Cancer Immunotherapy: Selected Targets and Small-Molecule Modulators

Blocking of the PD-1/PD-L1 Interaction by aD-Peptide Antagonist for Cancer Immunotherapy

(2015) Hao-Nan Chang et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Immunotherapeutic Impact of Toll-like Receptor Agonists in Breast Cancer

(2015) Christine Zhang et al.   Anti-Cancer Agents in Medicinal Chemistry

Targeted Activation of Toll-Like Receptors: Conjugation of a Toll-Like Receptor 7 Agonist to a Monoclonal Antibody Maintains Antigen Binding and Specificity

(2015) Adam J. R. Gadd et al.   BIOCONJUGATE CHEMISTRY

Cytosolic sensing of aberrant DNA: arming STING on the endoplasmic reticulum

(2015) Qiang Wang et al.   EXPERT OPINION ON THERAPEUTIC TARGETS

Therapeutic targeting of Toll-like receptors in cutaneous disorders

(2015) Nassim Matin et al.   EXPERT OPINION ON THERAPEUTIC TARGETS

The potential of targeting indoleamine 2,3-dioxygenase for cancer treatment

(2015) Johanna M Gostner et al.   EXPERT OPINION ON THERAPEUTIC TARGETS

Research progress of indoleamine 2,3-dioxygenase inhibitors

(2015) Tianze Jiang et al.   Future Medicinal Chemistry

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

α,β-Methylene-ADP (AOPCP) Derivatives and Analogues: Development of Potent and Selective ecto-5′-Nucleotidase (CD73) Inhibitors

(2015) Sanjay Bhattarai 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

Structure-Based Design of Human TLR8-Specific Agonists with Augmented Potency and Adjuvanticity

(2015) Mallesh Beesu 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

IDO inhibitors move center stage in immuno-oncology

(2015) Cormac Sheridan   NATURE BIOTECHNOLOGY

Combination cancer immunotherapy and new immunomodulatory targets

(2015) Kathleen M. Mahoney et al.   NATURE REVIEWS DRUG DISCOVERY

Oncolytic viruses: a new class of immunotherapy drugs

(2015) Howard L. Kaufman et al.   NATURE REVIEWS DRUG DISCOVERY

Big opportunities for small molecules in immuno-oncology

(2015) Jerry L. Adams et al.   NATURE REVIEWS DRUG DISCOVERY

Targeting the TGFβ pathway for cancer therapy

(2015) Cindy Neuzillet et al.   PHARMACOLOGY & THERAPEUTICS

Structure of the Complex of Human Programmed Death 1, PD-1, and Its Ligand PD-L1

(2015) Krzysztof M. Zak et al.   STRUCTURE

New immunotherapies targeting the PD-1 pathway

(2015) Jordan M. Chinai et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Inhibitors of the PD-1/PD-L1 Pathway Can Mobilize the Immune System: An Innovative Potential Therapy for Cancer and Chronic Infections

(2015) Ahmed F. Abdel-Magid   ACS Medicinal Chemistry Letters

Direct Activation of STING in the Tumor Microenvironment Leads to Potent and Systemic Tumor Regression and Immunity

(2015) Leticia Corrales et al.   Cell Reports

Adenosine Receptor 2A Blockade Increases the Efficacy of Anti–PD-1 through Enhanced Antitumor T-cell Responses

(2015) Paul A. Beavis et al.   Cancer Immunology Research

Targeting STING pathways for the treatment of cancer

(2015) Claudia Gravekamp et al.   OncoImmunology

A2aR antagonists: Next generation checkpoint blockade for cancer immunotherapy

(2015) Robert D. Leone et al.   Computational and Structural Biotechnology Journal

Directing the Immune System with Chemical Compounds

(2014) Rock J. Mancini et al.   ACS Chemical Biology

Programmed Death-1: Therapeutic Success after More than 100 Years of Cancer Immunotherapy

(2014) Alexander Dömling et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

A Phase I Dose-Finding Study of the Novel Toll-like Receptor 8 Agonist VTX-2337 in Adult Subjects with Advanced Solid Tumors or Lymphoma

(2014) D. W. Northfelt et al.   CLINICAL CANCER RESEARCH

First-in-Human Dose Study of the Novel Transforming Growth Factor-β Receptor I Kinase Inhibitor LY2157299 Monohydrate in Patients with Advanced Cancer and Glioma

(2014) Jordi Rodon et al.   CLINICAL CANCER RESEARCH

Towards Next Generation Adenosine A2A Receptor Antagonists

(2014) G. Yuan et al.   CURRENT MEDICINAL CHEMISTRY

TGF-beta Signaling in Cancer Treatment

(2014) Isabel Fabregat et al.   CURRENT PHARMACEUTICAL DESIGN

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

Adenosine pathway and cancer: where do we go from here?

(2014) Luca Antonioli et al.   EXPERT OPINION ON THERAPEUTIC TARGETS

Immunoregulatory activity of adenosine and its role in human cancer progression

(2014) Sylvia Muller-Haegele et al.   Expert Review of Clinical Immunology

Discovery of N-((4-([1,2,4]Triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): A Highly Potent, Selective, and Orally Bioavailable Inhibitor of TGF-β Type I Receptor Kinase as Cancer Immunotherapeutic/Antifibrotic Agent

(2014) Cheng Hua Jin et al.   JOURNAL OF MEDICINAL CHEMISTRY

Chemically Synthesized Molecules with the Targeting and Effector Functions of Antibodies

(2014) Patrick J. McEnaney et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Adenosine A2B receptor antagonist PSB603 suppresses tumor growth and metastasis by inhibiting induction of regulatory T cells

(2014) Wakako Kaji et al.   JOURNAL OF TOXICOLOGICAL SCIENCES

Genentech dives deeper into the next wave of cancer immunotherapies

(2014) Sarah Crunkhorn   NATURE REVIEWS DRUG DISCOVERY

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

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

Targeting Cancer-Derived Adenosine:New Therapeutic Approaches

(2014) A. Young et al.   Cancer Discovery

Hostile, Hypoxia-A2-Adenosinergic Tumor Biology as the Next Barrier to Overcome for Tumor Immunologists

(2014) M. V. Sitkovsky et al.   Cancer Immunology Research

Co-blockade of immune checkpoints and adenosine A2Areceptor suppresses metastasis

(2014) Arabella Young et al.   OncoImmunology

A Phase I study of NLG919 for adult patients with recurrent advanced solid tumors

(2014) Asha Nayak et al.   Journal for ImmunoTherapy of Cancer

Mechanism of tumor rejection with doublets of CTLA-4, PD-1/PD-L1, or IDO blockade involves restored IL-2 production and proliferation of CD8+ T cells directly within the tumor microenvironment

(2014) Stefani Spranger et al.   Journal for ImmunoTherapy of Cancer

Immune Modulation in Cancer with Antibodies

(2013) David B. Page et al.   Annual Review of Medicine

Using macrophage activation to augment immunotherapy of established tumours

(2013) Z G Fridlender et al.   BRITISH JOURNAL OF CANCER

Toll-like receptors as therapeutic targets for cancer

(2013) Johanna Holldack   DRUG DISCOVERY TODAY

Activin receptor-like kinase5 inhibition suppresses mouse melanoma by ubiquitin degradation of Smad4, thereby derepressing eomesodermin in cytotoxic T lymphocytes

(2013) Jeong-Hwan Yoon et al.   EMBO Molecular Medicine

Indoleamine 2,3-dioxygenase is a critical resistance mechanism in antitumor T cell immunotherapy targeting CTLA-4

(2013) Rikke B. Holmgaard et al.   JOURNAL OF EXPERIMENTAL MEDICINE

The role of PD-1 and PD-L1 in T-cell immune suppression in patients with hematological malignancies

(2013) Li Shi et al.   Journal of Hematology & Oncology

The Yin and Yang of Toll-like receptors in cancer

(2013) J-P Pradere et al.   ONCOGENE

Blockade of A2Areceptors potently suppresses the metastasis of CD73+tumors

(2013) Paul A. Beavis et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Molecular signatures of T-cell inhibition in HIV-1 infection

(2013) Marie Larsson et al.   Retrovirology

Targeting Toll-Like Receptors: Promising Therapeutic Strategies for the Management of Sepsis-Associated Pathology and Infectious Diseases

(2013) Athina Savva et al.   Frontiers in Immunology

A novel peptide therapeutic targeting PD1 immune checkpoint with equipotent antagonism of both ligands and a potential for better management of immune-related adverse events

(2013) Pottayil Sasikumar et al.   Journal for ImmunoTherapy of Cancer

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

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

Systemic delivery of a TLR7 agonist in combination with radiation primes durable antitumor immune responses in mouse models of lymphoma

(2012) S. J. Dovedi et al.   BLOOD

Abstract 2850: Demonstration of anti-tumor efficacy in multiple preclinical cancer models using a novel peptide inhibitor (Aurigene-012) of the PD1 signaling pathway

(2012) Pottayil G. Sasikumar et al.   CANCER RESEARCH

Necrostatin-1 blocks both RIPK1 and IDO: consequences for the study of cell death in experimental disease models

(2012) P Vandenabeele et al.   CELL DEATH AND DIFFERENTIATION

Molecular Pathways: Next-Generation Immunotherapy--Inhibiting Programmed Death-Ligand 1 and Programmed Death-1

(2012) D. S. Chen et al.   CLINICAL CANCER RESEARCH

New developments in Toll-like receptor targeted therapeutics

(2012) Dympna J Connolly et al.   CURRENT OPINION IN PHARMACOLOGY

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

Crystal structures of STING protein reveal basis for recognition of cyclic di-GMP

(2012) Guijun Shang et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

ENTPD1/CD39 is a promising therapeutic target in oncology

(2012) J Bastid et al.   ONCOGENE

Influence of Tryptophan Contained in 1-Methyl-Tryptophan on Antimicrobial and Immunoregulatory Functions of Indoleamine 2,3-Dioxygenase

(2012) Silvia K. Schmidt et al.   PLoS One

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

Raising the Bar: The Curative Potential of Human Cancer Immunotherapy

(2012) S. A. Rosenberg   Science Translational Medicine

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

Randomized Phase III Placebo-Controlled Trial of Carboplatin and Paclitaxel With or Without the Vascular Disrupting Agent Vadimezan (ASA404) in Advanced Non–Small-Cell Lung Cancer

(2011) Primo N. Lara et al.   JOURNAL OF CLINICAL ONCOLOGY

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

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

The kynurenine system and immunoregulation

(2011) Yvette Mándi et al.   JOURNAL OF NEURAL TRANSMISSION

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

(2011) Christiane A. Opitz et al.   NATURE

The Indoleamine-2,3-Dioxygenase (IDO) Inhibitor 1-Methyl-D-tryptophan Upregulates IDO1 in Human Cancer Cells

(2011) Christiane A. Opitz et al.   PLoS One

Induction of Heart Valve Lesions by Small-Molecule ALK5 Inhibitors

(2011) Mark J. Anderton et al.   TOXICOLOGIC PATHOLOGY

Selective inhibition of IDO1 effectively regulates mediators of antitumor immunity

(2010) X. Liu et al.   BLOOD

Toll-like receptor agonists in cancer therapy

(2009) Sylvia Adams   Immunotherapy

Cancer immunotherapeutic potential of novel small molecule TLR7 and TLR8 agonists

(2009) Svetlana Hamm et al.   Journal of Immunotoxicology

1-Alkyl-8-(piperazine-1-sulfonyl)phenylxanthines: Development and Characterization of Adenosine A2BReceptor Antagonists and a New Radioligand with Subnanomolar Affinity and Subtype Specificity

(2009) Thomas Borrmann 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

Therapeutic Targeting of Toll-Like Receptors for Infectious and Inflammatory Diseases and Cancer

(2009) L. A. J. O'Neill et al.   PHARMACOLOGICAL REVIEWS

Synthesis and immunostimulatory properties of the phosphorothioate analogues of cdiGMP

(2008) Hongbin Yan et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Twelve immunotherapy drugs that could cure cancers

(2008) Martin A. ‘Mac’ Cheever   IMMUNOLOGICAL REVIEWS

Identification of RIP1 kinase as a specific cellular target of necrostatins

(2008) Alexei Degterev et al.   Nature Chemical Biology

Structures of PD-1 with its ligands: Sideways and dancing cheek to cheek

(2008) G. J. Freeman   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Crystal structure of the complex between programmed death-1 (PD-1) and its ligand PD-L2

(2008) E. Lazar-Molnar et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Oncogenic kinase NPM/ALK induces through STAT3 expression of immunosuppressive protein CD274 (PD-L1, B7-H1)

(2008) M. Marzec et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA