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

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

(2019) Florent Cochet et al.   Scientific Reports

The TLR4 agonist adjuvant SLA-SE promotes functional mucosal antibodies against a parenterally delivered ETEC vaccine

(2019) Hong Liang et al.   npj Vaccines

Saturation of acyl chains converts cardiolipin from an antagonist to an activator of Toll-like receptor-4

(2019) Malvina Pizzuto et al.   CELLULAR AND MOLECULAR LIFE SCIENCES

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

Regulation of Toll-Like Receptor (TLR) Signaling Pathway by Polyphenols in the Treatment of Age-Linked Neurodegenerative Diseases: Focus on TLR4 Signaling

(2019) Shofiul Azam et al.   Frontiers in Immunology

Ferulic acid inhibits bovine endometrial epithelial cells against LPS-induced inflammation via suppressing NK-κB and MAPK pathway

(2019) Peng Yin et al.   RESEARCH IN VETERINARY SCIENCE

Aminosugar-based immunomodulator lipid A: synthetic approaches

(2018) Alla Zamyatina   Beilstein Journal of Organic Chemistry

Ferulic acid protects lipopolysaccharide-induced acute kidney injury by suppressing inflammatory events and upregulating antioxidant defenses in Balb/c mice

(2018) Salma Mukhtar Mir et al.   BIOMEDICINE & PHARMACOTHERAPY

Co-administration of Antimicrobial Peptides Enhances Toll-like Receptor 4 Antagonist Activity of a Synthetic Glycolipid

(2018) Fabio A. Facchini et al.   ChemMedChem

Rational design of novel TLR4 ligands by in silico screening and their functional and structural characterization in vitro

(2018) Jan Honegr et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Recent advances on Toll-like receptor 4 modulation: new therapeutic perspectives

(2018) Lenny Zaffaroni et al.   Future Medicinal 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

Selective Toll-Like Receptor 4 Antagonists Prevent Acute Blood-Brain Barrier Disruption After Subarachnoid Hemorrhage in Mice

(2018) Takeshi Okada et al.   MOLECULAR NEUROBIOLOGY

Rational Design of a New Class of Toll-Like Receptor 4 (TLR4) Tryptamine Related Agonists by Means of the Structure- and Ligand-Based Virtual Screening for Vaccine Adjuvant Discovery

(2018) Jan Honegr et al.   MOLECULES

Molecular structural diversity of mitochondrial cardiolipins

(2018) Gregor Oemer et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

A Thermodynamic Funnel Drives Bacterial Lipopolysaccharide Transfer in the TLR4 Pathway

(2018) Roland G. Huber et al.   STRUCTURE

A lipid A-based TLR4 mimetic effectively adjuvants a Yersinia pestis rF-V1 subunit vaccine in a murine challenge model

(2018) Kelsey A. Gregg et al.   VACCINE

Synthetic glycan-based TLR4 agonists targeting caspase-4/11 for the development of adjuvants and immunotherapeutics

(2018) Florian Adanitsch et al.   Chemical Science

Molecular Signatures of a TLR4 Agonist-Adjuvanted HIV-1 Vaccine Candidate in Humans

(2018) Jenna Anderson et al.   Frontiers in Immunology

The synthetic glycolipid-based TLR4 antagonist FP7 negatively regulates in vitro and in vivo haematopoietic and non-haematopoietic vascular TLR4 signalling

(2018) Charys Palmer et al.   Innate Immunity

Alpinetin ameliorates inflammatory response in LPS-induced endometritis in mice

(2018) Yuanjiao Liang et al.   INTERNATIONAL IMMUNOPHARMACOLOGY

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

(2018) Shafiq Ur Rehman et al.   MOLECULAR NEUROBIOLOGY

Disaccharide-Based Anionic Amphiphiles as Potent Inhibitors of Lipopolysaccharide-Induced Inflammation

(2018) Alessio Borio et al.   ChemMedChem

Computationally Designed Bispecific MD2/CD14 Binding Peptides Show TLR4 Agonist Activity

(2018) Amit Michaeli et al.   JOURNAL OF IMMUNOLOGY

Recent clinical trends in Toll-like receptor targeting therapeutics

(2018) Muhammad Ayaz Anwar et al.   MEDICINAL RESEARCH REVIEWS

Protective effects of alpinetin on lipopolysaccharide/d-Galactosamine-induced liver injury through inhibiting inflammatory and oxidative responses

(2018) Tong-gang Liu et al.   MICROBIAL PATHOGENESIS

E6020, a synthetic TLR4 agonist, accelerates myelin debris clearance, Schwann cell infiltration, and remyelination in the rat spinal cord

(2017) Jamie S. Church et al.   GLIA

Reconstruction of LPS Transfer Cascade Reveals Structural Determinants within LBP, CD14, and TLR4-MD2 for Efficient LPS Recognition and Transfer

(2017) Je-Kyung Ryu et al.   IMMUNITY

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

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

Synthetic Toll-Like Receptor 4 (TLR4) and TLR7 Ligands Work Additively via MyD88 To Induce Protective Antiviral Immunity in Mice

(2017) Peter H. Goff et al.   JOURNAL OF VIROLOGY

An Overview of Novel Adjuvants Designed for Improving Vaccine Efficacy

(2017) Srinivasa Reddy Bonam et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Rationally Designed TLR4 Ligands for Vaccine Adjuvant Discovery

(2017) Kelsey A. Gregg et al.   mBio

Monophosphoryl lipid a attenuates radiation injury through TLR4 activation

(2017) Jiaming Guo et al.   Oncotarget

TLR4-Mediated Placental Pathology and Pregnancy Outcome in Experimental Malaria

(2017) Renato Barboza et al.   Scientific Reports

TLR4 antagonist FP7 inhibits LPS-induced cytokine production and glycolytic reprogramming in dendritic cells and protects mice from lethal influenza infection

(2017) Laure Perrin-Cocon et al.   Scientific Reports

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

Bacterial Outer Membrane Vesicles Mediate Cytosolic Localization of LPS and Caspase-11 Activation

(2016) Sivapriya Kailasan Vanaja et al.   CELL

Glycolipid-based TLR4 Modulators and Fluorescent Probes: Rational Design, Synthesis, and Biological Properties

(2016) Carlotta Ciaramelli et al.   Chemical Biology & Drug Design

The molecular events behind ferulic acid mediated modulation of IL-6 expression in LPS-activated Raw 264.7 cells

(2016) Nadia Lampiasi et al.   IMMUNOBIOLOGY

Intratumoral Delivery of Immunotherapy—Act Locally, Think Globally

(2016) M. Angela Aznar et al.   JOURNAL OF IMMUNOLOGY

Synthetic and natural small molecule TLR4 antagonists inhibit motoneuron death in cultures from ALS mouse model

(2016) Massimiliano De Paola et al.   PHARMACOLOGICAL RESEARCH

Postulates for validating TLR4 agonists

(2015) Mateja Manček-Keber et al.   EUROPEAN JOURNAL OF IMMUNOLOGY

Synthetic Toll-Like Receptor 4 (TLR4) and TLR7 Ligands as Influenza Virus Vaccine Adjuvants Induce Rapid, Sustained, and Broadly Protective Responses

(2015) Peter H. Goff et al.   JOURNAL OF VIROLOGY

Molecular simplification of lipid A structure: TLR4-modulating cationic and anionic amphiphiles

(2015) Valentina Calabrese et al.   MOLECULAR IMMUNOLOGY

DAT isn’t all that: cocaine reward and reinforcement require Toll-like receptor 4 signaling

(2015) A L Northcutt et al.   MOLECULAR PSYCHIATRY

Dichotomous roles for externalized cardiolipin in extracellular signaling: Promotion of phagocytosis and attenuation of innate immunity

(2015) Krishnakumar Balasubramanian et al.   Science Signaling

Dichotomous roles for externalized cardiolipin in extracellular signaling: Promotion of phagocytosis and attenuation of innate immunity

(2015) Krishnakumar Balasubramanian et al.   Science Signaling

Trial Watch: Immunostimulation with Toll-like receptor agonists in cancer therapy

(2015) Kristina Iribarren et al.   OncoImmunology

Chemistry of Lipid A: At the Heart of Innate Immunity

(2014) Antonio Molinaro et al.   CHEMISTRY-A EUROPEAN JOURNAL

The attenuated inflammation of MPL is due to the lack of CD14-dependent tight dimerization of the TLR4/MD2 complex at the plasma membrane

(2014) Natsuko Tanimura et al.   INTERNATIONAL IMMUNOLOGY

Elucidation of the MD-2/TLR4 Interface Required for Signaling by Lipid IVa

(2014) C. Walsh et al.   JOURNAL OF IMMUNOLOGY

High Mobility Group Box 1 Protein Binding to Lipopolysaccharide Facilitates Transfer of Lipopolysaccharide to CD14 and Enhances Lipopolysaccharide-Mediated TNF-  Production in Human Monocytes

(2014) J. H. Youn et al.   JOURNAL OF IMMUNOLOGY

Glucopyranosyl Lipid A Adjuvant Significantly Enhances HIV Specific T and B Cell Responses Elicited by a DNA-MVA-Protein Vaccine Regimen

(2014) Paul F. McKay et al.   PLoS One

Toll-Like Receptor-4 Modulation for Cancer Immunotherapy

(2014) Shanjana Awasthi   Frontiers in Immunology

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

(2013) Roberto Cighetti et al.   CHEMBIOCHEM

Alpinetin inhibits LPS-induced inflammatory mediator response by activating PPAR-γ in THP-1-derived macrophages

(2013) Ke Hu et al.   EUROPEAN JOURNAL OF PHARMACOLOGY

Identification of Substituted Pyrimido[5,4-b]indoles as Selective Toll-Like Receptor 4 Ligands

(2013) Michael Chan et al.   JOURNAL OF MEDICINAL CHEMISTRY

The TLR4 antagonist Eritoran protects mice from lethal influenza infection

(2013) Kari Ann Shirey et al.   NATURE

Modulating the innate immune response by combinatorial engineering of endotoxin

(2013) Brittany D. Needham et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Cytoplasmic LPS Activates Caspase-11: Implications in TLR4-Independent Endotoxic Shock

(2013) J. A. Hagar et al.   SCIENCE

Cationic lipids activate intracellular signaling pathways

(2012) Caroline Lonez et al.   ADVANCED DRUG DELIVERY REVIEWS

Biological applications of functionalized calixarenes

(2012) Satish Balasaheb Nimse et al.   CHEMICAL SOCIETY REVIEWS

Glucopyranosyl Lipid Adjuvant (GLA), a Synthetic TLR4 Agonist, Promotes Potent Systemic and Mucosal Responses to Intranasal Immunization with HIVgp140

(2012) Mauricio A. Arias et al.   PLoS One

Spotlight on AS04-Adjuvanted Human Papillomavirus (HPV) Types 16 and 18 Vaccine (Cervarix®)†

(2011) Kate McKeage et al.   BIODRUGS

Traditional medicine alpinetin inhibits the inflammatory response in Raw 264.7 cells and mouse models

(2011) Meixia Huo et al.   INTERNATIONAL IMMUNOPHARMACOLOGY

Development and Characterization of Synthetic Glucopyranosyl Lipid Adjuvant System as a Vaccine Adjuvant

(2011) Rhea N. Coler et al.   PLoS One

The cationic amphiphile 3,4-bis(tetradecyloxy)benzylamine inhibits LPS signaling by competing with endotoxin for CD14 binding

(2010) Matteo Piazza et al.   BIOCHEMICAL PHARMACOLOGY

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

Toll-Like Receptor Signaling Pathways—Therapeutic Opportunities

(2010) Jiankun Zhu et al.   MEDIATORS OF INFLAMMATION

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

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

Physicochemical characterization and biological activity of synthetic TLR4 agonist formulations

(2009) Ryan C. Anderson et al.   COLLOIDS AND SURFACES B-BIOINTERFACES

Glycolipids and Benzylammonium Lipids as Novel Antisepsis Agents: Synthesis and Biological Characterization

(2009) Matteo Piazza et al.   JOURNAL OF MEDICINAL CHEMISTRY

Putting endotoxin to work for us: Monophosphoryl lipid A as a safe and effective vaccine adjuvant

(2008) C. R. Casella et al.   CELLULAR AND MOLECULAR LIFE SCIENCES