Abstract Number: 514 • 2017 ACR/ARHP Annual Meeting
BMS-986195, a Novel, Rapidly Acting, Covalent Inhibitor of Bruton’s Tyrosine Kinase: Safety, Pharmacokinetic and Pharmacodynamic Profiles in Healthy Participants
Background/Purpose: Bruton’s tyrosine kinase (BTK) is an attractive, novel therapeutic target for autoimmune disease, as it is required for signal transduction and activation via B-cell…Abstract Number: 1320 • 2017 ACR/ARHP Annual Meeting
TAS5315, a Novel Bruton’s Tyrosine Kinase Inhibitor, Ameliorates Inflammation and Bone Erosion in Murine Model for Rheumatoid Arthritis
Background/Purpose: The erosions of bone and cartilage are a cardinal feature of rheumatoid arthritis (RA) and associated with disease severity and poor functional outcome. Although…Abstract Number: 1567 • 2017 ACR/ARHP Annual Meeting
A Mitogen-Associated Protein Kinase (MAPK) Associated Kinase 2 Inhibitor Decreases in Vitro Th17 and Monocyte Inflammatory Responses in Spondyloarthritis
Background/Purpose: The current biologic treatment for Ankylosing Spondylitis (AS) and Psoriatic Arthritis (PsA) are limited to TNF-a inhibitors (TNFi) and, more recently, IL-17A monoclonal antibodies.…Abstract Number: 2771 • 2017 ACR/ARHP Annual Meeting
NOMID-Associated Complications in Mice Are Prevented By CDD-450, a Small Molecule Inhibitor of the Mitogen-Activated Protein Kinase-Activated Protein Kinase 2 (MK2) Pathway
Background/Purpose: NLRP3-activating mutations cause cryopyrinopathies of which NOMID is the most severe phenotype. NLRP3 assembles a protein complex, responsible for the maturation of IL-1β and…Abstract Number: 460 • 2016 ACR/ARHP Annual Meeting
TAS5315, a Novel Bruton’s Tyrosine Kinase Inhibitor, Demonstrates Anti-Inflammatory Effect in Autoimmune Disease Models
Background/Purpose: Bruton’s Tyrosine Kinase (BTK), a non-receptor tyrosine kinase is involved in intracellular signaling pathways downstream of several receptors, including the B cell receptor (BCR),…Abstract Number: 1436 • 2016 ACR/ARHP Annual Meeting
TAS8274, a Highly Selective Janus Kinase 3 Inhibitor, Demonstrates Potent Efficacy in an Animal Model of Rheumatoid Arthritis
Background/Purpose: The family of Janus kinases (JAKs) plays important roles in signaling pathway mediated by various cytokine receptors. An aberrant activation of JAK-STAT signaling…Abstract Number: 2166 • 2014 ACR/ARHP Annual Meeting
Bim Suppresses the Development of Glomerulonephritis By Inhibiting M2 Polarization
Background/Purpose Only recently have monocytes and macrophages been accepted as critical players in the pathogenesis of SLE. However, very little is known regarding the molecular…Abstract Number: 1500 • 2014 ACR/ARHP Annual Meeting
Preclinical and Clinical Characterization of MK-8457, a Selective Spleen Tyrosine Kinase and Zeta-Chain-Associated Protein Kinase 70 Inhibitor, in Normotensive and Hypertensive Cardiovascular Models
Background/Purpose: Spleen Tyrosine Kinase (SYK) and Zeta-chain-associated protein kinase 70 (ZAP70) are non-receptor protein kinases that bind phosophorylated receptor tyrosine-based activation motifs, critical in immune…Abstract Number: 267 • 2014 ACR/ARHP Annual Meeting
Selective and Peripheral-Specific Trk Inhibitor Shows Potent Analgesic Effect Comparable to Morphine in Rat Osteoarthritis Model without CNS Toxicity
Background/Purpose Tropomyosin receptor kinase (Trk) receptors are a family of three closely related receptor tyrosine kinases; TrkA, TrkB and TrkC. Especially, the peripheral TrkA in…Abstract Number: 2562 • 2013 ACR/ARHP Annual Meeting
Inhibition Of SOX9 Phosphorylation Abrogates The Increased Expression Of Profibrotic Genes In Systemic Sclerosis Dermal Fibroblasts
Background/Purpose: SOX9, a high mobility group transcription factor is a master regulator of chondrogenesis and plays a crucial role in the regulation of chondrocyte gene…Abstract Number: 880 • 2012 ACR/ARHP Annual Meeting
Interferon Regulatory Factor 8 Regulates BAFF Production in Murine Macrophages and Is a Nexus for Cross Talk Between IFN-γ and TGF-β
Background/Purpose: Lupus is a systemic autoimmune disease that can lead to severe end-organ damage characterized by unabated inflammation and aberrant tissue repair. Macrophage dysregulation plays…Abstract Number: 882 • 2012 ACR/ARHP Annual Meeting
Anti-Inflammatory Effects of Phosphodiesterase 4 Inhibition Are Mediated by Mitogen-Activated Protein Kinase Phosphatase-1
Background/Purpose: MAP kinase phosphatase-1 (MKP-1) is a nuclear tyrosine/threonine phosphatase that limits p38 MAP kinase activity. MKP-1 KO mice display excessive inflammatory response, and exhibit…Abstract Number: 329 • 2012 ACR/ARHP Annual Meeting
The SYK Inhibitor, Fostamatinib, Administered Alone or in Combination with Methotrexate in Rat Collagen-Induced Arthritis, Reduces Bone Erosions, Biomarkers of Cartilage/Bone Destruction, and Synovial Osteoclastogenic Cytokines
Background/Purpose: Spleen tyrosine kinase (SYK) is expressed in hematopoietic cells and is a major downstream regulator of signaling through Fcγ and immunoglobulin receptors as well…Abstract Number: 2525 • 2012 ACR/ARHP Annual Meeting
Bruton’s Tyrosine Kinase Inhibition Suppresses Inflammatory Cytokine Production and Affects Gene Expression in Human Macrophages and RA Synovial Tissue Explants
Background/Purpose: Rheumatoid arthritis (RA) is a chronic and progressive autoinflammatory disorder characterized by the infiltration of inflammatory cells, including B-cells, T-cells and macrophages, in the…Abstract Number: 2332 • 2012 ACR/ARHP Annual Meeting
Suppression of PP2Ac Causes DNA Hypermethylation Through Enhanced Pmek/Perk Activity in T Cells
Background/Purpose: Although many reports have focused on the impaired MEK-ERK signaling pathway in T cells from systemic lupus erythematosus (SLE) patients which results in suppression…
ACR Meeting Abstracts