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Bruton’s tyrosine kinase-bearing B cells and microglia in neuromyelitis optica spectrum disorder
BackgroundNeuromyelitis optica spectrum disorder (NMOSD) is an inflammatory autoimmune disease of the central nervous system that involves B-cell...
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Bruton’s tyrosine kinase inhibition reduces disease severity in a model of secondary progressive autoimmune demyelination
Bruton’s tyrosine kinase (BTK) is an emerging target in multiple sclerosis (MS). Alongside its role in B cell receptor signaling and B cell...
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Pirtobrutinib inhibits wild-type and mutant Bruton’s tyrosine kinase-mediated signaling in chronic lymphocytic leukemia
Pirtobrutinib (LOXO-305), a reversible inhibitor of Bruton’s tyrosine kinase (BTK), was designed as an alternative strategy to treat...
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Bruton’s tyrosine kinase drives neuroinflammation and anxiogenic behavior in mouse models of stress
BackgroundCurrent therapies targeting several neurotransmitter systems are only able to partially mitigate the symptoms of stress- and trauma-related...
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Tyrosine kinase inhibitor–induced hypothyroidism: mechanism and clinical implications
IntroductionSince the first experimentally proven tyrosine kinase inhibitor (TKI) imatinib was introduced in the clinical setting, TKIs have...
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Profiling tyrosine kinase inhibitors as AD therapeutics in a mouse model of AD
Alzheimer’s disease (AD) is a neurodegenerative disease characterized by Aβ deposition, tauopathy, neuroinflammation, and impaired cognition. The...
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Impact of therapeutic inhibition of oncogenic cell signaling tyrosine kinase on cell metabolism: in vivo-detectable metabolic biomarkers of inhibition
BackgroundInhibition of kinases is the ever-expanding therapeutic approach to various types of cancer. Typically, assessment of the treatment...
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Tyrosine Kinases: Targets for Epigenetic Influences and a New Direction in the Treatment of Multiple Sclerosis
Studies have shown that tyrosine kinases (TK) may play an important role in the pathogenesis of multiple sclerosis (MS) operating through a microRNA...
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An Open Label, Phase 1, Randomized, Seven-treatment, Seven-period, Crossover Study to Assess the Relative Bioavailability, pH Effect, Food Effect, and Dose Proportionality of CC-292, a Potent and Orally Available Bruton’s Tyrosine Kinase Inhibitor
Background and ObjectiveCC-292 is a potent, selective, orally administered small molecule inhibitor of Bruton’s tyrosine kinase (BTK). To support the...
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Enhancing therapeutic anti-cancer responses by combining immune checkpoint and tyrosine kinase inhibition
Over the past decade, immune checkpoint inhibitor (ICI) therapy has been established as the standard of care for many types of cancer, but the...
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Aberrantly expressed Bruton’s tyrosine kinase preferentially drives metastatic and stem cell-like phenotypes in neuroblastoma cells
PurposeNeuroblastoma, a common childhood tumor, remains one of the most elusive diseases to treat. To date, high-risk neuroblastoma is associated...
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Targeted selective degradation of Bruton’s tyrosine kinase by PROTACs
Bruton’s tyrosine kinase (BTK) is critical for B-cell receptor signaling and related to many types of human cancers. However, the drug resistance and...
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Epoxyquinophomopsins A and B from endophytic fungus Phomopsis sp. and their activity against tyrosine kinase
Two new quinone derivatives, epoxyquinophomopsins A ( 1 ) and B ( 2 ), were purified from the EtOAc extract of endophytic fungus Phomopsis sp isolated...
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Differential Inhibition of Equilibrative Nucleoside Transporter 1 (ENT1) Activity by Tyrosine Kinase Inhibitors
Background and ObjectivesEquilibrative nucleoside transporter (ENT) 1 is a widely-expressed drug transporter, handling nucleoside analogues as well...
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Protein kinases: drug targets for immunological disorders
Protein kinases play a major role in cellular activation processes, including signal transduction by diverse immunoreceptors. Given their roles in...
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Iguratimod suppresses plasma cell differentiation and ameliorates experimental Sjögren’s syndrome in mice by promoting TEC kinase degradation
Primary Sjögren’s syndrome (pSS) is a chronic inflammatory autoimmune disease with an unclear pathogenesis, and there is currently no approved drug...
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NLRP3 Phospho-residue Mapping by Phospho Dot Blots
When characterizing posttranslational modifications like phosphorylation, using efficient screening methods to map the phospho sites is essential,...
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Small molecule tyrosine kinase inhibitors modulated blood immune cell counts in patients with oncogene-driven NSCLC
BackgroundLack of biomarkers and in vitro models has contributed to inadequate understanding of the mechanisms underlying the inferior clinical...
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T-cell expression of Bruton’s tyrosine kinase promotes autoreactive T-cell activation and exacerbates aplastic anemia
The role of Bruton’s tyrosine kinase (BTK) in BCR signaling is well defined, and BTK is involved in B-cell development, differentiation, and...
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Update on the management of relapsed/refractory chronic lymphocytic leukemia
Chronic lymphocytic leukemia (CLL) predominantly affects older adults, characterized by a relapsing and remitting pattern with sequential treatments...
