|
Lupus Erythematosus, Systemic
|
0.100 |
Biomarker
|
disease |
BEFREE |
Pharmacokinetic/pharmacodynamic modeling showed that mean BTK occupancy in blood cells of 80% was linked to near-complete disease inhibition in both RA and SLE mouse models.
|
30988116 |
2019 |
|
Lupus Erythematosus, Systemic
|
0.100 |
Biomarker
|
disease |
BEFREE |
As a result, pharmacological inhibition of BTK is anticipated to provide an effective strategy for the clinical treatment of autoimmune diseases such as rheumatoid arthritis and lupus.
|
30893553 |
2019 |
|
Lupus Erythematosus, Systemic
|
0.100 |
AlteredExpression
|
disease |
BEFREE |
Compared with controls, the frequency of Btk+ B cells in SLE patients was upregulated (p < 0.01), and it was significantly correlated with the SLE Disease Activity Index (SLEDAI) (p < 0.01), levels of plasma anti-dsDNA antibody (p < 0.05), the amount of 24-h urine protein (p < 0.05), and levels of plasma C3 (p < 0.05).
|
28612243 |
2018 |
|
Lupus Erythematosus, Systemic
|
0.100 |
Biomarker
|
disease |
BEFREE |
Overall, our results suggest that inhibition of BTK may be a promising therapeutic option for cutaneous and neuropsychiatric disease associated with SLE.
|
29370834 |
2018 |
|
Lupus Erythematosus, Systemic
|
0.100 |
AlteredExpression
|
disease |
BEFREE |
Preclinical studies have indicated that inhibition of Btk activity might offer a potential therapy in autoimmune diseases such as rheumatoid arthritis and systemic lupus erythematosus.
|
29457982 |
2018 |
|
Lupus Erythematosus, Systemic
|
0.100 |
GeneticVariation
|
disease |
BEFREE |
Because of this overwhelming evidence of a pathogenic role of BTK in autoimmunity, several clinical trials in rheumatoid arthritis and systemic lupus erythematosus patients with BTK inhibitors are currently running.
|
29717662 |
2018 |
|
Lupus Erythematosus, Systemic
|
0.100 |
AlteredExpression
|
disease |
BEFREE |
These findings reveal the mechanism through which a selective Btk inhibitor blocks murine autoimmune kidney disease, highlighting pathway activity that may translate to human SLE.
|
28405610 |
2017 |
|
Lupus Erythematosus, Systemic
|
0.100 |
GeneticVariation
|
disease |
BEFREE |
In our continued effort to discover and develop best-in-class Bruton's tyrosine kinase (Btk) inhibitors for the treatment of B-cell lymphomas, rheumatoid arthritis, and systemic lupus erythematosus, we devised a series of novel tricyclic compounds that improved upon the druglike properties of our previous chemical matter.
|
28626519 |
2017 |
|
Lupus Erythematosus, Systemic
|
0.100 |
Biomarker
|
disease |
BEFREE |
While Btk has not been associated with SLE in GWAS studies, SLE B cells display signaling defects in components both upstream and downstream of Btk consistent with enhanced activation of Btk signaling pathways.
|
29403475 |
2017 |
|
Lupus Erythematosus, Systemic
|
0.100 |
Biomarker
|
disease |
BEFREE |
We aimed to investigate the impact of therapeutic intervention with HM71224 (LY3337641), a selective BTK inhibitor, on the development of murine SLE-like disease features.
|
28950886 |
2017 |
|
Lupus Erythematosus, Systemic
|
0.100 |
AlteredExpression
|
disease |
BEFREE |
Multiple cytokines (interferon, B lymphocyte stimulator, IL-6, and IL-17), signaling pathways (Bruton's Tyrosine Kinase, Janus kinase/signal transducer and activator of transcription), and immune cells are dysregulated in SLE.
|
28118202 |
2017 |
|
Lupus Erythematosus, Systemic
|
0.100 |
Biomarker
|
disease |
BEFREE |
Since promising effects of BTK inhibition were also seen in experimental animal models for lupus and rheumatoid arthritis, BTK may be a good target for controlling autoreactive B cells in patients with systemic autoimmune disease.
|
26341110 |
2016 |
|
Lupus Erythematosus, Systemic
|
0.100 |
AlteredExpression
|
disease |
BEFREE |
Transgenic CD19-hBtk mice with B cell-specific BTK overexpression show spontaneous germinal center formation, anti-nuclear autoantibodies, and systemic autoimmunity resembling lupus and Sjögren syndrome.
|
27226091 |
2016 |
|
Lupus Erythematosus, Systemic
|
0.100 |
Biomarker
|
disease |
BEFREE |
Small molecules that block the kinases CaMKIV (calcium and calmodulin dependent kinase IV) and Bruton Tyrosine kinase (Btk) and the phosphatase calcineurin were shown to be effective in treating murine lupus.
|
21720246 |
2011 |