Development of a mass spectrometry-based tryptophan 2, 3-dioxygenase assay using liver cytosol from multiple species.
Sign Up to like & getrecommendations! Published in 2018 at "Analytical biochemistry"
DOI: 10.1016/j.ab.2018.06.025
Abstract: A novel and rapid method to determine the potency of inhibitors for tryptophan 2, 3-dioxygenase (TDO2) activities in human and preclinical species was successfully developed and validated utilizing LC-MS/MS. Previously reported TDO2 activity assays are… read more here.
Keywords: tdo2; liver cytosol; development mass; multiple species ... See more keywords
Microtubule inhibitors containing immunostimulatory agents promote cancer immunochemotherapy by inhibiting tubulin polymerization and tryptophan-2,3-dioxygenase.
Sign Up to like & getrecommendations! Published in 2019 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2019.111949
Abstract: A combination therapeutic regimen via introducing tryptophan 2,3-dioxygenase inhibitors into microtubule inhibitors was performed and evaluated for their antitumor activity. Thereinto, HT2, composed of combretastatin A-4 (CA-4) and tryptophan-2,3-dioxygenase (TDO) inhibitor by a linker, displayed… read more here.
Keywords: microtubule inhibitors; tubulin polymerization; tryptophan dioxygenase; cancer ... See more keywords
Rational Design of Original Fused-Cycle Selective Inhibitors of Tryptophan 2,3-Dioxygenase.
Sign Up to like & getrecommendations! Published in 2021 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.1c00323
Abstract: Tryptophan 2,3-dioxygenase (TDO2) is a heme-containing enzyme constitutively expressed at high concentrations in the liver and responsible for l-tryptophan (l-Trp) homeostasis. Expression of TDO2 in cancer cells results in the inhibition of immune-mediated tumor rejection… read more here.
Keywords: fused cycle; design original; rational design; tryptophan dioxygenase ... See more keywords
Implementation of the CYP Index for the Design of Selective Tryptophan-2,3-dioxygenase Inhibitors.
Sign Up to like & getrecommendations! Published in 2020 at "ACS medicinal chemistry letters"
DOI: 10.1021/acsmedchemlett.0c00004
Abstract: A class of imidazoisoindole (III) heme-binding indoleamine-2,3-dioxygenase (IDO1) inhibitors were optimized via structure-based drug design into a series of tryptophan-2,3-dioxygenase (TDO)-selective inhibitors. Kynurenine pathway modulation was demonstrated in vivo, which enabled evaluation of TDO as… read more here.
Keywords: cyp index; drug; tryptophan dioxygenase; design ... See more keywords
Current state on tryptophan 2,3-dioxygenase inhibitors: a patent review
Sign Up to like & getrecommendations! Published in 2019 at "Expert Opinion on Therapeutic Patents"
DOI: 10.1080/13543776.2019.1556638
Abstract: ABSTRACT Introduction: Tryptophan-2, 3-dioxygenase (TDO2) is a tryptophan-degrading enzyme constitutively expressed in the liver and to a lesser extend in the brain. Before its link to cancer immunotherapy was discovered in 2011, the search for… read more here.
Keywords: dioxygenase inhibitors; current state; state tryptophan; tryptophan dioxygenase ... See more keywords
Synthetic Essentiality of Tryptophan 2,3-dioxygenase 2 in APC-Mutated Colorectal Cancer.
Sign Up to like & getrecommendations! Published in 2022 at "Cancer discovery"
DOI: 10.1158/2159-8290.cd-21-0680
Abstract: Inactivation of the adenomatous polyposis coli (APC) is common across many cancer types and serves as a critical initiating event in most sporadic colorectal cancers (CRC). APC-deficiency activates WNT signaling which remains an elusive target… read more here.
Keywords: tdo2; synthetic essentiality; cancer; tryptophan dioxygenase ... See more keywords
Targeting Indoleamine Dioxygenase and Tryptophan Dioxygenase in Cancer Immunotherapy: Clinical Progress and Challenges
Sign Up to like & getrecommendations! Published in 2022 at "Drug Design, Development and Therapy"
DOI: 10.2147/dddt.s373780
Abstract: Abstract Indoleamine 2.3-dioxygenases (IDO1/2) and tryptophan 2.3-dioxygenase (TDO) are the initial and rate-limiting enzymes in tryptophan metabolism, which play an essential role in mediating immunosuppression in tumor microenvironment. Accumulating evidence has indicated that both IDO1… read more here.
Keywords: progress; dioxygenase; ido1 tdo; cancer ... See more keywords
The Tobacco β-Cembrenediol: A Prostate Cancer Recurrence Suppressor Lead and Prospective Scaffold via Modulation of Indoleamine 2,3-Dioxygenase and Tryptophan Dioxygenase
Sign Up to like & getrecommendations! Published in 2022 at "Nutrients"
DOI: 10.3390/nu14071505
Abstract: Prostate cancer (PC) is the second leading cause of death in men in the US. PC has a high recurrence rate, and limited therapeutic options are available to prevent disease recurrence. The tryptophan-degrading enzymes 2,3-indoleamine… read more here.
Keywords: prostate cancer; cbt; recurrence; indoleamine dioxygenase ... See more keywords
Dexamethasone Induces the Expression and Function of Tryptophan-2-3-Dioxygenase in SK-MEL-28 Melanoma Cells
Sign Up to like & getrecommendations! Published in 2021 at "Pharmaceuticals"
DOI: 10.3390/ph14030211
Abstract: Tryptophan-2,3-dioxygenase (TDO) is one of the key tryptophan-catabolizing enzymes with immunoregulatory properties in cancer. Contrary to expectation, clinical trials showed that inhibitors of the ubiquitously expressed enzyme, indoleamine-2,3-dioxygenase-1 (IDO1), do not provide benefits in melanoma… read more here.
Keywords: melanoma; mel melanoma; melanoma cells; expression ... See more keywords