A Series of 2‐((1‐Phenyl‐1H‐imidazol‐5‐yl)methyl)‐1H‐indoles as Indoleamine 2,3‐Dioxygenase 1 (IDO1) Inhibitors
Sign Up to like & getrecommendations! Published in 2021 at "ChemMedChem"
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
The ups, downs and new trends of IDO1 inhibitors.
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DOI: 10.1016/j.bioorg.2021.104815
Abstract: Cancer immunotherapy has become an emerging driving force in the development of innovative strategies to fight against cancer. Despite the significant clinical benefits that many cancer patients have gained, the generally average response rate of ~ 20%… read more here.
Keywords: new trends; downs new; ups downs; ido1 inhibitors ... See more keywords
Discovery and evaluation of inhibitors to the immunosuppressive enzyme indoleamine 2,3-dioxygenase 1 (IDO1): Probing the active site-inhibitor interactions.
Sign Up to like & getrecommendations! Published in 2017 at "European journal of medicinal chemistry"
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
Discovery of potent IDO1 inhibitors derived from tryptophan using scaffold-hopping and structure-based design approaches.
Sign Up to like & getrecommendations! Published in 2017 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2017.06.039
Abstract: Indoleamine 2,3-dioxygenase 1 (IDO1) is frequently hijacked by tumors to escape the host immune response, and the enzyme is now firmly established as an attractive target for cancer immunotherapy. To identify novel IDO1 inhibitors suitable… read more here.
Keywords: discovery potent; scaffold hopping; potent ido1; ido1 inhibitors ... See more keywords
Indoleamine 2,3‐dioxygenase 1 (IDO1) inhibitors activate the aryl hydrocarbon receptor
Sign Up to like & getrecommendations! Published in 2017 at "Toxicology and Applied Pharmacology"
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
Discovery of Carbono(di)thioates as Indoleamine 2,3-Dioxygenase 1 Inhibitors.
Sign Up to like & getrecommendations! Published in 2021 at "ACS medicinal chemistry letters"
DOI: 10.1021/acsmedchemlett.0c00527
Abstract: A structure-activity relationship study unexpectedly showed that carbonothioates 4a and 4b, obtained by a unique alkaline hydrolysis of 2-alkylthio-oxazolines 3a and 3b, respectively, are a novel scaffold for indoleamine 2,3-dioxygenase 1 (IDO1) inhibitors. Derivatization of… read more here.
Keywords: carbono thioates; thioates indoleamine; discovery carbono; dioxygenase ... 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
Advances in the discovery and development of selective heme-displacing IDO1 inhibitors
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DOI: 10.1080/17460441.2020.1781811
Abstract: ABSTRACT Introduction Indoleamine 2,3-dioxygenase 1 (IDO1) has been considered as an attractive intracellular target for the development of small-molecule cancer immunotherapy. Results in human clinical studies indicated that the first-generation IDO1 inhibitor epacadostat lacked anticancer… read more here.
Keywords: heme; heme displacing; displacing ido1; ido1 inhibitors ... See more keywords
Abstract B060: Side-by-side comparison of small molecule IDO1 inhibitors in biochemical and cell-based assays and development of aIDO1-expressing mouse model to evaluate target modulation
Sign Up to like & getrecommendations! Published in 2019 at "Molecular Cancer Therapeutics"
DOI: 10.1158/1535-7163.targ-19-b060
Abstract: Introduction: Indoleamine 2,3-dioxygenase (IDO1) is a heme-containing oxidoreductase enzyme that converts L-tryptophan (Trp) into N’-formylkynurenine (NFK). IDO1 is broadly expressed by tumor cells as well as immune cells in the tumor microenvironment of many cancers,… read more here.
Keywords: target modulation; ido1 inhibitors; model; cell ... See more keywords
Immune Suppression in CLL Is Mediated By the L-Amino Acid Oxidase IL4I1, a Reason for the Treatment Failure of IDO1 Inhibitors
Sign Up to like & getrecommendations! Published in 2020 at "Blood"
DOI: 10.1182/blood-2020-141317
Abstract: A better understanding of cancer-induced immune suppression has led to the development of novel immunotherapy approaches, some of which are considered as breakthrough in cancer treatment. One of the promising targets that was followed in… read more here.
Keywords: mice; ido1 inhibitors; cancer; cll ... See more keywords
Indoleamine 2, 3-dioxygenase 1 inhibitory compounds from natural sources
Sign Up to like & getrecommendations! Published in 2022 at "Frontiers in Pharmacology"
DOI: 10.3389/fphar.2022.1046818
Abstract: L-tryptophan metabolism is involved in the regulation of many important physiological processes, such as, immune response, inflammation, and neuronal function. Indoleamine 2, 3-dioxygenase 1 (IDO1) is a key enzyme that catalyzes the first rate-limiting step… read more here.
Keywords: inhibitory activity; inhibitory; indoleamine dioxygenase; ido1 inhibitors ... See more keywords