ArticleACS medicinal chemistry letters2015
N (1)-Fluoroalkyltryptophan Analogues: Synthesis and in vitro Study as Potential Substrates for Indoleamine 2,3-Dioxygenase.
Article in ACS medicinal chemistry letters, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers, 1 of them a synthesis that pooled it.
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Who cites it
14 citing papers in PubMed, 1 synthesis or guideline pooled it.
- Fluorine-18-Labeled PET Radiotracers for Imaging Tryptophan Uptake and Metabolism: a Systematic Review.Molecular imaging and biology · 2020Pooled it
- The role of the kynurenine pathway in the pathogenesis of pain and affective disorders after traumatic brain injury.Brain, behavior, & immunity - health · 2026Review
- Improved automated one-pot two-step radiosynthesis of (S)-[EJNMMI radiopharmacy and chemistry · 2024Article
- The First Human Application of an F-18-Labeled Tryptophan Analog for PET Imaging of Cancer.Molecular imaging and biology · 2024Article
- Preparation ofInternational journal of molecular sciences · 2023Article
- Development of [Journal of medicinal chemistry · 2023Article
- Utility of MRI, PET, and ictal SPECT in presurgical evaluation of non-lesional pediatric epilepsy.Seizure · 2020Review
- The therapeutic potential of targeting tryptophan catabolism in cancer.British journal of cancer · 2020Review
- Evaluation of L-1-[Molecular imaging and biology · 2019Article
- Synthesis and evaluation of an AZD2461 [Bioorganic chemistry · 2019Article
- Improved Radiosynthesis and Biological Evaluations of L- and D-1-[Molecular imaging and biology · 2017Article
- Advances in indoleamine 2,3-dioxygenase 1 medicinal chemistry.MedChemComm · 2017Review
- Assessment of Tryptophan Uptake and Kinetics Using 1-(2-18F-Fluoroethyl)-l-Tryptophan and α-11C-Methyl-l-Tryptophan PET Imaging in Mice Implanted with Patient-Derived Brain Tumor Xenografts.Journal of nuclear medicine : official publication, Society of Nuclear Medicine · 2017Article
- Imaging cerebral tryptophan metabolism in brain tumor-associated depression.EJNMMI research · 2015Article
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9 authors.
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Abstract
Indoleamine 2,3-dioxygenase (hIDO) is an enzyme that catalyzes the oxidative cleavage of the indole ring of l-tryptophan through the kynurenine pathway, thereby exerting immunosuppressive properties in inflammatory and tumoral tissues. The syntheses of 1-(2-fluoroethyl)-tryptophan (1-FETrp) and 1-((1-(2-fluoroethyl)-1H-1,2,3-triazol-4-yl)methyl)-tryptophan, two N (1)-fluoroalkylated tryptophan derivatives, are described here. In vitro enzymatic assays with these two new potential substrates of hIDO show that 1-FETrp is a good and specific substrate of hIDO. Therefore, its radioactive isotopomer, 1-[(18)F]FETrp, should be a molecule of choice to visualize tumoral and inflammatory tissues and/or to validate new potential inhibitors.
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