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MOLECULAR CANCER THERAPEUTICS, ISSN 1535-7163, 12/2018, Volume 17, Issue 12, pp. 2530 - 2542
Tumors use indoleamine 2,3-dioxygenase-1 (IDO1) as a major mechanism to induce an immunosuppressive microenvironment. IDO1 expression is upregulated in many... 
T-CELL PROLIFERATION | DENDRITIC CELLS | ONCOLOGY | ARYL-HYDROCARBON RECEPTOR | IMMUNOTHERAPY | INDOLEAMINE 2,3-DIOXYGENASE | TUMORAL IMMUNE RESISTANCE | TRYPTOPHAN DEGRADATION | SUPPRESSION | CANCER | EXPRESSION
Journal Article
ACS MEDICINAL CHEMISTRY LETTERS, ISSN 1948-5875, 05/2017, Volume 8, Issue 5, pp. 486 - 491
A data-centric medicinal chemistry approach led to the invention of a potent and selective IDO1 inhibitor 41, INCB24360 (epacadostat). The molecular structure... 
TARGET | CHEMISTRY, MEDICINAL | INDOLEAMINE 2,3-DIOXYGENASE | DRUG DISCOVERY | Epacadostat | data-centric medicinal chemistry | TRYPTOPHAN CATABOLISM | COMBINATIONS | METABOLISM | IDO | immuno-oncology | ANTITUMOR IMMUNITY | TUMORAL IMMUNE RESISTANCE | INCB24360 | IPILIMUMAB | IDO1
Journal Article
Journal of the American Chemical Society, ISSN 0002-7863, 08/2017, Volume 139, Issue 34, pp. 11887 - 11894
3-Substituted 2-oxindoles are important structural motifs found in many biologically active natural products and pharmaceutical lead compounds. Here, we report... 
ENANTIOSELECTIVE SYNTHESIS | MECHANISM | 2ND ENZYME | CRYSTAL-STRUCTURE | INDOLEAMINE 2,3-DIOXYGENASE | PYRROLNITRIN BIOSYNTHETIC-PATHWAY | TUMORAL IMMUNE RESISTANCE | CHEMISTRY, MULTIDISCIPLINARY | SUBSTRATE RECOGNITION | SPIROOXINDOLES | INSIGHTS
Journal Article
Journal of the American Chemical Society, ISSN 0002-7863, 07/2018, Volume 140, Issue 27, pp. 8518 - 8525
Human indoleamine 2,3-dioxygenase 1 (hIDO1) and tryptophan dioxygenase (hTDO) catalyze the same dioxygenation reaction of Trp to generate N-formyl kynurenine... 
REFINEMENT | SUBSTRATE-BINDING | METABOLISM | TOLERANCE | DISEASE | TRYPTOPHAN 2,3-DIOXYGENASE | TUMORAL IMMUNE RESISTANCE | EXPRESSION | CHEMISTRY, MULTIDISCIPLINARY | DISCOVERY | IDO1 INHIBITORS
Journal Article
NATURE REVIEWS DRUG DISCOVERY, ISSN 1474-1776, 05/2019, Volume 18, Issue 5, pp. 379 - 401
L-Tryptophan (Trp) metabolism through the kynurenine pathway (KP) is involved in the regulation of immunity, neuronal function and intestinal homeostasis.... 
QUINOLINIC ACID | DENDRITIC CELLS | ARYL-HYDROCARBON RECEPTOR | BIOTECHNOLOGY & APPLIED MICROBIOLOGY | XANTHURENIC ACID | REGULATORY T-CELLS | KYNURENINE-AMINOTRANSFERASE-II | LEVO-1-METHYL TRYPTOPHAN | PHARMACOLOGY & PHARMACY | PATHWAY METABOLISM | TUMORAL IMMUNE RESISTANCE | INDOLEAMINE 2,3-DIOXYGENASE ACTIVITY
Journal Article