Differential impact of BTK active site inhibitors on the conformational state of full-length BTK
eLife, 2020 Bruton’s tyrosine kinase (BTK) is targeted in the treatment of B-cell disorders including leukemias and lymphomas. Currently approved BTK inhibitors, including Ibrutinib, a first-in-class covalent inhibitor of BTK, bind directly to the kinase active site.
Raji E Joseph +5 more
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Translational autoimmunity in pemphigus and the role of novel Bruton tyrosine kinase inhibitors
Journal of Translational Autoimmunity, 2022 Bruton tyrosine kinase (BTK) is involved in a multifarious inflammatory and autoimmune process. As a result, BTK has emerged as a promising novel remedial target for amalgamated autoimmune diseases.
Piyu Parth Naik
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The Use of Bruton Tyrosine Kinase Inhibitors in Waldenström’s Macroglobulinemia
Clinical Hematology International, 2022 The use of Bruton Tyrosine Kinase (BTK) inhibitors in Waldenström’s Macroglobulinemia (WM) is evolving. Ibrutinib, a first-generation BTK inhibitor, is currently approved for use in frontline and relapsed/refractory disease.
Obada Ababneh +4 more
doaj +1 more source
Frontiers in Pharmacology, 2022 Background: Bruton’s tyrosine kinase (BTK) inhibitors are commonly used in the targeted therapy of B-cell malignancies. It is reported that myelosuppression and fungal infections might occur during antitumor therapy of BTK inhibitors, therefore a ...
Lu Chen +5 more
doaj +1 more source
BTK inhibitors in the treatment of hematological malignancies and inflammatory diseases: mechanisms and clinical studies. [PDF]
J Hematol Oncol, 2022 Alu A, Lei H, Han X, Wei Y, Wei X.
europepmc +2 more sources
Structure of BTK kinase domain with the second-generation inhibitors acalabrutinib and tirabrutinib.
PLoS ONE, 2023 Bruton's tyrosine kinase (BTK) is the target of the therapeutic agent, Ibrutinib, that treats chronic lymphocyte leukemia (CLL), mantle cell lymphoma (MCL) and other B cell malignancies. Ibrutinib is a first in class, covalent BTK inhibitor that limits B-
David Y Lin, Amy H Andreotti
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Cross Fire: BTK Inhibitors Alone or in Combination are the Best Frontline Therapy for CLL
Hematology/Oncology and Stem Cell Therapy, 2023 BTK (Bruton's tyrosine kinase) inhibitors are highly effective front-line therapy for CLL (chronic lymphocytic leukemia) due to high response rates and prolonged progression-free survival, even in patients with high-risk disease features.
Theo Sottero, Farrukh T. Awan
doaj +1 more source
A Fast and Clean BTK Inhibitor [PDF]
Journal of Medicinal Chemistry, 2020 Bruton's tyrosine kinase (BTK) is a major drug target for B-cell related malignancies; however, existing BTK inhibitors approved for cancer treatment have significant off-targets that limit their use for autoimmune and inflammatory diseases. Remibrutinib (LOU064) is a novel covalent BTK inhibitor that binds an inactive BTK conformation, which affords ...
Ronen Gabizon, Nir London
openaire +2 more sources
Integrin Signaling Shaping BTK-Inhibitor Resistance
Cells, 2022 Integrins are adhesion molecules that function as anchors in retaining tumor cells in supportive tissues and facilitating metastasis. Beta1 integrins are known to contribute to cell adhesion-mediated drug resistance in cancer. Very late antigen-4 (VLA-4), a CD49d/CD29 heterodimer, is a beta1 integrin implicated in therapy resistance in both solid ...
Laura Polcik +5 more
openaire +4 more sources
Dasatinib inhibits CXCR4 signaling in chronic lymphocytic leukaemia cells and impairs migration towards CXCL12 [PDF]
, 2012 Chemokines and their ligands play a critical role in enabling chronic lymphocytic leukaemia (CLL) cells access to protective microenvironmental niches within tissues, ultimately resulting in chemoresistance and relapse: disruption of these signaling ...
A Hochhaus +38 more
core +5 more sources