TP53‐altered chronic lymphocytic leukemia treated with firstline Bruton's tyrosine kinase inhibitor‐based therapy: A retrospective analysis
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DOI: 10.1002/ajh.26595
Abstract: Long‐term follow up of prospective studies has shown that continuous Bruton's tyrosine kinase inhibitor (BTKi) therapy leads to durable remissions in previously untreated patients with TP53‐altered chronic lymphocytic leukemia (CLL); however, it is unknown how… read more here.
Keywords: tp53 altered; bruton tyrosine; inhibitor; kinase inhibitor ... See more keywords
Bruton tyrosine kinase inhibitors in the management of Waldenström macroglobulinemia
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DOI: 10.1002/ajh.26788
Abstract: Bruton tyrosine kinase (BTK) inhibitors have taken a central role in the management of patients with Waldenström macroglobulinemia and are the only agents approved by the Food and Drug Administration (FDA) to treat these patients.… read more here.
Keywords: bruton tyrosine; management; tyrosine kinase; waldenstr macroglobulinemia ... See more keywords
Bruton's tyrosine kinase inhibition induces rewiring of proximal and distal B‐cell receptor signaling in mice
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DOI: 10.1002/eji.202048968
Abstract: Bruton′s tyrosine kinase (Btk) is a crucial signaling molecule in BCR signaling and a key regulator of B‐ cell differentiation and function. Btk inhibition has shown impressive clinical efficacy in various B‐cell malignancies. However, it… read more here.
Keywords: kinase; bruton tyrosine; inhibition; bcr signaling ... See more keywords
Drug interactions with Bruton’s tyrosine kinase inhibitors: clinical implications and management
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DOI: 10.1007/s00280-020-04137-6
Abstract: Bruton’s tyrosine kinase (BTK) plays an essential role in B-cell development, differentiation and B-cell receptor (BCR) signaling. The use of Bruton’s tyrosine kinase inhibitors (BTKi) in the treatment of lymphoid malignancies has dramatically increased, owing… read more here.
Keywords: kinase inhibitors; drug drug; drug; bruton tyrosine ... See more keywords
The development of Bruton's tyrosine kinase (BTK) inhibitors from 2012 to 2017: A mini-review.
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DOI: 10.1016/j.ejmech.2018.03.062
Abstract: Bruton's tyrosine kinase (BTK) has emerged as a promising drug target for multiple diseases, particularly haematopoietic malignancies and autoimmune diseases related to B lymphocytes. This review focuses on the diverse, small-molecule inhibitors of BTK kinase… read more here.
Keywords: btk; kinase btk; btk inhibitors; bruton tyrosine ... See more keywords
Discovery of potent and highly selective covalent inhibitors of Bruton's tyrosine kinase bearing triazine scaffold.
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DOI: 10.1016/j.ejmech.2020.112339
Abstract: Bruton's tyrosine kinase (BTK), as a key regulator of the B cell receptor (BCR) signaling pathway, is an attractive therapeutic target for the treatment of various diseases such as leukemia and B-cell malignancies. Herein, a… read more here.
Keywords: bearing triazine; discovery potent; kinase; btk ... See more keywords
Emerging small-molecule inhibitors of the Bruton's tyrosine kinase (BTK): Current development.
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DOI: 10.1016/j.ejmech.2021.113329
Abstract: Therapy based on Bruton's tyrosine kinase (BTK) inhibitors one of the major treatment options currently recommended for lymphoma patients. The first generation of BTK inhibitor, Ibrutinib, achieved remarkable progress in the treatment of B-cell malignancies,… read more here.
Keywords: development; btk; kinase btk; btk inhibitors ... See more keywords
First-Generation and Second-Generation Bruton Tyrosine Kinase Inhibitors in Waldenström Macroglobulinemia.
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DOI: 10.1016/j.hoc.2018.05.012
Abstract: Waldenström macroglobulinemia (WM) is an indolent B-cell lymphoma that is heavily dependent on Bruton tyrosine kinase (BTK) hyperactivation. Ibrutinib is a first-generation BTK inhibitor that has shown high activity and durable responses in patients with… read more here.
Keywords: first generation; waldenstr macroglobulinemia; generation; second generation ... See more keywords
Targeting the C481S Ibrutinib-Resistance Mutation in Bruton's Tyrosine Kinase Using PROTAC-Mediated Degradation.
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DOI: 10.1021/acs.biochem.8b00391
Abstract: Inhibition of Bruton's tyrosine kinase (BTK) with the irreversible inhibitor ibrutinib has emerged as a transformative treatment option for patients with chronic lymphocytic leukemia (CLL) and other B-cell malignancies, yet >80% of CLL patients develop… read more here.
Keywords: degradation; protac; btk; bruton tyrosine ... See more keywords
Discovery of BIIB068: A Selective, Potent, Reversible Bruton's Tyrosine Kinase Inhibitor as an Orally Efficacious Agent for Autoimmune Diseases.
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DOI: 10.1021/acs.jmedchem.0c00702
Abstract: Autoreactive B cell-derived antibodies form immune-complexes that likely play a pathogenic role in autoimmune diseases. In Systemic Lupus Erythematosus (SLE), these antibodies bind Fc receptors on myeloid cells and induce proinflammatory cytokine production by monocytes… read more here.
Keywords: potent reversible; kinase; autoimmune diseases; bruton tyrosine ... See more keywords
Discovery of AS-1763: A Potent, Selective, Noncovalent, and Orally Available Inhibitor of Bruton's Tyrosine Kinase.
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DOI: 10.1021/acs.jmedchem.1c01279
Abstract: Although Bruton's tyrosine kinase (BTK) has been recognized as a validated drug target for the treatment of B-cell malignances, the emergence of clinical resistance to the first-generation covalent BTK inhibitors is becoming a serious concern.… read more here.
Keywords: potent selective; inhibitor; btk; orally available ... See more keywords