Results 11 to 20 of about 618,162 (164)

Utilization of Metabolite Identification and Structural Data to Guide Design of Low-Dose IDO1 Inhibitors [PDF]

ACS Medicinal Chemistry Letters, 2021
Herein the discovery of potent IDO1 inhibitors with low predicted human dose is discussed. Metabolite identification (MetID) and structural data were used to strategically incorporate cyclopropane rings into this tetrahydronaphthyridine series of IDO1 ...
Ian Knemeyer, Charles Lesburg, Hua Zhou   +2 more
exaly   +3 more sources

Updates in the Clinical Development of Epacadostat and Other Indoleamine 2,3-Dioxygenase 1 Inhibitors (IDO1) for Human Cancers [PDF]

Frontiers in Oncology, 2018
Recent application of immunotherapy in clinical oncology revolutionized our management of advanced human cancers. Check point inhibitors targeting CTLA4 and PD-1/PD-L1 axis are immunotherapeutic agents currently available to treat a variety of cancers ...
Takefumi Komiya, Chao H. Huang, Chao H. Huang   +2 more
doaj   +4 more sources

Evaluation of Novel Inhibitors of Tryptophan Dioxygenases for Enzyme and Species Selectivity Using Engineered Tumour Cell Lines Expressing Either Murine or Human IDO1 or TDO2

Pharmaceuticals, 2022
Indoleamine 2, 3-dioxygenase 1 (IDO1) is commonly expressed by cancers as a mechanism for evading the immune system. Preclinical and clinical studies have indicated the potential of combining IDO1 inhibitors with immune therapies for the treatment of ...
Sofian M Tijono, Brian D. Palmer, Petr Tomek, Jack U. Flanagan, Kimiora Henare, Swarna Gamage, Lukas Braun, Lai-Ming Ching   +7 more
doaj   +2 more sources

Adverse pro-tumorigenic effects of IDO1 catalytic inhibitors mediated by the non-enzymatic function of IDO1 in tumor cells

Frontiers in Immunology
Indoleamine 2,3-dioxygenase 1 (IDO1) inhibitors have been developed with the aim of reinvigorating antitumor T-cell responses in the tumor microenvironment by blocking the conversion of the essential amino acid tryptophan into immunoregulatory ...
Sofia Rossini, Sara Ambrosino, Claudia Volpi, Chiara Suvieri, Maria Teresa Pallotta, Maria Laura Belladonna, Daniele Sorcini, Antonio Macchiarulo, Elisabeth Hennes, Slava Ziegler, Herbert Waldmann, Ciriana Orabona   +11 more
doaj   +2 more sources

A Novel IDO1/NE Dual Inhibitor, IMM-H018 Prevents the Primary and Secondary Sepsis and Ameliorates the Kidney Injury Through Inhibiting the Cytokine Storm and Microthrombosis, and Reversing Immunosuppression. [PDF]

Adv Sci (Weinh)
IMM‐H018, a dual IDO1/NE inhibitor, demonstrates potent therapeutic efficacy in sepsis by simultaneously targeting excessive inflammation and immune dysfunction. It prevents both primary and secondary sepsis through anti‐inflammatory, immune‐restoring, and renoprotective mechanisms, reducing organ damage, improving immune homeostasis, preserving kidney
Zhou Y, Zhao X, Pan X, Ma Z, Cui H, Wen H, Wang P, Liao X, Qin K, Wang Y, Sheng L, Zhang S.   +11 more
europepmc   +2 more sources

Discovery of cyanopyridine scaffold as novel indoleamine-2,3-dioxygenase 1 (IDO1) inhibitors through virtual screening and preliminary hit optimisation [PDF]

Journal of Enzyme Inhibition and Medicinal Chemistry, 2019
With the aim of discovering novel IDO1 inhibitors, a combined similarity search and molecular docking approach was employed to the discovery of 32 hit compounds.
Xi Xu, Jie Ren, Yinghe Ma, Hongting Liu, Quanjin Rong, Yifan Feng, Yameng Wang, Yu Cheng, Ruijia Ge, Zhiyu Li, Jinlei Bian   +10 more
doaj   +2 more sources

Tryptophan metabolism in colorectal cancer: From mechanistic insights to novel therapeutic strategies. [PDF]

Clin Transl Med
Tryptophan metabolism modulates CRC via three microbiota‐regulated pathways with distinct dual‐mode effects. The kynurenine pathway provides biomarkers, serotonin pathway supports SSRI‐combined immunotherapy, indole pathway yields immunostimulatory metabolites, collectively offering translational prospects.
Wang R, Shen W, Yang P, Yang D, Cao Y, Zhou Y.   +5 more
europepmc   +2 more sources

Discovery of 1‑(Hetero)aryl-β-carboline Derivatives as IDO1/TDO Dual Inhibitors with Antidepressant Activity

, 2022
Depression is the leading cause of global burden of disease and disability. Abnormalities in the kynurenine pathway of tryptophan degradation have been closely linked to the pathogenesis of depression.
Yingchun Li (636496), Ruxin Gu (13211490), Dongyin Chen (13211493), Yu Zhang (12946), Xu Dong (366886), Feng Han (10919), Guoli Wang (59357), Chao Chen (195669), Xiang Chen (10398), Xuan Chen (158617), Li Wang (15202), Fei Li (143236)   +11 more
core   +8 more sources

Synthesis, activity exploration, molecular docking, and affinity assessment of theophylline derivatives as inhibitors targeting IDO1

Heterocyclic Communications
Indoleamine 2,3-dioxygenase 1 (IDO1) is an immunomodulatory enzyme associated with tumor immune evasion, making it a promising target for cancer therapy. This study aimed to identify novel holo-IDO1 inhibitors with distinct structural scaffolds. A series
Wu Ziyuan, Liang Songmao, Hu Shunhua, Wang Yimian, Mao Long-Fei, Hou Xixi, Yang Jianxue   +6 more
doaj   +2 more sources

Structure-based optimization of type III indoleamine 2,3-dioxygenase 1 (IDO1) inhibitors. [PDF]

J Enzyme Inhib Med Chem, 2022
The haem enzyme indoleamine 2,3-dioxygenase 1 (IDO1) catalyses the rate-limiting step in the kynurenine pathway of tryptophan metabolism and plays an essential role in immunity, neuronal function, and ageing. Expression of IDO1 in cancer cells results in
Röhrig UF, Majjigapu SR, Vogel P, Reynaud A, Pojer F, Dilek N, Reichenbach P, Ascenção K, Irving M, Coukos G, Michielin O, Zoete V.   +11 more
europepmc   +3 more sources