Heme-containing enzymes and inhibitors for tryptophan metabolism

Epacadostat plus pembrolizumab in patients with advanced melanoma and select solid tumors: Updated phase 1 results from ECHO-202/KEYNOTE-037

(2016) T.C. Gangadhar et al.   ANNALS OF ONCOLOGY

Analysis of Reaction Intermediates in Tryptophan 2,3-Dioxygenase: A Comparison with Indoleamine 2,3-Dioxygenase

(2016) Jaswir Basran et al.   BIOCHEMISTRY

Discovery and preliminary structure–activity relationship of 1H-indazoles with promising indoleamine-2,3-dioxygenase 1 (IDO1) inhibition properties

(2016) Shan Qian et al.   BIOORGANIC & MEDICINAL CHEMISTRY

1,2,3-Triazoles as inhibitors of indoleamine 2,3-dioxygenase 2 (IDO2)

(2016) Ute F. Röhrig et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Novel substituted hydrazono indolo[2,1- b ]quinazoline-6,12-dione analogues as cytostatic agents: Synthesis, crystal structure, biological evaluation and molecular docking studies

(2016) Ramu Guda et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Discovery of a Novel Scaffold as an Indoleamine 2,3-Dioxygenase 1 (IDO1) Inhibitor Based on the Pyrrolopiperazinone Alkaloid, Longamide B

(2016) Zenyu Shiokawa et al.   ChemMedChem

O-alkylhydroxylamines as rationally-designed mechanism-based inhibitors of indoleamine 2,3-dioxygenase-1

(2016) William P. Malachowski et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Establishment of a human indoleamine 2, 3-dioxygenase 2 (hIDO2) bioassay system and discovery of tryptanthrin derivatives as potent hIDO2 inhibitors

(2016) Juanjuan Li et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Nitrobenzofurazan derivatives of N ′ - hydroxyamidines as potent inhibitors of indoleamine-2,3-dioxygenase 1

(2016) Saurav Paul et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Potential Underprediction of Warfarin Drug Interaction From Conventional Interaction Studies and Risk Mitigation: A Case Study With Epacadostat, an IDO1 Inhibitor

(2016) Jack G. Shi et al.   JOURNAL OF CLINICAL PHARMACOLOGY

Population Pharmacokinetic and Pharmacodynamic Modeling of Epacadostat in Patients With Advanced Solid Malignancies

(2016) Jack G. Shi et al.   JOURNAL OF CLINICAL PHARMACOLOGY

Insights into the mechanism of inhibition of tryptophan 2,3-dioxygenase by isatin derivatives

(2016) Georgios Pantouris et al.   JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY

New Inhibitors of Indoleamine 2,3-Dioxygenase 1: Molecular Modeling Studies, Synthesis, and Biological Evaluation

(2016) Antonio Coluccia et al.   JOURNAL OF MEDICINAL CHEMISTRY

In silico-driven multicomponent synthesis of 4,5- and 1,5-disubstituted imidazoles as indoleamine 2,3-dioxygenase inhibitors

(2016) S. Fallarini et al.   MedChemComm

Fused Heterocyclic Compounds as Potent Indoleamine-2,3-dioxygenase 1 Inhibitors

(2016) Subhankar Panda et al.   ACS Medicinal Chemistry Letters

Benzo[b]quinolizinium Derivatives Have a Strong Antimalarial Activity and Inhibit Indoleamine Dioxygenase

(2015) Esther Jortzik et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Carborane-Containing Hydroxyamidine Scaffolds as Novel Inhibitors of Indoleamine 2,3-Dioxygenase 1 (IDO1)

(2015) Christopher J. D. Austin et al.   AUSTRALIAN JOURNAL OF CHEMISTRY

Molecular Pathways: Targeting IDO1 and Other Tryptophan Dioxygenases for Cancer Immunotherapy

(2015) L. Zhai et al.   CLINICAL CANCER RESEARCH

Role of indoleamine 2,3-dioxygenase in health and disease

(2015) Amanda W.S. Yeung et al.   CLINICAL SCIENCE

Targeting key dioxygenases in tryptophan–kynurenine metabolism for immunomodulation and cancer chemotherapy

(2015) Christopher J.D. Austin et al.   DRUG DISCOVERY TODAY

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

Phenyl Benzenesulfonylhydrazides Exhibit Selective Indoleamine 2,3-Dioxygenase Inhibition with Potent in Vivo Pharmacodynamic Activity and Antitumor Efficacy

(2015) Shu-Yu Lin et al.   JOURNAL OF MEDICINAL CHEMISTRY

Challenges and Opportunities in the Discovery of New Therapeutics Targeting the Kynurenine Pathway

(2015) Amy B. Dounay et al.   JOURNAL OF MEDICINAL CHEMISTRY

Challenges in the Discovery of Indoleamine 2,3-Dioxygenase 1 (IDO1) Inhibitors

(2015) Ute F. Röhrig et al.   JOURNAL OF MEDICINAL CHEMISTRY

Important Hydrogen Bond Networks in Indoleamine 2,3-Dioxygenase 1 (IDO1) Inhibitor Design Revealed by Crystal Structures of Imidazoleisoindole Derivatives with IDO1

(2015) Yi-Hui Peng et al.   JOURNAL OF MEDICINAL CHEMISTRY

Indoleamine 2,3-dioxygenase vaccination

(2015) Mads Hald Andersen et al.   OncoImmunology

A first in man phase I trial of the oral immunomodulator, indoximod, combined with docetaxel in patients with metastatic solid tumors

(2015) Hatem H. Soliman et al.   Oncotarget

Human indoleamine 2,3-dioxygenase-2 has substrate specificity and inhibition characteristics distinct from those of indoleamine 2,3-dioxygenase-1

(2014) Georgios Pantouris et al.   AMINO ACIDS

Heme Enzyme Structure and Function

(2014) Thomas L. Poulos   CHEMICAL REVIEWS

The first indoleamine-2,3-dioxygenase-1 (IDO1) inhibitors containing carborane

(2014) Christopher J. D. Austin et al.   DALTON TRANSACTIONS

Detailed analysis and follow-up studies of a high-throughput screening for indoleamine 2,3-dioxygenase 1 (IDO1) inhibitors

(2014) Ute F. Röhrig et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

IDO2 is critical for IDO1-mediated T-cell regulation and exerts a non-redundant function in inflammation

(2014) Richard Metz et al.   INTERNATIONAL IMMUNOLOGY

Effects of Various Phytochemicals on Indoleamine 2,3-Dioxygenase 1 Activity: Galanal Is a Novel, Competitive Inhibitor of the Enzyme

(2014) Rie Yamamoto et al.   PLoS One

Mechanism of Action of Immunotherapy

(2014) Mary L. Disis   SEMINARS IN ONCOLOGY

Crystal Structures and Structure–Activity Relationships of Imidazothiazole Derivatives as IDO1 Inhibitors

(2014) Shingo Tojo et al.   ACS Medicinal Chemistry Letters

Indoleamine 2,3-dioxygenase 2 (IDO2) and the kynurenine pathway: characteristics and potential roles in health and disease

(2013) Amos A. Fatokun et al.   AMINO ACIDS

Heme-dependent dioxygenases in tryptophan oxidation

(2013) Jiafeng Geng et al.   ARCHIVES OF BIOCHEMISTRY AND BIOPHYSICS

Antitumour agents as inhibitors of tryptophan 2,3-dioxygenase

(2013) Georgios Pantouris et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

Long-lasting Disease Stabilization in the Absence of Toxicity in Metastatic Lung Cancer Patients Vaccinated with an Epitope Derived from Indoleamine 2,3 Dioxygenase

(2013) T. Z. Iversen et al.   CLINICAL CANCER RESEARCH

Indoleamine 2,3-dioxygenase inhibitors: a patent review (2008 – 2012)

(2013) Eduard Dolušić et al.   EXPERT OPINION ON THERAPEUTIC PATENTS

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

Crystal structure of Drosophila melanogaster tryptophan 2,3-dioxygenase reveals insights into substrate recognition and catalytic mechanism

(2013) Wei Huang et al.   JOURNAL OF STRUCTURAL BIOLOGY

Natural Product-Inspired Pyranonaphthoquinone Inhibitors of Indoleamine 2,3-Dioxygenase-1 (IDO-1)

(2012) David J. A. Bridewell et al.   AUSTRALIAN JOURNAL OF CHEMISTRY

Identification of selective inhibitors of indoleamine 2,3-dioxygenase 2

(2012) Supun M. Bakmiwewa et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Heme-containing dioxygenases involved in tryptophan oxidation

(2012) Elizabeth S Millett et al.   CURRENT OPINION IN CHEMICAL BIOLOGY

Synthesis, crystal structures and electronic properties of isomers of chloro-pyridinylvinyl-1H-indoles

(2012) Laurence Moineaux et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Rational Design of 4-Aryl-1,2,3-Triazoles for Indoleamine 2,3-Dioxygenase 1 Inhibition

(2012) Ute F. Röhrig et al.   JOURNAL OF MEDICINAL CHEMISTRY

Kynurenines in the CNS: recent advances and new questions

(2012) László Vécsei et al.   NATURE REVIEWS DRUG DISCOVERY

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

Trial watch

(2012) Erika Vacchelli et al.   OncoImmunology

Purification and kinetic characterization of human indoleamine 2,3-dioxygenases 1 and 2 (IDO1 and IDO2) and discovery of selective IDO1 inhibitors

(2011) David Meininger et al.   BIOCHIMICA ET BIOPHYSICA ACTA-PROTEINS AND PROTEOMICS

Synthesis and inhibition study of monoamine oxidase, indoleamine 2,3-dioxygenase and tryptophan 2,3-dioxygenase by 3,8-substituted 5H-indeno[1,2-c]pyridazin-5-one derivatives

(2011) J. Reniers et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

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

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

Complete Reaction Mechanism of Indoleamine 2,3-Dioxygenase as Revealed by QM/MM Simulations

(2011) Luciana Capece et al.   JOURNAL OF PHYSICAL CHEMISTRY B

The Mechanism of Formation ofN-Formylkynurenine by Heme Dioxygenases

(2011) Jaswir Basran et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Biochemical characteristics and inhibitor selectivity of mouse indoleamine 2,3-dioxygenase-2

(2010) Christopher Jonathan Daraius Austin et al.   AMINO ACIDS

Selective inhibition of IDO1 effectively regulates mediators of antitumor immunity

(2010) X. Liu et al.   BLOOD

Novel 1-alkyl-tryptophan derivatives downregulate IDO1 and IDO2 mRNA expression induced by interferon-gamma in dendritic cells

(2010) Ting Sun et al.   MOLECULAR AND CELLULAR BIOCHEMISTRY

Oxidation of L-tryptophan in biology: a comparison between tryptophan 2,3-dioxygenase and indoleamine 2,3-dioxygenase

(2009) Sara A. Rafice et al.   BIOCHEMICAL SOCIETY TRANSACTIONS

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

Evidence for a ferryl intermediate in a heme-based dioxygenase

(2009) A. Lewis-Ballester et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Histidine 55 of Tryptophan 2,3-Dioxygenase Is Not an Active Site Base but Regulates Catalysis by Controlling Substrate Binding‡

(2008) Sarah J. Thackray et al.   BIOCHEMISTRY

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

(2008) Jaswir Basran et al.   BIOCHEMISTRY

Indoleamine 2,3-dioxygenase-2; a new enzyme in the kynurenine pathway

(2008) Helen J. Ball et al.   INTERNATIONAL JOURNAL OF BIOCHEMISTRY & CELL BIOLOGY

Density Functional Theory Study on a Missing Piece in Understanding of Heme Chemistry: The Reaction Mechanism for Indoleamine 2,3-Dioxygenase and Tryptophan 2,3-Dioxygenase

(2008) Lung Wa Chung et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY