Search Results - "Cenni, Bruno"
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Discovery of LOU064 (Remibrutinib), a Potent and Highly Selective Covalent Inhibitor of Bruton’s Tyrosine Kinase
Published in Journal of medicinal chemistry (28-05-2020)“…Bruton’s tyrosine kinase (BTK), a cytoplasmic tyrosine kinase, plays a central role in immunity and is considered an attractive target for treating autoimmune…”
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Remibrutinib (LOU064): A selective potent oral BTK inhibitor with promising clinical safety and pharmacodynamics in a randomized phase I trial
Published in Clinical and translational science (01-09-2021)“…Safe and effective new oral therapies for autoimmune, allergic, and inflammatory conditions remain a significant therapeutic need. Here, we investigate the…”
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Remibrutinib (LOU064) inhibits neuroinflammation driven by B cells and myeloid cells in preclinical models of multiple sclerosis
Published in Journal of neuroinflammation (26-08-2023)“…Abstract Background Bruton’s tyrosine kinase (BTK) is a key signaling node in B cell receptor (BCR) and Fc receptor (FcR) signaling. BTK inhibitors (BTKi) are…”
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Endothelial Bmx tyrosine kinase activity is essential for myocardial hypertrophy and remodeling
Published in Proceedings of the National Academy of Sciences - PNAS (20-10-2015)“…Cardiac hypertrophy accompanies many forms of heart disease, including ischemic disease, hypertension, heart failure, and valvular disease, and it is a strong…”
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Remibrutinib inhibits hives effector cells stimulated by serum from chronic urticaria patients independently of FcεR1 expression level and omalizumab clinical response
Published in Clinical and translational allergy (01-03-2023)“…Background Despite advances in the treatment of chronic urticaria, in a significant percentage of the patients symptoms are not fully controlled with…”
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The Lysosomal Transmembrane Protein 9B Regulates the Activity of Inflammatory Signaling Pathways
Published in The Journal of biological chemistry (01-08-2008)“…The intracellular signaling pathway by which tumor necrosis factor (TNF) induces its pleiotropic actions is well characterized and includes unique components…”
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Remibrutinib, a Novel Bruton’s Tyrosine Kinase Inhibitor, Exhibits Improved Target Selectivity and Potency In Vitro (P8-3.003)
Published in Neurology (25-04-2023)“…Abstract only…”
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Remibrutinib Inhibits Neuroinflammation Driven by B Cells and Myeloid Cells in Preclinical Models of Multiple Sclerosis (P2-3.013)
Published in Neurology (25-04-2023)“…Abstract only…”
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Meta-analysis for Neurofilament Light Chain as a Biomarker in Mouse Experimental Autoimmune Encephalomyelitis Studies (S17.008)
Published in Neurology (09-04-2024)“…Abstract only…”
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BMX and Its Role in Inflammation, Cardiovascular Disease, and Cancer
Published in International Reviews of Immunology (01-04-2012)“…Bone marrow kinase on chromosome X (BMX) is a cytosolic tyrosine kinase and a member of the TEC kinase family. BMX is expressed in hematopoietic cells of the…”
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Efficacy and safety of remibrutinib, a selective potent oral BTK inhibitor, in Sjögren's syndrome: results from a randomised, double-blind, placebo-controlled phase 2 trial
Published in Annals of the rheumatic diseases (01-03-2024)“…To evaluate the safety and efficacy of remibrutinib in patients with moderate-to-severe Sjögren's syndrome (SjS) in a phase 2 randomised, double-blind trial…”
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Remibrutinib, a Novel Bruton Tyrosine Kinase Inhibitor, Exhibits Improved Target Selectivity and Potency in Vitro
Published in Multiple sclerosis and related disorders (01-12-2023)“…Several Bruton's tyrosine kinase inhibitors (BTKis) are in clinical development for multiple sclerosis (MS). In human blood, in vitro binding of covalent…”
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Safety of Remibrutinib Across Immune-mediated Diseases Supports Development in Multiple Sclerosis (P8-6.015)
Published in Neurology (09-04-2024)“…Abstract only…”
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Estradiol Decreases IGF-1 and IGF-1 Receptor Expression in Rat Aortic Smooth Muscle Cells
Published in The Journal of biological chemistry (08-12-2000)“…Insulin-like growth factor (IGF-1) is a potent mitogen for vascular smooth muscle cells. Both IGF-1 and its receptor have been shown to be highly expressed in…”
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Remibrutinib: A Novel BTKi in Development for MS With a Favorable Safety Profile in Various Autoimmune Disorders (P7-3.015)
Published in Neurology (25-04-2023)“…Abstract only…”
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CARM1 mediates the ligand-independent and tamoxifen-resistant activation of the estrogen receptor alpha by cAMP
Published in Genes & development (01-04-2010)“…The estrogen receptor alpha (ERalpha) is activated as a transcription factor by both estrogen and a large variety of other extracellular signals. The…”
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Design of Potent and Selective Covalent Inhibitors of Bruton’s Tyrosine Kinase Targeting an Inactive Conformation
Published in ACS medicinal chemistry letters (10-10-2019)“…Bruton’s tyrosine kinase (BTK) is a member of the TEC kinase family and is selectively expressed in a subset of immune cells. It is a key regulator of antigen…”
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Evaluation of protease‐activated receptor 2 in murine models of arthritis
Published in Arthritis and rheumatism (01-01-2007)“…Objective Protease‐activated receptor 2 (PAR‐2) activation has been linked to pro‐ and antiinflammatory cellular responses. We undertook this study to explore…”
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The tyrosine kinase BMX is an essential mediator of inflammatory arthritis in a kinase-independent manner
Published in The Journal of immunology (1950) (15-05-2011)“…Inflammatory cytokines like TNF play a central role in autoimmune disorders such as rheumatoid arthritis. We identified the tyrosine kinase bone marrow kinase…”
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The in vitro distribution of halofantrine in human blood and Plasmodium falciparum-parasitised red blood cells
Published in Chemotherapy (Basel) (1995)“…The in vitro distribution of the antimalarial drug halofantrine was measured in drug-preincubated whole blood after separation of the blood cells from the…”
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