Results 51 to 60 of about 29,794,370 (246)

Janus Reactivity of a Mononuclear Non‐Heme Iron(III)‐Peroxo Complex Toward Indole Oxidation

open access: yesAngewandte Chemie, EarlyView.
The iron(III)‐peroxo complex [FeIII(O2)(12‐TMC)]+ exhibits bifurcating pathways in indole oxidation. N─H indoles undergo N─H H‐atom abstraction, supported by a KIE of 5.2 for N─H/N–D 2,3‐dimethylindoles, whereas N‐methylindoles react via electrophilic addition of the iron‐peroxo group to the C2–C3 double bond of the indole ring, forming iron ...
Wenjuan Zhu   +4 more
wiley   +2 more sources

Diverse chemical space of indoleamine-2,3-dioxygenase 1 (Ido1) inhibitors

open access: yesEuropean Journal of Medicinal Chemistry, 2021
Indoleamine-2,3-dioxygenase 1 (IDO1) catalyses the first and rate limiting step of kynurenine pathway accounting for the major contributor of L-Tryptophan degradation. The Kynurenine metabolites are identified as essential cofactors, antagonists, neurotoxins, immunomodulators, antioxidants as well as carcinogens.
Singh, Rahul, Salunke, Deepak B.
openaire   +2 more sources

Structural insights into substrate and inhibitor binding sites in human indoleamine 2,3-dioxygenase 1

open access: yesNature Communications, 2017
Human indoleamine 2,3-dioxygenase 1 (hIDO1) is an immunotherapeutic target for cancer therapy. Here, the authors present the substrate-, inhibitor- and effector-bound hIDO1 crystal structures, which give insights into the mechanism and reveal a second ...
Ariel Lewis-Ballester   +6 more
doaj   +1 more source

In vivo metabolism of tryptophan in meningiomas is mediated by indoleamine 2,3-dioxygenase 1 [PDF]

open access: yesCancer Biology & Therapy, 2013
Expression and activity of indoleamine 2,3-dioxygenase (IDO), the first and rate-limiting step of the kynurenine pathway of tryptophan catabolism, can enable tumor cells to effectively evade the host's immune response. The potential role of this system was investigated in meningiomas.
Ian M, Zitron   +4 more
openaire   +2 more sources

Discovery of Carbono(di)thioates as Indoleamine 2,3-Dioxygenase 1 Inhibitors

open access: yesACS Medicinal Chemistry Letters, 2021
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.
Miyuki Kumazawa   +13 more
openaire   +4 more sources

HIV-Induced Type I Interferon and Tryptophan Catabolism Drive T Cell Dysfunction Despite Phenotypic Activation [PDF]

open access: yes, 2008
10.03.14 KB.
Shearer, GM   +14 more
core   +1 more source

Synthesis, Docking and Biological Evaluation of a Novel Class of Imidazothiazoles as IDO1 Inhibitors

open access: yesMolecules, 2019
IDO1, a key dioxygenase in tryptophan-kynurenine metabolism, appeared in the last 10 years at the vanguard of druggable targets in cancer therapy due to its well-established role both in immune escape and inflammatory neovascularization.
Marta Serafini   +5 more
doaj   +1 more source

Reliable chromatographic assay for measuring of indoleamine 2,3-dioxygenase 1 (IDO1) activity in human cancer cells

open access: yesJournal of Enzyme Inhibition and Medicinal Chemistry, 2021
The kynurenine pathway is the major tryptophan degradation routes generating bioactive compounds important in physiology and diseases. Depending on cell type it is initiated enzymatically by tryptophan-2,3-dioxygenase (TDO) or indoleamine-2,3-dioxygenase
Ilona Sadok   +3 more
doaj   +1 more source

Indoleamine 2,3-Dioxygenase as a Therapeutic Target for Alzheimer’s Disease and Geriatric Depression

open access: yesBrain Sciences, 2023
Neuroimmune-triggered neuroinflammation of the central nervous system is emerging as an important aetiopathogenic factor for multiple neurological disorders, including depression, dementia, Alzheimer’s disease, multiple sclerosis and others.
Karl Savonije   +2 more
doaj   +1 more source

Engineering Approaches to Modify Immunomodulatory Functions of Mesenchymal Stromal Cells (MSCs): Tissue Regeneration and Clinical Application

open access: yesAdvanced Science, EarlyView.
Mesenchymal stromal cells (MSCs) show promise for treating immune‐related disorders through immunomodulation and tissue regeneration. This review gives a brief overview of current clinical approval of MSC therapies. It also discussed how bioengineering, including genetic modification, biomaterial delivery, extracellular vesicles, and iPSC‐derived MSCs,
Sichen Yang   +6 more
wiley   +1 more source

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