A Series of 2‐((1‐Phenyl‐1H‐imidazol‐5‐yl)methyl)‐1H‐indoles as Indoleamine 2,3‐Dioxygenase 1 (IDO1) Inhibitors
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DOI: 10.1002/cmdc.202100107
Abstract: Indoleamine 2,3‐dioxygenase 1 (IDO1) is a promising therapeutic target in cancer immunotherapy and neurological disease. Thus, searching for highly active inhibitors for use in human cancers is now a focus of widespread research and development… read more here.
Keywords: brain penetrant; dioxygenase ido1; ido1 inhibitors; indoleamine dioxygenase ... See more keywords
Discovery and evaluation of inhibitors to the immunosuppressive enzyme indoleamine 2,3-dioxygenase 1 (IDO1): Probing the active site-inhibitor interactions.
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DOI: 10.1016/j.ejmech.2016.12.029
Abstract: High expression of the immunosuppressive enzyme, indoleamine 2,3-dioxygenase 1 (IDO1) for a broad range of malignancies is associated with poor patient prognosis, and the enzyme is a validated target for cancer intervention. To identify novel… read more here.
Keywords: ido1; enzyme indoleamine; dioxygenase ido1; ido1 inhibitors ... See more keywords
Indoleamine 2,3‐dioxygenase 1 (IDO1) inhibitors activate the aryl hydrocarbon receptor
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DOI: 10.1016/j.taap.2017.03.012
Abstract: ABSTRACT Indoleamine 2,3‐dioxygenase 1 (IDO1) plays a key role in the immune system by regulating tryptophan levels and T cell differentiation. Several tumor types overexpress IDO1 to avoid immune surveillance making IDO1 of interest as… read more here.
Keywords: ido1; aryl hydrocarbon; indoleamine dioxygenase; ido1 inhibitors ... See more keywords
Structure and Plasticity of Indoleamine 2,3-Dioxygenase 1 (IDO1).
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DOI: 10.1021/acs.jmedchem.1c01665
Abstract: Since the discovery of the implication of indoleamine 2,3-dioxygenase 1 (IDO1) in tumoral immune resistance in 2003, the search for inhibitors has been intensely pursued both in academia and in pharmaceutical companies, supported by the… read more here.
Keywords: indoleamine dioxygenase; dioxygenase ido1; ido1; ido1 structure ... See more keywords
Structure-based optimization of type III indoleamine 2,3-dioxygenase 1 (IDO1) inhibitors
Sign Up to like & getrecommendations! Published in 2022 at "Journal of Enzyme Inhibition and Medicinal Chemistry"
DOI: 10.1080/14756366.2022.2089665
Abstract: Abstract 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… read more here.
Keywords: indoleamine dioxygenase; based optimization; ido1 inhibitors; dioxygenase ido1 ... See more keywords
Discovery and Characterisation of Dual Inhibitors of Tryptophan 2,3-Dioxygenase (TDO2) and Indoleamine 2,3-Dioxygenase 1 (IDO1) Using Virtual Screening
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DOI: 10.3390/molecules24234346
Abstract: Cancers express tryptophan catabolising enzymes indoleamine 2,3-dioxygenase 1 (IDO1) and tryptophan 2,3-dioxygenase (TDO2) to produce immunosuppressive tryptophan metabolites that undermine patients’ immune systems, leading to poor disease outcomes. Both enzymes are validated targets for cancer… read more here.
Keywords: ido1; tdo2; dioxygenase ido1; indoleamine dioxygenase ... See more keywords