Implementation of the CYP Index for the Design of Selective Tryptophan-2,3-dioxygenase Inhibitors

[Image: see text] A class of imidazoisoindole (III) heme-binding indoleamine-2,3-dioxygenase (IDO1) inhibitors were optimized via structure-based drug design into a series of tryptophan-2,3-dioxygenase (TDO)-selective inhibitors. Kynurenine pathway modulation was demonstrated in vivo, which enabled...

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Vydáno v:ACS Med Chem Lett
Hlavní autoři: Parr, Brendan T., Pastor, Richard, Sellers, Benjamin D., Pei, Zhonghua, Jaipuri, Firoz A., Castanedo, Georgette M., Gazzard, Lewis, Kumar, Sanjeev, Li, Xiaokai, Liu, Wen, Mendonca, Rohan, Pavana, Roheeth K., Potturi, Hima, Shao, Cheng, Velvadapu, Venkata, Waldo, Jesse P., Wu, Guosheng, Yuen, Po-wai, Zhang, Zuhui, Zhang, Yamin, Harris, Seth F., Oh, Angela J., DiPasquale, Antonio, Dement, Kevin, La, Hank, Goon, Leanne, Gustafson, Amy, VanderPorten, Erica C., Mautino, Mario R., Liu, Yichin
Médium: Artigo
Jazyk:Inglês
Vydáno: American Chemical Society 2020
On-line přístup:https://ncbi.nlm.nih.gov/pmc/articles/PMC7153281/
https://ncbi.nlm.nih.gov/pubmed/32292562
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acsmedchemlett.0c00004
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