Pharmacological Inhibitors of the NLRP3 Inflammasome

Nanobody: outstanding features for diagnostic and therapeutic applications

(2019) J.-Pablo Salvador et al.   ANALYTICAL AND BIOANALYTICAL CHEMISTRY

A novel small molecular NLRP3 inflammasome inhibitor alleviates neuroinflammatory response following traumatic brain injury

(2019) Ram Kuwar et al.   Journal of Neuroinflammation

MCC950 directly targets the NLRP3 ATP-hydrolysis motif for inflammasome inhibition

(2019) Rebecca C. Coll et al.   Nature Chemical Biology

Structural mechanism for NEK7-licensed activation of NLRP3 inflammasome

(2019) Humayun Sharif et al.   NATURE

Caspase-1 inhibition by VX-765 administered at reperfusion in P2Y12 receptor antagonist-treated rats provides long-term reduction in myocardial infarct size and preservation of ventricular function

(2018) Jonathon P. Audia et al.   BASIC RESEARCH IN CARDIOLOGY

The NLRP3 inflammasome: Role in metabolic disorders and regulation by metabolic pathways

(2018) Danlu Jiang et al.   CANCER LETTERS

Tranilast directly targets NLRP3 to treat inflammasome‐driven diseases

(2018) Yi Huang et al.   EMBO Molecular Medicine

GSDMD is critical for autoinflammatory pathology in a mouse model of Familial Mediterranean Fever

(2018) Apurva Kanneganti et al.   JOURNAL OF EXPERIMENTAL MEDICINE

Structural Insights of Benzenesulfonamide Analogues as NLRP3 Inflammasome Inhibitors: Design, Synthesis, and Biological Characterization

(2018) Jacob Fulp et al.   JOURNAL OF MEDICINAL CHEMISTRY

The NLRP3 Inflammasome Renders Cell Death Pro-inflammatory

(2018) Moritz M. Gaidt et al.   JOURNAL OF MOLECULAR BIOLOGY

Targeting the NLRP3 inflammasome in inflammatory diseases

(2018) Matthew S. J. Mangan et al.   NATURE REVIEWS DRUG DISCOVERY

OLT1177, a β-sulfonyl nitrile compound, safe in humans, inhibits the NLRP3 inflammasome and reverses the metabolic cost of inflammation

(2018) Carlo Marchetti et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Oridonin is a covalent NLRP3 inhibitor with strong anti-inflammasome activity

(2018) Hongbin He et al.   Nature Communications

Caspase-1 inhibition alleviates cognitive impairment and neuropathology in an Alzheimer’s disease mouse model

(2018) Joseph Flores et al.   Nature Communications

Inflammasome inhibition prevents α-synuclein pathology and dopaminergic neurodegeneration in mice

(2018) Richard Gordon et al.   Science Translational Medicine

Gasdermin D mediates the pathogenesis of neonatal-onset multisystem inflammatory disease in mice

(2018) Jianqiu Xiao et al.   PLOS BIOLOGY

Identification of a selective and direct NLRP3 inhibitor to treat inflammatory disorders

(2017) Hua Jiang et al.   JOURNAL OF EXPERIMENTAL MEDICINE

NLRP3 Inflammasome Inhibitor Ameliorates Amyloid Pathology in a Mouse Model of Alzheimer’s Disease

(2017) Jun Yin et al.   MOLECULAR NEUROBIOLOGY

The NLRP3 inflammasome in acute myocardial infarction

(2017) Stefano Toldo et al.   Nature Reviews Cardiology

Oridonin attenuates the release of pro-inflammatory cytokines in lipopolysaccharide-induced RAW264.7 cells and acute lung injury

(2017) Gan Zhao et al.   Oncotarget

Inflammasomes and Cancer

(2017) Rajendra Karki et al.   Cancer Immunology Research

Inflammasome-dependent IL-1β release depends upon membrane permeabilisation

(2016) F Martín-Sánchez et al.   CELL DEATH AND DIFFERENTIATION

Pore formation by GSDMD is the effector mechanism of pyroptosis

(2016) Moritz M Gaidt et al.   EMBO JOURNAL

Discovery and development of natural product oridonin-inspired anticancer agents

(2016) Ye Ding et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Efficacy and Pharmacology of the NLRP3 Inflammasome Inhibitor CP-456,773 (CRID3) in Murine Models of Dermal and Pulmonary Inflammation

(2016) Michael J. Primiano et al.   JOURNAL OF IMMUNOLOGY

Inflammasome-activated gasdermin D causes pyroptosis by forming membrane pores

(2016) Xing Liu et al.   NATURE

Fenamate NSAIDs inhibit the NLRP3 inflammasome and protect against Alzheimer’s disease in rodent models

(2016) Michael J. D. Daniels et al.   Nature Communications

Wogonoside protects against dextran sulfate sodium-induced experimental colitis in mice by inhibiting NF-κB and NLRP3 inflammasome activation

(2015) Yang Sun et al.   BIOCHEMICAL PHARMACOLOGY

Epithelial IL-18 Equilibrium Controls Barrier Function in Colitis

(2015) Roni Nowarski et al.   CELL

NLRP3 inflammasome in peripheral blood monocytes of acute coronary syndrome patients and its relationship with statins

(2015) Afrasyab Altaf et al.   CORONARY ARTERY DISEASE

Effect of enterohaemorrhagicEscherichia coliO157:H7-specific enterohaemolysin on interleukin-1βproduction differs between human and mouse macrophages due to the different sensitivity of NLRP3 activation

(2015) Yu-Li Cheng et al.   IMMUNOLOGY

Asiatic acid ameliorates dextran sulfate sodium-induced murine experimental colitis via suppressing mitochondria-mediated NLRP3 inflammasome activation

(2015) Wenjie Guo et al.   INTERNATIONAL IMMUNOPHARMACOLOGY

P2X7R is involved in the progression of atherosclerosis by promoting NLRP3 inflammasome activation

(2015) KUANG PENG et al.   INTERNATIONAL JOURNAL OF MOLECULAR MEDICINE

Pharmacologic Inhibition of the NLRP3 Inflammasome Preserves Cardiac Function After Ischemic and Nonischemic Injury in the Mouse

(2015) Carlo Marchetti et al.   JOURNAL OF CARDIOVASCULAR PHARMACOLOGY

Oridonin's therapeutic effect: Suppressing Th1/Th17 simultaneously in a mouse model of Crohn's disease

(2015) Shubei Wang et al.   JOURNAL OF GASTROENTEROLOGY AND HEPATOLOGY

Increased expression of the NLRP3 inflammasome components in patients with Behçet’s disease

(2015) En Hyung Kim et al.   Journal of Inflammation-London

The ketone metabolite β-hydroxybutyrate blocks NLRP3 inflammasome–mediated inflammatory disease

(2015) Yun-Hee Youm et al.   NATURE MEDICINE

A small-molecule inhibitor of the NLRP3 inflammasome for the treatment of inflammatory diseases

(2015) Rebecca C Coll et al.   NATURE MEDICINE

Tranilast: A review of its therapeutic applications

(2015) Sara Darakhshan et al.   PHARMACOLOGICAL RESEARCH

Role of innate immune system in systemic sclerosis

(2015) Nicola Fullard et al.   Seminars in Immunopathology

Mitochondria: diversity in the regulation of the NLRP3 inflammasome

(2015) Prajwal Gurung et al.   TRENDS IN MOLECULAR MEDICINE

Single-cell imaging of inflammatory caspase dimerization reveals differential recruitment to inflammasomes

(2015) M G Sanders et al.   Cell Death & Disease

Bruton’s tyrosine kinase is essential for NLRP3 inflammasome activation and contributes to ischaemic brain injury

(2015) Minako Ito et al.   Nature Communications

Mechanism of NLRP3 inflammasome activation

(2014) Fayyaz S. Sutterwala et al.   Annals of the New York Academy of Sciences

TXNIP mediates NLRP3 inflammasome activation in cardiac microvascular endothelial cells as a novel mechanism in myocardial ischemia/reperfusion injury

(2014) Yi Liu et al.   BASIC RESEARCH IN CARDIOLOGY

Activating Cannabinoid Receptor 2 Alleviates Pathogenesis of Experimental Autoimmune Encephalomyelitis Via Activation of Autophagy and Inhibiting NLRP3 Inflammasome

(2014) Bo-Zong Shao et al.   CNS Neuroscience & Therapeutics

The Lysosome Rupture-activated TAK1-JNK Pathway Regulates NLRP3 Inflammasome Activation

(2014) Masahiro Okada et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Cytosolic Double-Stranded RNA Activates the NLRP3 Inflammasome via MAVS-Induced Membrane Permeabilization and K+Efflux

(2014) Luigi Franchi et al.   JOURNAL OF IMMUNOLOGY

Inflammasome Priming by Lipopolysaccharide Is Dependent upon ERK Signaling and Proteasome Function

(2014) M. G. Ghonime et al.   JOURNAL OF IMMUNOLOGY

Intracellular Glutathione Depletion by Oridonin Leads to Apoptosis in Hepatic Stellate Cells

(2014) Liang-Mou Kuo et al.   MOLECULES

Antimicrobial Cathelicidin Peptide LL-37 Inhibits the LPS/ATP-Induced Pyroptosis of Macrophages by Dual Mechanism

(2014) Zhongshuang Hu et al.   PLoS One

Oridonin Attenuates Aβ1–42-Induced Neuroinflammation and Inhibits NF-κB Pathway

(2014) Sulei Wang et al.   PLoS One

Hematopoietic IKBKE limits the chronicity of inflammasome priming and metaflammation

(2014) Meghana N. Patel et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Inflammasomes in cancer: a double-edged sword

(2014) Ryan Kolb et al.   Protein & Cell

The anti-inflammatory drug BAY 11-7082 suppresses the MyD88-dependent signalling network by targeting the ubiquitin system

(2013) Sam Strickson et al.   BIOCHEMICAL JOURNAL

A novel benzo[d]imidazole derivate prevents the development of dextran sulfate sodium-induced murine experimental colitis via inhibition of NLRP3 inflammasome

(2013) Wen Liu et al.   BIOCHEMICAL PHARMACOLOGY

The anti-inflammatory compound BAY-11-7082 is a potent inhibitor of protein tyrosine phosphatases

(2013) Navasona Krishnan et al.   FEBS Journal

Human astrocytes express a novel NLRP2 inflammasome

(2013) Julia Minkiewicz et al.   GLIA

The role of interferon-β in the treatment of multiple sclerosis and experimental autoimmune encephalomyelitis - in the perspective of inflammasomes

(2013) Makoto Inoue et al.   IMMUNOLOGY

3,4-Methylenedioxy-β-nitrostyrene Inhibits NLRP3 Inflammasome Activation by Blocking Assembly of the Inflammasome

(2013) Yuan He et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

A Novel Pharmacologic Inhibitor of the NLRP3 Inflammasome Limits Myocardial Injury After Ischemia–Reperfusion in the Mouse

(2013) Carlo Marchetti et al.   JOURNAL OF CARDIOVASCULAR PHARMACOLOGY

Oridonin ameliorates neuropathological changes and behavioural deficits in a mouse model of cerebral amyloidosis

(2013) Zhi-Yuan Zhang et al.   JOURNAL OF CELLULAR AND MOLECULAR MEDICINE

Mitochondrial Reactive Oxygen Species Induces NLRP3-Dependent Lysosomal Damage and Inflammasome Activation

(2013) M. E. Heid et al.   JOURNAL OF IMMUNOLOGY

Treating inflammation by blocking interleukin-1 in humans

(2013) Charles A. Dinarello et al.   SEMINARS IN IMMUNOLOGY

Parthenolide generates reactive oxygen species and autophagy in MDA-MB231 cells. A soluble parthenolide analogue inhibits tumour growth and metastasis in a xenograft model of breast cancer

(2013) A D'Anneo et al.   Cell Death & Disease

Functions of NOD-Like Receptors in Human Diseases

(2013) Yifei Zhong et al.   Frontiers in Immunology

Upregulated NLRP3 Inflammasome Activation in Patients With Type 2 Diabetes

(2012) Hye-Mi Lee et al.   DIABETES

Non-transcriptional Priming and Deubiquitination Regulate NLRP3 Inflammasome Activation

(2012) Christine Juliana et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Deubiquitination of NLRP3 by BRCC3 Critically Regulates Inflammasome Activity

(2012) Bénédicte F. Py et al.   MOLECULAR CELL

Novel role of PKR in inflammasome activation and HMGB1 release

(2012) Ben Lu et al.   NATURE

Sensing and reacting to microbes through the inflammasomes

(2012) Luigi Franchi et al.   NATURE IMMUNOLOGY

NLRP3 has a protective role in age-related macular degeneration through the induction of IL-18 by drusen components

(2012) Sarah L Doyle et al.   NATURE MEDICINE

NLRP3 inflammasome induces chemotactic immune cell migration to the CNS in experimental autoimmune encephalomyelitis

(2012) M. Inoue et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Immunology in clinic review series; focus on autoinflammatory diseases: role of inflammasomes in autoinflammatory syndromes

(2011) V. U. Ozkurede et al.   CLINICAL AND EXPERIMENTAL IMMUNOLOGY

Interleukin-1 type 1 receptor/Toll-like receptor signalling in epilepsy: the importance of IL-1beta and high-mobility group box 1

(2011) M. Maroso et al.   JOURNAL OF INTERNAL MEDICINE

The Inflammasomes

(2010) Kate Schroder et al.   CELL

Anti-inflammatory Compounds Parthenolide and Bay 11-7082 Are Direct Inhibitors of the Inflammasome

(2010) Christine Juliana et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Nuocytes represent a new innate effector leukocyte that mediates type-2 immunity

(2010) Daniel R. Neill et al.   NATURE

NLRP3 inflammasomes are required for atherogenesis and activated by cholesterol crystals

(2010) Peter Duewell et al.   NATURE

Activation of the NLRP3 inflammasome by islet amyloid polypeptide provides a mechanism for enhanced IL-1β in type 2 diabetes

(2010) Seth L Masters et al.   NATURE IMMUNOLOGY

IKK inhibitor bay 11-7082 induces necroptotic cell death in precursor-B acute lymphoblastic leukaemic blasts

(2009) Xiangbing Meng et al.   BRITISH JOURNAL OF HAEMATOLOGY

Multiple-modulation effects of Oridonin on the production of proinflammatory cytokines and neurotrophic factors in LPS-activated microglia

(2009) Yan Xu et al.   INTERNATIONAL IMMUNOPHARMACOLOGY

Vinyl Sulfones as Antiparasitic Agents and a Structural Basis for Drug Design

(2009) Iain D. Kerr et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Glyburide inhibits the Cryopyrin/Nalp3 inflammasome

(2009) Mohamed Lamkanfi et al.   JOURNAL OF CELL BIOLOGY

Cutting Edge: NF- B Activating Pattern Recognition and Cytokine Receptors License NLRP3 Inflammasome Activation by Regulating NLRP3 Expression

(2009) F. G. Bauernfeind et al.   JOURNAL OF IMMUNOLOGY

Randomized controlled trial design in rheumatoid arthritis: the past decade

(2009) Vibeke Strand et al.   ARTHRITIS RESEARCH & THERAPY

Thiazolidinone CFTR inhibitors with improved water solubility identified by structure–activity analysis

(2008) N.D. Sonawane et al.   BIOORGANIC & MEDICINAL CHEMISTRY

The NALP3 inflammasome is involved in the innate immune response to amyloid-β

(2008) Annett Halle et al.   NATURE IMMUNOLOGY