1065608-70-9Relevant academic research and scientific papers
Implementation of the CYP Index for the Design of Selective Tryptophan-2,3-dioxygenase Inhibitors
Castanedo, Georgette M.,Dement, Kevin,Dipasquale, Antonio,Gazzard, Lewis,Goon, Leanne,Gustafson, Amy,Harris, Seth F.,Jaipuri, Firoz A.,Kumar, Sanjeev,La, Hank,Li, Xiaokai,Liu, Wen,Liu, Yichin,Mautino, Mario R.,Mendonca, Rohan,Oh, Angela J.,Parr, Brendan T.,Pastor, Richard,Pavana, Roheeth K.,Pei, Zhonghua,Potturi, Hima,Sellers, Benjamin D.,Shao, Cheng,Vanderporten, Erica C.,Velvadapu, Venkata,Waldo, Jesse P.,Wu, Guosheng,Yuen, Po-Wai,Zhang, Yamin,Zhang, Zuhui
, p. 541 - 549 (2020/04/30)
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 evaluation of TDO as a potential cancer immunotherapy target. As means of mitigating the risk of drug-drug interactions arising from cytochrome P450 inhibition, a novel property-based drug design parameter, herein referred to as the CYP Index, was implemented for the design of inhibitors with appreciable selectivity for TDO over CYP3A4. We anticipate the CYP Index will be a valuable design parameter for optimizing CYP inhibition of any small molecule inhibitor containing a Lewis basic motif capable of binding heme.
TDO2 INHIBITORS
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, (2017/07/14)
Presently provided are inhibitors of cellularly expressed TDO2 and pharmaceutical compositions thereof, useful for modulating an activity of tryptophan 2, 3 dioxygenase; treating immunosuppression; treating a medical conditions that benefit from the inhibition of tryptophan degradation; enhancing the effectiveness of an anti-cancer treatment comprising administering an anti-cancer agent; and treating tumor-specific immunosuppression associated with cancer.
2-AMINOPYRIDINE ANALOGS AS GLUCOKINASE ACTIVATORS
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, (2008/12/04)
Provided are compounds that are useful in the treatment and/or prevention of diseases mediated by deficient levels of glucokinase activity, such as diabetes mellitus. Also provided are methods of treating or preventing diseases and disorders characterized by underactivity of glucokinase or which can be treated by activating glucokinase.
1,2,4-Triazolo[4,3-a]pyridines
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, (2008/06/13)
There are disclosed herein certain 1,2,4-triazolo-[4,3-a]pyridine compounds which are useful in the treatment of peptic ulcer diseases.
1,3,4-Triazolo[1,5-a]pyridines
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, (2008/06/13)
There are disclosed herein certain 1,3,4-triazolo[1,5-a]pyridine compounds which are useful in the treatment of peptic ulcer diseases.
