Novel 5-Substituted Oxindoles Derivatives as Bruton\u27s Tyrosine Kinase Inhibitors: Design, Synthesis, Docking, Molecular Dynamic Simulation, and Biological Evaluation [PDF]
Bruton\u27s tyrosine kinase (BTK) is a non-RTK cytoplasmic kinase predominantly expressed by haemopoietic lineages, particularly B-cells. A new Oxindole-based focused library was designed to identify potent compounds targeting the BTK protein as ...
Marián , Hajdúch +9 more
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Hemophilia A is a rare hemorrhagic disorder caused by the lack of functional pro-coagulant factor VIII. Factor VIII replacement therapy in patients with severe hemophilia A results in the development of inhibitory anti-factor VIII IgG in up to 30% of ...
Sandrine Delignat +7 more
doaj +1 more source
Ibrutinib, a Bruton tyrosine kinase inhibitor, provides effective treatment for chronic lymphocytic leukemia (CLL). Here, the authors describe time-dependent molecular changes to malignant cells and to the immune system in patients undergoing ibrutinib ...
André F. Rendeiro +14 more
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Structure-Function Relationships of Covalent and Non-Covalent BTK Inhibitors
Low-molecular weight chemical compounds have a longstanding history as drugs. Target specificity and binding efficiency represent major obstacles for small molecules to become clinically relevant. Protein kinases are attractive cellular targets; however,
Rula Zain, Rula Zain, Mauno Vihinen
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Spontaneous Spinal Subdural Hematoma Secondary to Hemophilia A and Zanubrutinib
Spontaneous spinal subdural hematomas (SSH) are rare occurrences that can occur most commonly secondary to vascular malformations or coagulopathies. Only a small fraction of spontaneous SSHs are caused by acquired coagulation disorders such as leukemia ...
John Lynes +7 more
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Receptor-specific regulation of phosphatidylinositol 3'-kinase activation by the protein tyrosine phosphatase Shp2 [PDF]
Receptor tyrosine kinases (RTKs) play distinct roles in multiple biological systems. Many RTKs transmit similar signals, raising questions about how specificity is achieved.
Zhang, S. +13 more
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Targeting Bruton tyrosine kinase using non-covalent inhibitors in B cell malignancies
B cell receptor (BCR) signaling is involved in the pathogenesis of B cell malignancies. Activation of BCR signaling promotes the survival and proliferation of malignant B cells.
Danling Gu +4 more
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Primary CNS lymphoma (PCNSL) is a highly aggressive malignant disease with a high recurrence rate and a poor prognosis. We present the case of a 71-year-old woman diagnosed with PCNSL in June 2010.
Anna Mair +5 more
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Deep evolutionary conservation of an intramolecular protein kinase activation mechanism [PDF]
DYRK-family kinases employ an intramolecular mechanism to autophosphorylate a critical tyrosine residue in the activation loop. Once phosphorylated, DYRKs lose tyrosine kinase activity and function as serine/threonine kinases.
Cleghon Vaughn +31 more
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Evolution of breast cancer therapeutics: Breast tumour kinase’s role in breast cancer and hope for breast tumour kinase targeted therapy [PDF]
This is an open access article distributed under the terms of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/). © 2014 Baishideng Publishing Group Inc.There have been significant improvements in the detection
Hussain, HA, Harvey, A
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