IDO1/TDO dual inhibitor RY103 targets Kyn-AhR pathway and exhibits preclinical efficacy on pancreatic cancer

How the AHR Became Important in Cancer: The Role of Chronically Active AHR in Cancer Aggression

(2021) Zhongyan Wang et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

GBP1 Facilitates Indoleamine 2,3-Dioxygenase Extracellular Secretion to Promote the Malignant Progression of Lung Cancer

(2021) Yinnan Meng et al.   Frontiers in Immunology

What is the prospect of indoleamine 2,3-dioxygenase 1 inhibition in cancer? Extrapolation from the past

(2021) Yu Yao et al.   JOURNAL OF EXPERIMENTAL & CLINICAL CANCER RESEARCH

Revisiting the role of CD4+ T cells in cancer immunotherapy—new insights into old paradigms

(2020) Rong En Tay et al.   CANCER GENE THERAPY

Synthesis of novel tryptanthrin derivatives as dual inhibitors of indoleamine 2,3-dioxygenase 1 and tryptophan 2,3-dioxygenase

(2020) Yuanyuan Li et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Discovery and structure-activity relationship studies of 1-aryl-1H-naphtho[2,3-d][1,2,3]triazole-4,9-dione derivatives as potent dual inhibitors of indoleamine 2,3-dioxygenase 1 (Ido1) and trytophan 2,3-dioxygenase (TDO)

(2020) Shulei Pan et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

IL4I1 Is a Metabolic Immune Checkpoint that Activates the AHR and Promotes Tumor Progression

(2020) Ahmed Sadik et al.   CELL

Preclinical investigations and a first-in-human phase I trial of M4112, the first dual inhibitor of indoleamine 2,3-dioxygenase 1 and tryptophan 2,3-dioxygenase 2, in patients with advanced solid tumors

(2020) Aung Naing et al.   Journal for ImmunoTherapy of Cancer

Tryptophan metabolism as a common therapeutic target in cancer, neurodegeneration and beyond

(2019) Michael Platten et al.   NATURE REVIEWS DRUG DISCOVERY

IDO1 inhibition potentiates vaccine-induced immunity against pancreatic adenocarcinoma

(2019) Alex B. Blair et al.   JOURNAL OF CLINICAL INVESTIGATION

4,6-Substituted-1H-Indazoles as potent IDO1/TDO dual inhibitors

(2019) Lingling Yang et al.   BIOORGANIC & MEDICINAL CHEMISTRY

AhR Activation in Pharmaceutical Development: Applying Liver Gene Expression Biomarker Thresholds to Identify Doses Associated with Tumorigenic Risks in Rats

(2019) Chunhua Qin et al.   TOXICOLOGICAL SCIENCES

A positive feedback between IDO1 metabolite and COL12A1 via MAPK pathway to promote gastric cancer metastasis

(2019) Zhen Xiang et al.   JOURNAL OF EXPERIMENTAL & CLINICAL CANCER RESEARCH

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

Immunomodulatory and antioxidant effects of pomegranate peel polysaccharides on immunosuppressed mice

(2019) Yuan Wu et al.   INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES

Synthesis and in vivo antitumor evaluation of an orally active potent phosphonamidate derivative targeting IDO1/IDO2/TDO

(2019) Xi Feng et al.   BIOCHEMICAL PHARMACOLOGY

Neoadjuvant Therapy Remodels the Pancreatic Cancer Microenvironment via Depletion of Protumorigenic Immune Cells

(2019) Carmen Mota Reyes et al.   CLINICAL CANCER RESEARCH

NO • /RUNX3/kynurenine metabolic signaling enhances disease aggressiveness in pancreatic cancer

(2019) Limin Wang et al.   INTERNATIONAL JOURNAL OF CANCER

N-Benzyl/Aryl Substituted Tryptanthrin as Dual Inhibitors of Indoleamine 2,3-Dioxygenase and Tryptophan 2,3-Dioxygenase

(2019) Dan Yang et al.   JOURNAL OF MEDICINAL CHEMISTRY

Design, synthesis and biological evaluation of indole-2-carboxylic acid derivatives as IDO1/TDO dual inhibitors

(2019) Guonan Cui et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

The global, regional, and national burden of pancreatic cancer and its attributable risk factors in 195 countries and territories, 1990–2017: a systematic analysis for the Global Burden of Disease Study 2017

(2019) Akram Pourshams et al.   Lancet Gastroenterology & Hepatology

Myeloid-derived suppressor cells coming of age

(2018) Filippo Veglia et al.   NATURE IMMUNOLOGY

Indoleamine 2, 3-dioxygenase and B7-H1 expressions as prognostic and follow-up markers in human pancreatic carcinoma

(2018) Liancai Wang et al.   PATHOLOGY RESEARCH AND PRACTICE

Targeting the IDO1/TDO2–KYN–AhR Pathway for Cancer Immunotherapy – Challenges and Opportunities

(2018) Jae Eun Cheong et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

1-Methyl-D-tryptophan Reduces Tumor CD133+ cells, Wnt/β-catenin and NF-κβp65 while Enhances Lymphocytes NF-κβ2, STAT3, and STAT4 Pathways in Murine Pancreatic Adenocarcinoma

(2018) Murad Alahdal et al.   Scientific Reports

Targeting the IDO1 pathway in cancer: from bench to bedside

(2018) Ming Liu et al.   Journal of Hematology & Oncology

Characterization of the Selective Indoleamine 2,3-Dioxygenase-1 (IDO1) Catalytic Inhibitor EOS200271/PF-06840003 Supports IDO1 as a Critical Resistance Mechanism to PD-(L)1 Blockade Therapy

(2018) Bruno Gomes et al.   MOLECULAR CANCER THERAPEUTICS

Diaryl hydroxylamines as pan or dual inhibitors of indoleamine 2,3-dioxygenase-1, indoleamine 2,3-dioxygenase-2 and tryptophan dioxygenase

(2018) Maria Winters et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Tumor cell expression of immune inhibitory molecules and tumor-infiltrating lymphocyte count predict cancer-specific survival in pancreatic and ampullary cancer

(2017) Kostandinos Sideras et al.   INTERNATIONAL JOURNAL OF CANCER

Nano-enabled pancreas cancer immunotherapy using immunogenic cell death and reversing immunosuppression

(2017) Jianqin Lu et al.   Nature Communications

Nutritional Stress Induced by Tryptophan-Degrading Enzymes Results in ATF4-Dependent Reprogramming of the Amino Acid Transporter Profile in Tumor Cells

(2016) Elina Timosenko et al.   CANCER RESEARCH

IDO in the Tumor Microenvironment: Inflammation, Counter-Regulation, and Tolerance

(2016) David H. Munn et al.   TRENDS IN IMMUNOLOGY

Recommendations for myeloid-derived suppressor cell nomenclature and characterization standards

(2016) Vincenzo Bronte et al.   Nature Communications

A TDO2-AhR Signaling Axis Facilitates Anoikis Resistance and Metastasis in Triple-Negative Breast Cancer

(2015) Nicholas C. D'Amato et al.   CANCER RESEARCH

Omeprazole Inhibits Pancreatic Cancer Cell Invasion through a Nongenomic Aryl Hydrocarbon Receptor Pathway

(2015) Un-Ho Jin et al.   CHEMICAL RESEARCH IN TOXICOLOGY

Tumor-Expressed IDO Recruits and Activates MDSCs in a Treg-Dependent Manner

(2015) Rikke B. Holmgaard et al.   Cell Reports

Salmonella-Based Therapy Targeting Indoleamine 2,3-Dioxygenase Coupled with Enzymatic Depletion of Tumor Hyaluronan Induces Complete Regression of Aggressive Pancreatic Tumors

(2015) E. R. Manuel et al.   Cancer Immunology Research

Tryptophan 2,3-dioxygenase (TDO)-reactive T cells differ in their functional characteristics in health and cancer

(2015) Mads Duus Hjortsø et al.   OncoImmunology

Elevation of MMP-9 and IDO induced by pancreatic cancer cells mediates natural killer cell dysfunction

(2014) Yun-Peng Peng et al.   BMC CANCER

A biological basis for depression in pancreatic cancer

(2014) Isadora C. Botwinick et al.   HPB

The pancreatic cancer microenvironment: an immunologic battleground

(2014) Venu G Pillarisetty   OncoImmunology

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

(2011) Christiane A. Opitz et al.   NATURE

Selective inhibition of IDO1 effectively regulates mediators of antitumor immunity

(2010) X. Liu et al.   BLOOD

1-MT enhances potency of tumor cell lysate-pulsed dendritic cells against pancreatic adenocarcinoma by downregulating the percentage of tregs

(2010) Yuandong Li et al.   Journal of Huazhong University of Science and Technology-Medical Sciences

Hydroxyamidine Inhibitors of Indoleamine-2,3-dioxygenase Potently Suppress Systemic Tryptophan Catabolism and the Growth of IDO-Expressing Tumors

(2010) H. K. Koblish et al.   MOLECULAR CANCER THERAPEUTICS