Chunxiang Kuang 2,  Qing Yang 3
Affiliations

Affiliations

  • 1 State Key Laboratory of Genetic Engineering, School of Life Sciences, Fudan University, Songhu Road 2005, Shanghai, 200438, China.
  • 2 Department of Chemistry, Tongji University, Siping Road 1239, Shanghai, 200092, China.
  • 3 State Key Laboratory of Genetic Engineering, School of Life Sciences, Fudan University, Songhu Road 2005, Shanghai, 200438, China; Shanghai Collaborative Innovation Center for Biomanufacturing (SCICB), East China University of Science and Technology, 130 Meilong Road, Shanghai, 200237, China. Electronic address: yangqing68@fudan.edu.cn.
PMID: 27475108 DOI: 10.1016/j.ejmech.2016.07.013
Abstract

As an analogue of IDO1 (indoleamine 2, 3-dioxygenase 1), the well-known new therapeutic target, IDO2 is receiving increased attention. Herein, the expression and purification of recombinant human IDO2 (hIDO2) and the establishment of a hIDO2 bioassay system on both enzymatic and cellular levels are described. Nine tryptanthrin derivatives were screened for potential hIDO2 inhibitory activities, and their Ki values, enzymatic and cellular IC50 values, as well as the types of inhibition were measured. The typtanthrin derivatives 5i, 5c and 5d (especially 5i) were found to be potent hIDO2 inhibitors with superior efficiency far better than that of the most frequently-used inhibitor L-1-MT. Two ultimate purposes of the present study have been achieved: establishing an IDO2 bioassay system and screening novel IDO2 inhibitors that can be used (directly or with some modifications) for potential therapeutic applications.

Keywords

3-dioxygenase 2; IDO2 bioassay system; IDO2 inhibitor; Indoleamine 2; Tryptanthrin derivatives.

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