Parallel discovery of selective and dual inhibitors of tryptophan dioxygenases IDO1 and TDO2 with a newly-modified enzymatic assay

Discovery of Clinical Candidate (1R,4r)-4-((R)-2-((S)-6-Fluoro-5H-imidazo[5,1-a]isoindol-5-yl)-1-hydroxyethyl)cyclohexan-1-ol (Navoximod), a Potent and Selective Inhibitor of Indoleamine 2,3-Dioxygenase 1

(2019) Sanjeev Kumar et al.   JOURNAL OF MEDICINAL CHEMISTRY

Epacadostat plus pembrolizumab versus placebo plus pembrolizumab in patients with unresectable or metastatic melanoma (ECHO-301/KEYNOTE-252): a phase 3, randomised, double-blind study

(2019) Georgina V Long et al.   LANCET ONCOLOGY

Discovery and Characterisation of Dual Inhibitors of Tryptophan 2,3-Dioxygenase (TDO2) and Indoleamine 2,3-Dioxygenase 1 (IDO1) Using Virtual Screening

(2019) Suat Sari et al.   MOLECULES

Discovery of Amino-cyclobutarene-derived Indoleamine-2,3-dioxygenase 1 (IDO1) Inhibitors for Cancer Immunotherapy

(2019) Hongjun Zhang et al.   ACS Medicinal Chemistry Letters

In silico and in vitro analysis of small molecules and natural compounds targeting the 3CL protease of feline infectious peritonitis virus

(2019) Sirin Theerawatanasirikul et al.   ANTIVIRAL RESEARCH

Tryptophan 2,3-Dioxygenase Expression Identified in Human Hepatocellular Carcinoma Cells and in Intratumoral Pericytes of Most Cancers

(2019) Delia Hoffmann et al.   Cancer Immunology Research

IDO1 Inhibition Synergizes with Radiation and PD-1 Blockade to Durably Increase Survival Against Advanced Glioblastoma

(2018) Erik Ladomersky et al.   CLINICAL CANCER RESEARCH

Chiral resolution, absolute configuration determination, and stereo-activity relationship study of IDO1 inhibitor NLG919

(2018) Wen-Qiang Liu et al.   TETRAHEDRON

Aminoisoxazoles as Potent Inhibitors of Tryptophan 2,3-Dioxygenase 2 (TDO2)

(2018) Zhonghua Pei et al.   ACS Medicinal Chemistry Letters

Discovery of small molecule WWP2 ubiquitin ligase inhibitors

(2018) Andrew Chantry et al.   CHEMISTRY-A EUROPEAN JOURNAL

Design, synthesis and biological evaluation of novel naphthoquinone derivatives as IDO1 inhibitors

(2018) Liangkun Pan et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Updates in the Clinical Development of Epacadostat and Other Indoleamine 2,3-Dioxygenase 1 Inhibitors (IDO1) for Human Cancers

(2018) Takefumi Komiya et al.   Frontiers in Oncology

Discovery and evaluation of inhibitors to the immunosuppressive enzyme indoleamine 2,3-dioxygenase 1 (IDO1): Probing the active site-inhibitor interactions

(2017) Petr Tomek et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Discovery of a Novel and Selective Indoleamine 2,3-Dioxygenase (IDO-1) Inhibitor 3-(5-Fluoro-1H-indol-3-yl)pyrrolidine-2,5-dione (EOS200271/PF-06840003) and Its Characterization as a Potential Clinical Candidate

(2017) Stefano Crosignani et al.   JOURNAL OF MEDICINAL CHEMISTRY

INCB24360 (Epacadostat), a Highly Potent and Selective Indoleamine-2,3-dioxygenase 1 (IDO1) Inhibitor for Immuno-oncology

(2017) Eddy W. Yue et al.   ACS Medicinal Chemistry Letters

Identification of inhibitors for single-stranded DNA-binding proteins in eubacteria

(2016) Jason G. Glanzer et al.   JOURNAL OF ANTIMICROBIAL CHEMOTHERAPY

Targeting the Inhibition of Tryptophan 2,3-Dioxygenase (TDO-2) for Cancer Treatment

(2016) Ahmed F. Abdel-Magid   ACS Medicinal Chemistry Letters

Establishing Virulence Associated Polyphosphate Kinase 2 as a drug target for Mycobacterium tuberculosis

(2016) Mamta Singh et al.   Scientific Reports

Active Compounds AgainstAnopheles minimusCarboxypeptidase B for Malaria Transmission-Blocking Strategy

(2015) Watcharakorn Mongkol et al.   JOURNAL OF MEDICAL ENTOMOLOGY

Identification of Substituted Naphthotriazolediones as Novel Tryptophan 2,3-Dioxygenase (TDO) Inhibitors through Structure-Based Virtual Screening

(2015) Jian-Sung Wu et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of Novel Inhibitors of HIV-1 Reverse Transcriptase Through Virtual Screening of Experimental and Theoretical Ensembles

(2014) Anthony Ivetac et al.   Chemical Biology & Drug Design

Chemistry: Chemical con artists foil drug discovery

(2014) Jonathan Baell et al.   NATURE

Trial watch

(2014) Erika Vacchelli et al.   OncoImmunology

Formation of an N-formylkynurenine-derived fluorophore and its use for measuring indoleamine 2,3-dioxygenase 1 activity

(2013) Petr Tomek et al.   ANALYTICAL AND BIOANALYTICAL CHEMISTRY

Discovery of Tryptanthrin Derivatives as Potent Inhibitors of Indoleamine 2,3-Dioxygenase with Therapeutic Activity in Lewis Lung Cancer (LLC) Tumor-Bearing Mice

(2013) Shuangshuang Yang et al.   JOURNAL OF MEDICINAL CHEMISTRY

IDO Expression in Brain Tumors Increases the Recruitment of Regulatory T Cells and Negatively Impacts Survival

(2012) D. A. Wainwright et al.   CLINICAL CANCER RESEARCH

Reversal of tumoral immune resistance by inhibition of tryptophan 2,3-dioxygenase

(2012) L. Pilotte et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Indoleamine 2,3 dioxygenase and metabolic control of immune responses

(2012) David H. Munn et al.   TRENDS IN IMMUNOLOGY

IDO inhibits a tryptophan sufficiency signal that stimulates mTOR: A novel IDO effector pathway targeted by D-1-methyl-tryptophan

(2012) Richard Metz et al.   OncoImmunology

Clinicopathological significance of indoleamine 2,3-dioxygenase 1 expression in colorectal cancer

(2011) L Ferdinande et al.   BRITISH JOURNAL OF CANCER

Indoleamine 2,3-dioxygenase, a new prognostic marker in sentinel lymph nodes of melanoma patients

(2011) Reinhart Speeckaert et al.   EUROPEAN JOURNAL OF CANCER

Tryptophan 2,3-Dioxygenase (TDO) Inhibitors. 3-(2-(Pyridyl)ethenyl)indoles as Potential Anticancer Immunomodulators

(2011) Eduard Dolušić et al.   JOURNAL OF MEDICINAL CHEMISTRY

An endogenous tumour-promoting ligand of the human aryl hydrocarbon receptor

(2011) Christiane A. Opitz et al.   NATURE

In Vitro Modulation of Cytochrome P450 Reductase Supported Indoleamine 2,3-Dioxygenase Activity by Allosteric Effectors Cytochromeb5and Methylene Blue

(2010) Josh T. Pearson et al.   BIOCHEMISTRY

Indol-2-yl ethanones as novel indoleamine 2,3-dioxygenase (IDO) inhibitors

(2010) Eduard Dolušić et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Selective inhibition of IDO1 effectively regulates mediators of antitumor immunity

(2010) X. Liu et al.   BLOOD

Rational Design of Indoleamine 2,3-Dioxygenase Inhibitors

(2010) Ute F. Röhrig et al.   JOURNAL OF MEDICINAL CHEMISTRY

New Substructure Filters for Removal of Pan Assay Interference Compounds (PAINS) from Screening Libraries and for Their Exclusion in Bioassays

(2010) Jonathan B. Baell et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of Potent Competitive Inhibitors of Indoleamine 2,3-Dioxygenase with in Vivo Pharmacodynamic Activity and Efficacy in a Mouse Melanoma Model

(2009) Eddy W. Yue et al.   JOURNAL OF MEDICINAL CHEMISTRY

Pharmacogenomic Approach Reveals a Role for the xFormula Cystine/Glutamate Antiporter in Growth and Celastrol Resistance of Glioma Cell Lines

(2009) A.-N. Pham et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

A Kinetic, Spectroscopic, and Redox Study of Human Tryptophan 2,3-Dioxygenase†

(2008) Jaswir Basran et al.   BIOCHEMISTRY

IDO1 and IDO2 are expressed in human tumors: levo- but not dextro-1-methyl tryptophan inhibits tryptophan catabolism

(2008) Stefan Löb et al.   CANCER IMMUNOLOGY IMMUNOTHERAPY

Tryptophan-derived ultraviolet filter compounds covalently bound to lens proteins are photosensitizers of oxidative damage

(2008) Jasminka Mizdrak et al.   FREE RADICAL BIOLOGY AND MEDICINE

Indoleamine 2,3-Dioxygenase Is the Anticancer Target for a Novel Series of Potent Naphthoquinone-Based Inhibitors

(2008) Sanjeev Kumar et al.   JOURNAL OF MEDICINAL CHEMISTRY

Chronic inflammation that facilitates tumor progression creates local immune suppression by inducing indoleamine 2,3 dioxygenase

(2008) A. J. Muller et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA