Recent progress in the development of Toll-like receptor (TLR) antagonists

The critical role of toll-like receptors — From microbial recognition to autoimmunity: A comprehensive review

(2016) Maximiliano Javier Jiménez-Dalmaroni et al.   AUTOIMMUNITY REVIEWS

Pharmacological characterization of the opioid inactive isomers (+)-naltrexone and (+)-naloxone as antagonists of toll-like receptor 4

(2016) X Wang et al.   BRITISH JOURNAL OF PHARMACOLOGY

Identification of a Human Toll-Like Receptor (TLR) 8-Specific Agonist and a Functional Pan-TLR Inhibitor in 2-Aminoimidazoles

(2016) Mallesh Beesu et al.   JOURNAL OF MEDICINAL CHEMISTRY

Toll-like receptors: potential targets for lupus treatment

(2015) Yan-wei Wu et al.   ACTA PHARMACOLOGICA SINICA

Microbially Driven TLR5-Dependent Signaling Governs Distal Malignant Progression through Tumor-Promoting Inflammation

(2015) Melanie R. Rutkowski et al.   CANCER CELL

Pyrimidine Triazole Thioether Derivatives as Toll-Like Receptor 5 (TLR5)/Flagellin Complex Inhibitors

(2015) Lei Yan et al.   ChemMedChem

Patents for Toll-like receptor ligands as radiation countermeasures for acute radiation syndrome

(2015) Vijay K Singh et al.   EXPERT OPINION ON THERAPEUTIC PATENTS

Leucine-rich repeat 2 of human Toll-like receptor 4 contains the binding site for inhibitory monoclonal antibodies

(2015) Hiroki Tsukamoto et al.   FEBS LETTERS

A randomized trial of Mycobacterium w in severe sepsis

(2015) Inderpaul Singh Sehgal et al.   JOURNAL OF CRITICAL CARE

Toll-like Receptor 10 inHelicobacter pyloriInfection

(2015) Hiroyuki Nagashima et al.   JOURNAL OF INFECTIOUS DISEASES

Structure–Activity Relationships of (+)-Naltrexone-Inspired Toll-like Receptor 4 (TLR4) Antagonists

(2015) Brandon R. Selfridge et al.   JOURNAL OF MEDICINAL CHEMISTRY

Control of adaptive immunity by the innate immune system

(2015) Akiko Iwasaki et al.   NATURE IMMUNOLOGY

Structural basis for inhibition of TLR2 by staphylococcal superantigen-like protein 3 (SSL3)

(2015) Kirsten J. Koymans et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Inhibition of TLR2 signaling by small molecule inhibitors targeting a pocket within the TLR2 TIR domain

(2015) Pragnesh Mistry et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

A Decoy Peptide that Disrupts TIRAP Recruitment to TLRs Is Protective in a Murine Model of Influenza

(2015) Wenji Piao et al.   Cell Reports

Prospective Virtual Screening in a Sparse Data Scenario: Design of Small-Molecule TLR2 Antagonists

(2014) Manuela S. Murgueitio et al.   ChemMedChem

The use of low-dose naltrexone (LDN) as a novel anti-inflammatory treatment for chronic pain

(2014) Jarred Younger et al.   CLINICAL RHEUMATOLOGY

Toll-like receptor agonists: a patent review (2011 – 2013)

(2014) Waleed M Hussein et al.   EXPERT OPINION ON THERAPEUTIC PATENTS

Effects of Hydroxychloroquine on Symptomatic Improvement in Primary Sjögren Syndrome

(2014) Jacques-Eric Gottenberg et al.   JAMA-JOURNAL OF THE AMERICAN MEDICAL ASSOCIATION

Vizantin Inhibits Endotoxin-Mediated Immune Responses via the TLR 4/MD-2 Complex

(2014) Masataka Oda et al.   JOURNAL OF IMMUNOLOGY

Sequence-dependent off-target inhibition of TLR7/8 sensing by synthetic microRNA inhibitors

(2014) Soroush T. Sarvestani et al.   NUCLEIC ACIDS RESEARCH

UNC93B1 is essential for the plasma membrane localization and signaling of Toll-like receptor 5

(2014) J.-W. Huh et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Toll-like receptor 10 is involved in induction of innate immune responses to influenza virus infection

(2014) S. M. Y. Lee et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Blockade of TLR3 protects mice from lethal radiation-induced gastrointestinal syndrome

(2014) Naoki Takemura et al.   Nature Communications

Functional TLR5 Genetic Variants Affect Human Colorectal Cancer Survival

(2013) S. N. Klimosch et al.   CANCER RESEARCH

Modulation of CD14 and TLR4⋅MD-2 Activities by a Synthetic Lipid A Mimetic

(2013) Roberto Cighetti et al.   CHEMBIOCHEM

Randomized, Double-Blind, Placebo-Controlled, Dose-Escalating Phase I, Healthy Subjects Study of Intravenous OPN-305, a Humanized Anti-TLR2 Antibody

(2013) M Reilly et al.   CLINICAL PHARMACOLOGY & THERAPEUTICS

TLR2 and TLR4 in Autoimmune Diseases: a Comprehensive Review

(2013) Yu Liu et al.   CLINICAL REVIEWS IN ALLERGY & IMMUNOLOGY

Effect of Eritoran, an Antagonist of MD2-TLR4, on Mortality in Patients With Severe Sepsis

(2013) Steven M. Opal et al.   JAMA-JOURNAL OF THE AMERICAN MEDICAL ASSOCIATION

Identification of TLR10 as a Key Mediator of the Inflammatory Response to Listeria monocytogenes in Intestinal Epithelial Cells and Macrophages

(2013) T. Regan et al.   JOURNAL OF IMMUNOLOGY

A Novel Small-Molecule Enantiomeric Analogue of Traditional (-)-Morphinans Has Specific TLR9 Antagonist Properties and Reduces Sterile Inflammation-Induced Organ Damage

(2013) R. Hoque et al.   JOURNAL OF IMMUNOLOGY

CD103−CD11b+ dendritic cells regulate the sensitivity of CD4 T-cell responses to bacterial flagellin

(2013) S M Atif et al.   Mucosal Immunology

The TLR4 antagonist Eritoran protects mice from lethal influenza infection

(2013) Kari Ann Shirey et al.   NATURE

A toll-like receptor 9 antagonist reduces pain hypersensitivity and the inflammatory response in spinal cord injury

(2013) Brian T. David et al.   NEUROBIOLOGY OF DISEASE

Design, synthesis and biological evaluation of novel antagonist compounds of Toll-like receptors 7, 8 and 9

(2013) Ekambar R. Kandimalla et al.   NUCLEIC ACIDS RESEARCH

Structural Reorganization of the Toll-Like Receptor 8 Dimer Induced by Agonistic Ligands

(2013) H. Tanji et al.   SCIENCE

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

Fine-Tuning Multiprotein Complexes Using Small Molecules

(2012) Andrea D. Thompson et al.   ACS Chemical Biology

Discovery of Small-Molecule Inhibitors of the TLR1/TLR2 Complex

(2012) Kui Cheng et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Treatment With OPN-305, a Humanized Anti–Toll-Like Receptor-2 Antibody, Reduces Myocardial Ischemia/Reperfusion Injury in Pigs

(2012) Fatih Arslan et al.   Circulation-Cardiovascular Interventions

The Role of UNC93B1 Protein in Surface Localization of TLR3 Receptor and in Cell Priming to Nucleic Acid Agonists

(2012) Jelka Pohar et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Lateral Clustering of TLR3:dsRNA Signaling Units Revealed by TLR3ecd:3Fabs Quaternary Structure

(2012) Jinquan Luo et al.   JOURNAL OF MOLECULAR BIOLOGY

Toll-like receptors in transplantation: sensing and reacting to injury

(2012) Jeremy S. Leventhal et al.   KIDNEY INTERNATIONAL

Morphine activates neuroinflammation in a manner parallel to endotoxin

(2012) X. Wang et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Structural Basis of TLR5-Flagellin Recognition and Signaling

(2012) S.-i. Yoon et al.   SCIENCE

Prevention and diminished expression of experimental autoimmune encephalomyelitis by low dose naltrexone (LDN) or opioid growth factor (OGF) for an extended period: Therapeutic implications for multiple sclerosis

(2011) Kristen A. Rahn et al.   BRAIN RESEARCH

Innate immune DNA sensing pathways: STING, AIMII and the regulation of interferon production and inflammatory responses

(2011) Glen N Barber   CURRENT OPINION IN IMMUNOLOGY

Therapy with the Opioid Antagonist Naltrexone Promotes Mucosal Healing in Active Crohn’s Disease: A Randomized Placebo-Controlled Trial

(2011) Jill P. Smith et al.   DIGESTIVE DISEASES AND SCIENCES

Toll-like receptor modulators: a patent review (2006 – 2010)

(2011) Shaherin Basith et al.   EXPERT OPINION ON THERAPEUTIC PATENTS

Immune Signaling by RIG-I-like Receptors

(2011) Yueh-Ming Loo et al.   IMMUNITY

Myeloid C-type Lectin Receptors in Pathogen Recognition and Host Defense

(2011) Fabiola Osorio et al.   IMMUNITY

Regulation of the Antimicrobial Response by NLR Proteins

(2011) Eran Elinav et al.   IMMUNITY

Toll-like Receptors and Their Crosstalk with Other Innate Receptors in Infection and Immunity

(2011) Taro Kawai et al.   IMMUNITY

Optimal oligonucleotide sequences for TLR9 inhibitory activity in human cells: lack of correlation with TLR9 binding

(2011) Robert F. Ashman et al.   INTERNATIONAL IMMUNOLOGY

Contribution of Different Mechanisms to Pancreatic Beta-cell Hyper-secretion in Non-obese Diabetic (NOD) Mice during Pre-diabetes

(2011) Kuo Liang et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Herpes simplex virus encephalitis in a patient with complete TLR3 deficiency: TLR3 is otherwise redundant in protective immunity

(2011) Yiqi Guo et al.   JOURNAL OF EXPERIMENTAL MEDICINE

Targeting TLR4 Signaling by TLR4 Toll/IL-1 Receptor Domain-Derived Decoy Peptides: Identification of the TLR4 Toll/IL-1 Receptor Domain Dimerization Interface

(2011) V. Y. Toshchakov et al.   JOURNAL OF IMMUNOLOGY

Mechanism of Endosomal TLR Inhibition by Antimalarial Drugs and Imidazoquinolines

(2011) A. Kuznik et al.   JOURNAL OF IMMUNOLOGY

Small-Molecule Inhibitors of the TLR3/dsRNA Complex

(2011) Kui Cheng et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Therapeutical targeting of nucleic acid-sensing Toll-like receptors prevents experimental cerebral malaria

(2011) Bernardo S. Franklin et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

The Structural Biology of Toll-like Receptors

(2011) Istvan Botos et al.   STRUCTURE

A randomized, double-blind, placebo-controlled trial of TAK-242 for the treatment of severe sepsis*

(2010) Todd W. Rice et al.   CRITICAL CARE MEDICINE

TAK-242 (Resatorvid), a Small-Molecule Inhibitor of Toll-Like Receptor (TLR) 4 Signaling, Binds Selectively to TLR4 and Interferes with Interactions between TLR4 and Its Adaptor Molecules

(2010) N. Matsunaga et al.   MOLECULAR PHARMACOLOGY

IFI16 is an innate immune sensor for intracellular DNA

(2010) Leonie Unterholzner et al.   NATURE IMMUNOLOGY

The role of pattern-recognition receptors in innate immunity: update on Toll-like receptors

(2010) Taro Kawai et al.   NATURE IMMUNOLOGY

Targeting Toll-like receptors: emerging therapeutics?

(2010) Elizabeth J. Hennessy et al.   NATURE REVIEWS DRUG DISCOVERY

Metabolic Syndrome and Altered Gut Microbiota in Mice Lacking Toll-Like Receptor 5

(2010) M. Vijay-Kumar et al.   SCIENCE

Selection, Preparation, and Evaluation of Small-Molecule Inhibitors of Toll-Like Receptor 4

(2010) Douglas E. Bevan et al.   ACS Medicinal Chemistry Letters

Stilbene glycosides are natural product inhibitors of FGF-2-induced angiogenesis

(2009) Sajjad Hussain et al.   BMC CELL BIOLOGY

Recognition of Lipopeptide Patterns by Toll-like Receptor 2-Toll-like Receptor 6 Heterodimer

(2009) Jin Young Kang et al.   IMMUNITY

AIM2 activates the inflammasome and cell death in response to cytoplasmic DNA

(2009) Teresa Fernandes-Alnemri et al.   NATURE

Toll-Like Receptor 3 Signaling on Macrophages Is Required for Survival Following Coxsackievirus B4 Infection

(2009) Martin J. Richer et al.   PLoS One

Antimalarial Activity of a New Stilbene Glycoside from Parthenocissus tricuspidata in Mice

(2008) W.-H. Park et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

TLRs and innate immunity

(2008) B. A. Beutler   BLOOD

Functional diversification of the toll-like receptor gene family

(2008) Austin L. Hughes et al.   IMMUNOGENETICS

An Agonist of Toll-Like Receptor 5 Has Radioprotective Activity in Mouse and Primate Models

(2008) L. G. Burdelya et al.   SCIENCE

Structural Basis of Toll-Like Receptor 3 Signaling with Double-Stranded RNA

(2008) L. Liu et al.   SCIENCE