Toll-like receptor 4 (TLR4) inhibitors: Current research and prospective

Toll-Like Receptors in Acute Kidney Injury

(2021) Cristina Vázquez-Carballo et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

COVID-19 and Toll-Like Receptor 4 (TLR4): SARS-CoV-2 May Bind and Activate TLR4 to Increase ACE2 Expression, Facilitating Entry and Causing Hyperinflammation

(2021) Mohamed M. Aboudounya et al.   MEDIATORS OF INFLAMMATION

Small Immunomodulatory Molecules as Potential Therapeutics in Experimental Murine Models of Acute Lung Injury (ALI)/Acute Respiratory Distress Syndrome (ARDS)

(2021) Dilip Shah et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

TLR4 as a therapeutic target for respiratory and neurological complications of SARS-CoV-2

(2021) Dhriti Kaushik et al.   EXPERT OPINION ON THERAPEUTIC TARGETS

Synthesis and evaluation of the anti-inflammatory activity of novel 8-quinolinesulfonamide derivatives as TLR4/MD-2 inhibitors with efficacy in adjuvant-induced arthritis

(2021) Tongtong Liu et al.   BIOORGANIC CHEMISTRY

The interplay of DAMPs, TLR4, and proinflammatory cytokines in pulmonary fibrosis

(2021) Siavash Bolourani et al.   JOURNAL OF MOLECULAR MEDICINE-JMM

Sulfatides are endogenous ligands for the TLR4–MD-2 complex

(2021) Lijing Su et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Targeting TLR4 Signaling to Blunt Viral-Mediated Acute Lung Injury

(2021) Kari Ann Shirey et al.   Frontiers in Immunology

The impact of DAMP-mediated inflammation in severe COVID-19 and related disorders

(2021) Upasana Parthasarathy et al.   BIOCHEMICAL PHARMACOLOGY

Synthesis, activity and mechanism for double-ring conjugated enones

(2021) Shiyang Zhou et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Effect of chitosan on blood profile, inflammatory cytokines by activating TLR4/NF-κB signaling pathway in intestine of heat stressed mice

(2021) Sahar Ghulam Mohyuddin et al.   Scientific Reports

Toll-like receptor-4 antagonist (+)-naltrexone protects against carbamyl-platelet activating factor (Cpaf)-induced preterm labor in mice

(2020) Hanan H. Wahid et al.   AMERICAN JOURNAL OF PATHOLOGY

TLR4-Targeting Therapeutics: Structural Basis and Computer-Aided Drug Discovery Approaches

(2020) Qurat ul Ain et al.   MOLECULES

Design and Catalyzed Activation of Tak-242 Prodrugs for Localized Inhibition of TLR4-Induced Inflammation

(2020) Michael A. Plunk et al.   ACS Medicinal Chemistry Letters

Novel paeonol derivatives: Design, synthesis and anti-inflammatory activity in vitro and in vivo

(2020) Yang Sheng Hu et al.   BIOORGANIC CHEMISTRY

Protective Effect of a Novel (2S, 3R, 4S)-Chromene-3-Carboxamide Derivative, Z20 Against Sepsis-Induced Organ Injury

(2020) Liyan Zeng et al.   INFLAMMATION

The human milk oligosaccharides 2’-fucosyllactose and 6’-sialyllactose protect against the development of necrotizing enterocolitis by inhibiting toll-like receptor 4 signaling

(2020) Chhinder P. Sodhi et al.   PEDIATRIC RESEARCH

Insight Into TLR4-Mediated Immunomodulation in Normal Pregnancy and Related Disorders

(2020) Priyanka Firmal et al.   Frontiers in Immunology

Antidepressive Effect of Arctiin by Attenuating Neuroinflammation via HMGB1/TLR4- and TNF-α/TNFR1-Mediated NF-κB Activation

(2020) Xiang Xu et al.   ACS Chemical Neuroscience

Crocin attenuates cisplatin-induced hepatotoxicity via TLR4/NF-κBp50 signaling and BAMBI modulation of TGF-β activity: Involvement of miRNA-9 and miRNA-29

(2020) L.H. Khedr et al.   FOOD AND CHEMICAL TOXICOLOGY

Danshen ( Salvia miltiorrhiza ) restricts MD2/TLR4‐MyD88 complex formation and signalling in acute myocardial infarction‐induced heart failure

(2020) Xiaoping Wang et al.   JOURNAL OF CELLULAR AND MOLECULAR MEDICINE

Blockade of the TLR4–MD2 complex lowers blood pressure and improves vascular function in a murine model of type 1 diabetes

(2020) Amanda Almeida de Oliveira et al.   Scientific Reports

Increasing the Chemical Variety of Small-Molecule-Based TLR4 Modulators: An Overview

(2020) Alessio Romerio et al.   Frontiers in Immunology

Ruscogenin attenuates particulate matter-induced acute lung injury in mice via protecting pulmonary endothelial barrier and inhibiting TLR4 signaling pathway

(2020) Yu-wei Wang et al.   ACTA PHARMACOLOGICA SINICA

TLR4 and CD14 trafficking and its influence on LPS-induced pro-inflammatory signaling

(2020) Anna Ciesielska et al.   CELLULAR AND MOLECULAR LIFE SCIENCES

Autophagy alleviates mitochondrial DAMP-induced acute lung injury by inhibiting NLRP3 inflammasome

(2020) Wei Peng et al.   LIFE SCIENCES

Toll-Like Receptor 4 Signaling and Drug Addiction

(2020) Ruyan Wu et al.   Frontiers in Pharmacology

Acylpolyamine Mygalin as a TLR4 Antagonist Based on Molecular Docking and In Vitro Analyses

(2020) Abraham Espinoza-Culupú et al.   Biomolecules

Key Player in Cardiac Hypertrophy, Emphasizing the Role of Toll-Like Receptor 4

(2020) Zheng Xiao et al.   Frontiers in Cardiovascular Medicine

Novel Chitohexaose Analog Protects Young and Aged mice from CLP Induced Polymicrobial Sepsis

(2019) Pragnya Das et al.   Scientific Reports

Novel carboxylate-based glycolipids: TLR4 antagonism, MD-2 binding and self-assembly properties

(2019) Florent Cochet et al.   Scientific Reports

Below the surface: The inner lives of TLR4 and TLR9

(2019) Laura Marongiu et al.   JOURNAL OF LEUKOCYTE BIOLOGY

Loganetin protects against rhabdomyolysis‐induced acute kidney injury by modulating the toll‐like receptor 4 signalling pathway

(2019) Jie Li et al.   BRITISH JOURNAL OF PHARMACOLOGY

Discovery of 3-(Indol-5-yl)-indazole Derivatives as Novel Myeloid Differentiation Protein 2/Toll-like Receptor 4 Antagonists for Treatment of Acute Lung Injury

(2019) Zhiguo Liu et al.   JOURNAL OF MEDICINAL CHEMISTRY

Type I interferon signaling, regulation and gene stimulation in chronic virus infection

(2019) Sabelo Lukhele et al.   SEMINARS IN IMMUNOLOGY

Linear and Rationally Designed Stapled Peptides Abrogate TLR4 Pathway and Relieve Inflammatory Symptoms in Rheumatoid Arthritis Rat Model

(2019) Asma Achek et al.   JOURNAL OF MEDICINAL CHEMISTRY

Novel resveratrol-based flavonol derivatives: Synthesis and anti-inflammatory activity in vitro and in vivo

(2019) Liu Zeng Chen et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Diastereoselective Synthesis of 3,4-Dihydropyran-3-carboxamides with in Vitro Anti-inflammatory Activity

(2019) Li-Yan Zeng et al.   ACS Combinatorial Science

Scoparone alleviates inflammation, apoptosis and fibrosis of non-alcoholic steatohepatitis by suppressing the TLR4/NF-κB signaling pathway in mice

(2019) Beibei Liu et al.   INTERNATIONAL IMMUNOPHARMACOLOGY

Key residues in TLR4-MD2 tetramer formation identified by free energy simulations

(2019) Alireza Tafazzol et al.   PLoS Computational Biology

Scoparone prevents IL-1β-induced inflammatory response in human osteoarthritis chondrocytes through the PI3K/Akt/NF-κB pathway

(2018) Chao Lu et al.   BIOMEDICINE & PHARMACOTHERAPY

Calpain inhibitor I attenuates atherosclerosis and inflammation in atherosclerotic rats through eNOS/NO/NF-κB pathway

(2018) Lan Yu et al.   CANADIAN JOURNAL OF PHYSIOLOGY AND PHARMACOLOGY

Recent progress in the discovery of myeloid differentiation 2 (MD2) modulators for inflammatory diseases

(2018) Lingfeng Chen et al.   DRUG DISCOVERY TODAY

Discovery of novel small molecule TLR4 inhibitors as potent anti-inflammatory agents

(2018) Yao Xu et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Discovery of caffeic acid phenethyl ester derivatives as novel myeloid differentiation protein 2 inhibitors for treatment of acute lung injury

(2018) Lingfeng Chen et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Lipopolysaccharide (LPS)-binding protein stimulates CD14-dependent Toll-like receptor 4 internalization and LPS-induced TBK1–IKKϵ–IRF3 axis activation

(2018) Hiroki Tsukamoto et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Dissecting the Innate Immune Recognition of Opioid Inactive Isomer (+)-Naltrexone Derived Toll-like Receptor 4 (TLR4) Antagonists

(2018) Xiaozheng Zhang et al.   Journal of Chemical Information and Modeling

Structure–Activity Relationship in Monosaccharide-Based Toll-Like Receptor 4 (TLR4) Antagonists

(2018) Fabio A. Facchini et al.   JOURNAL OF MEDICINAL CHEMISTRY

The Cancer Prevention, Anti-Inflammatory and Anti-Oxidation of Bioactive Phytochemicals Targeting the TLR4 Signaling Pathway

(2018) Chung-Yi Chen et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

Ferulic Acid Rescues LPS-Induced Neurotoxicity via Modulation of the TLR4 Receptor in the Mouse Hippocampus

(2018) Shafiq Ur Rehman et al.   MOLECULAR NEUROBIOLOGY

Amphiphilic Guanidinocalixarenes Inhibit Lipopolysaccharide (LPS)- and Lectin-Stimulated Toll-like Receptor 4 (TLR4) Signaling

(2017) Stefania E. Sestito et al.   JOURNAL OF MEDICINAL CHEMISTRY

Quantitative single-molecule imaging of TLR4 reveals ligand-specific receptor dimerization

(2017) Carmen L. Krüger et al.   Science Signaling

Quantitative single-molecule imaging of TLR4 reveals ligand-specific receptor dimerization

(2017) Carmen L. Krüger et al.   Science Signaling

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

Carvedilol attenuates paraquat-induced lung injury by inhibition of proinflammatory cytokines, chemokine MCP-1, NF-κB activation and oxidative stress mediators

(2016) Keyvan Amirshahrokhi et al.   CYTOKINE

Discovery of novel sesquistilbene indanone analogues as potent anti-inflammatory agents

(2016) Mei-Lin Tang et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Oil-in-water nanoemulsions are suitable for carrying hydrophobic compounds: Indomethacin as a model of anti-inflammatory drug

(2016) Björn Kwasigroch et al.   INTERNATIONAL JOURNAL OF PHARMACEUTICS

TRIF-dependent TLR signaling, its functions in host defense and inflammation, and its potential as a therapeutic target

(2016) M. Obayed Ullah et al.   JOURNAL OF LEUKOCYTE BIOLOGY

Synthesis and Biological Evaluation of N-Aryl-N'-(5-(2-hydroxybenzoyl) pyrimidin-2-yl)guanidines as Toll-Like Receptor 4 Antagonists

(2016) Matej Sova et al.   Medicinal Chemistry

Scoparone Inhibits LPS-Simulated Inflammatory Response by Suppressing IRF3 and ERK in BV-2 Microglial Cells

(2016) Duk-Yeon Cho et al.   MOLECULES

Necrotizing enterocolitis: new insights into pathogenesis and mechanisms

(2016) Diego F. Niño et al.   Nature Reviews Gastroenterology & Hepatology

Moulding calixarenes for biomacromolecule targeting

(2015) Marta Giuliani et al.   CHEMICAL COMMUNICATIONS

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

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

Extractable and non-extractable polyphenols from blueberries modulate LPS-induced expression of iNOS and COX-2 in RAW264.7 macrophages via the NF-κB signalling pathway

(2015) Anwei Cheng et al.   JOURNAL OF THE SCIENCE OF FOOD AND AGRICULTURE

Phosphorylation of innate immune adaptor proteins MAVS, STING, and TRIF induces IRF3 activation

(2015) S. Liu et al.   SCIENCE

Activation of MEK/ERK pathways through NF-κB activation is involved in interleukin-1β-induced cyclooxygenease-2 expression in canine dermal fibroblasts

(2015) Hisashi Tsuchiya et al.   VETERINARY IMMUNOLOGY AND IMMUNOPATHOLOGY

Biosynthesis and Export of Bacterial Lipopolysaccharides

(2014) Chris Whitfield et al.   Annual Review of Biochemistry

A Promiscuous Lipid-Binding Protein Diversifies the Subcellular Sites of Toll-like Receptor Signal Transduction

(2014) Kevin S. Bonham et al.   CELL

Co-operation of TLR4 and raft proteins in LPS-induced pro-inflammatory signaling

(2014) Agnieszka Płóciennikowska et al.   CELLULAR AND MOLECULAR LIFE SCIENCES

Sepsis: Current Dogma and New Perspectives

(2014) Clifford S. Deutschman et al.   IMMUNITY

Structure of vaccinia virus A46, an inhibitor of TLR4 signaling pathway, shows the conformation of VIPER motif

(2014) Yongwoon Kim et al.   PROTEIN SCIENCE

Conformationally Constrained Lipid A Mimetics for Exploration of Structural Basis of TLR4/MD-2 Activation by Lipopolysaccharide

(2013) Daniel Artner et al.   ACS Chemical Biology

Synthesis and neuroprotective effect of E-3,4-dihydroxy styryl aralkyl ketones derivatives against oxidative stress and inflammation

(2013) Xianling Ning et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Inhibitory effect of resveratrol dimerized derivatives on nitric oxide production in lipopolysaccharide-induced RAW 264.7 cells

(2013) Chen Zhong et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Novel toll-like receptor 4 (TLR4) antagonists identified by structure- and ligand-based virtual screening

(2013) Urban Švajger et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

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

Direct Proteomic Quantification of the Secretome of Activated Immune Cells

(2013) F. Meissner et al.   SCIENCE

Mechanisms of gut barrier failure in the pathogenesis of necrotizing enterocolitis: Toll-like receptors throw the switch

(2013) David J. Hackam et al.   Seminars in Pediatric Surgery

Toll-Like Receptor Signaling

(2013) K.-H. Lim et al.   Cold Spring Harbor Perspectives in Biology

Selection, synthesis, and anti-inflammatory evaluation of the arylidene malonate derivatives as TLR4 signaling inhibitors

(2012) Shuting Zhang et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Suppression of Toll-like receptor 4 activation by caffeic acid phenethyl ester is mediated by interference of LPS binding to MD2

(2012) So Young Kim et al.   BRITISH JOURNAL OF PHARMACOLOGY

Toll-like Receptor Signaling Pathways in Cardiovascular Diseases: Challenges and Opportunities

(2012) Faezeh Moghimpour Bijani et al.   INTERNATIONAL REVIEWS OF IMMUNOLOGY

CD14 Controls the LPS-Induced Endocytosis of Toll-like Receptor 4

(2011) Ivan Zanoni et al.   CELL

Studying protein–protein interactions using peptide arrays

(2011) Chen Katz et al.   CHEMICAL SOCIETY REVIEWS

Eritoran tetrasodium (E5564) treatment for sepsis: review of preclinical and clinical studies

(2011) Amisha Barochia et al.   Expert Opinion on Drug Metabolism & Toxicology

Development of β-Amino Alcohol Derivatives That Inhibit Toll-like Receptor 4 Mediated Inflammatory Response as Potential Antiseptics

(2011) Sherry A. Chavez et al.   JOURNAL OF MEDICINAL CHEMISTRY

Application of a novel in silico high-throughput screen to identify selective inhibitors for protein–protein interactions

(2010) Catherine Joce et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

SARM inhibits both TRIF- and MyD88-mediated AP-1 activation

(2010) Jun Peng et al.   EUROPEAN JOURNAL OF IMMUNOLOGY

MD-2 Residues Tyrosine 42, Arginine 69, Aspartic Acid 122, and Leucine 125 Provide Species Specificity for Lipid IVA

(2010) Jianmin Meng et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Determinants of BH3 Binding Specificity for Mcl-1 versus Bcl-xL

(2010) Sanjib Dutta et al.   JOURNAL OF MOLECULAR BIOLOGY

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

(2010) Taro Kawai et al.   NATURE IMMUNOLOGY

Interaction of the TNFR-Receptor Associated Factor TRAF1 with I-Kappa B Kinase-2 and TRAF2 Indicates a Regulatory Function for NF-Kappa B Signaling

(2010) Kalsoom Sughra et al.   PLoS One

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

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

Analysis of binding site for the novel small-molecule TLR4 signal transduction inhibitor TAK-242 and its therapeutic effect on mouse sepsis model

(2009) K Takashima et al.   BRITISH JOURNAL OF PHARMACOLOGY

Essential Roles of Hydrophobic Residues in Both MD-2 and Toll-like Receptor 4 in Activation by Endotoxin

(2009) Nuša Resman et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

The structural basis of lipopolysaccharide recognition by the TLR4–MD-2 complex

(2009) Beom Seok Park et al.   NATURE

Roles for LPS-dependent interaction and relocation of TLR4 and TRAM in TRIF-signaling

(2008) Natsuko Tanimura et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

Structures of the Toll-like Receptor Family and Its Ligand Complexes

(2008) Mi Sun Jin et al.   IMMUNITY

Activation of innate immunity system during aging: NF-kB signaling is the molecular culprit of inflamm-aging

(2007) Antero Salminen et al.   AGEING RESEARCH REVIEWS