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10.1080/14756366.2018.1471688

http://scihub22266oqcxt.onion/10.1080/14756366.2018.1471688
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C6022239!6022239!29932010
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suck abstract from ncbi


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pmid29932010      J+Enzyme+Inhib+Med+Chem 2018 ; 33 (1): 1089-94
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  • A highly potent and selective inhibitor Roxyl-WL targeting IDO1 promotes immune response against melanoma #MMPMID29932010
  • Xu G; Wang T; Li Y; Huang Z; Wang X; Zheng J; Yang S; Fan Y; Xiang R
  • J Enzyme Inhib Med Chem 2018[]; 33 (1): 1089-94 PMID29932010show ga
  • Indoleamine 2,3-dioxygenase 1 (IDO1) activity links to immune escape of cancers. Inhibition of IDO1 provides a new approach for cancer treatment. Most clinical IDO1 drugs show marginal efficacy as single agents. On basis of molecular docking and pharmacophore modelling, a novel inhibitor Roxyl-WL was discovered with a half maximal inhibitory concentration (IC50) value of 1?nM against IDO1 and 10?100-fold increased potent activity compared with IDO1 drugs in clinical trials. Roxyl-WL displayed excellent kinase spectrum selectivity with no activity out of the 337 protein kinases. In vitro, Roxyl-WL effectively augmented the proliferation of T cells and reduced the number of regulatory T cell (Tregs).When administered to melanoma (B16F10) tumor-bearing mice orally, Roxyl-WL significantly suppressed tumor growth and induced immune response.
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