Corrigendum: Discovery of a Potent BTK Inhibitor with a Novel Binding Mode by Using Parallel Selections with a DNAEncoded Chemical Library
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DOI: 10.1002/cbic.201700610
Abstract: The authors would like to acknowledge Andreas Kuglstatter and Christine Lukacs (Roche Pharma Research and Early Development), who provided an initial analysis of the binding mode of compound 3 in relation to Roche compound RN486… read more here.
Keywords: mode; discovery potent; corrigendum discovery; potent btk ... See more keywords
MOLECULAR MECHANISMS AND COMBINATION STRATEGIES WITH PI3K AND BTK INHIBITORS TO OVERCOME INTRINSIC AND ACQUIRED RESISTANCE IN PRECLINICAL MODELS OF ABC‐DLBCL
Sign Up to like & getrecommendations! Published in 2017 at "Hematological Oncology"
DOI: 10.1002/hon.2439_179
Abstract: The Bruton's tyrosine kinase (Btk) inhibitor ibrutinib has demonstrated promising efficacy in a variety of hematologic malignancies. However, the precise mechanism of action of the drug remains to be fully elucidated. Tumor‐infiltrating macrophages presented in… read more here.
Keywords: inhibitor; mechanisms combination; combination strategies; btk inhibitor ... See more keywords
RAPID AND DURABLE RESPONSES WITH THE SYK/JAK INHIBITOR CERDULATINIB IN A PHASE 2 STUDY IN RELAPSED/REFRACTORY FOLLICULAR LYMPHOMA—ALONE OR IN COMBINATION WITH RITUXIMAB
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DOI: 10.1002/hon.30_2629
Abstract: treated with the Bruton tyrosine kinase (BTK) inhibitor ibrutinib, intolerance was the most common reason for discontinuation (50% to 63%; Mato AR, et al. Haematologica. 2018). This Phase 2 trial evaluated acalabrutinib, a highly selective,… read more here.
Keywords: relapsed refractory; phase; inhibitor; disease ... See more keywords
A Fast and Clean BTK Inhibitor
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DOI: 10.1021/acs.jmedchem.0c00597
Abstract: 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)… read more here.
Keywords: clean btk; chemistry; btk; fast clean ... See more keywords
Target modulation and pharmacokinetics/pharmacodynamics translation of the BTK inhibitor poseltinib for model-informed phase II dose selection
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DOI: 10.1038/s41598-021-98255-7
Abstract: The selective Bruton tyrosine kinase (BTK) inhibitor poseltinib has been shown to inhibit the BCR signal transduction pathway and cytokine production in B cells (Park et al. Arthritis Res. Ther. 18, 91, 10.1186/s13075-016-0988-z, 2016). This… read more here.
Keywords: dose selection; btk; btk inhibitor; inhibitor poseltinib ... See more keywords
Structure-based virtual screening and biological evaluation of novel small-molecule BTK inhibitors
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DOI: 10.1080/14756366.2021.1999237
Abstract: Abstract Bruton tyrosine kinase (BTK) is linked to multiple signalling pathways that regulate cellular survival, activation, and proliferation. A covalent BTK inhibitor has shown favourable outcomes for treating B cell malignant leukaemia. However, covalent inhibitors… read more here.
Keywords: inhibitor; btk inhibitor; based virtual; btk inhibitors ... See more keywords
Cardiotoxicity of BTK inhibitors: ibrutinib and beyond
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DOI: 10.1080/17474086.2022.2067526
Abstract: ABSTRACT Introduction The development of Brutons Tyrosine Kinase (BTK) inhibitors has transformed the treatment of B-cell malignancies and other non-malignant conditions. Management of the unique cardiotoxic profile of these agents requires prompt recognition and a… read more here.
Keywords: btk inhibitor; btk; cardiotoxicity btk; inhibitors ibrutinib ... See more keywords
BTK inhibitor selection for chronic lymphocytic leukemia: which drug for which patient?
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DOI: 10.1080/17474086.2022.2074393
Abstract: ABSTRACT Introduction The development of BTK inhibitors has revolutionized the management of CLL. Currently, there are 3 BTK inhibitors available to treat CLL: ibrutinib, acalabrutinib, and zanubrutinib (the latter not yet approved for this disease… read more here.
Keywords: patient; btk inhibitor; inhibitor selection; btk ... See more keywords
The Btk inhibitor AB‐95‐LH34 potently inhibits atherosclerotic plaque–induced thrombus formation and platelet procoagulant activity
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DOI: 10.1111/jth.15899
Abstract: New antithrombotic therapies with less effect on bleeding are needed for coronary artery disease. The Btk inhibitor ibrutinib blocks atherosclerotic plaque–mediated thrombus formation. However, it is associated with increased bleeding, possibly due to non–Btk‐mediated effects.… read more here.
Keywords: thrombus formation; atherosclerotic plaque; btk inhibitor; btk ... See more keywords
Abstract 3232: Development of novel Btk inhibitor, CB988 targering ibrutinib-resistant Btk C481S mutant
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DOI: 10.1158/1538-7445.am2017-3232
Abstract: Introduction: Bruton9s tyrosine kinase (Btk) is a member of the Tec family of cytoplasmic tyrosine kinase. Btk plays a crucial role in the BCR signaling, essential for B-cell development, and Btk has been recognized as… read more here.
Keywords: inhibitor cb988; btk c481s; btk; btk inhibitor ... See more keywords
Zanubrutinib in lymphoproliferative disorders: a comprehensive review
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DOI: 10.1177/20406207221093980
Abstract: The availability of Bruton tyrosine kinase (BTK) inhibitors has brought about a paradigm shift in the treatment of patients with B-cell lymphomas and chronic lymphocytic leukemia. BTK was clinically validated as a target by the… read more here.
Keywords: btk inhibitor; btk; side effects; treatment ... See more keywords