Discovery of Selective Irreversible Inhibitors for Bruton’s Tyrosine Kinase
By Z. Pan, H. Scheerens, Shyr-Jiann Li, B. Schultz, P. Sprengeler, Leland C. Burrill, Rohan V Mendonca, M. Sweeney, K. Scott, P. Grothaus and 6 more. ChemMedChem, 2007
662 citations recorded by the source corpus.
Subfields: Genetics, Oncology, Radiology, Nuclear Medicine and Imaging
View Paper: https://www.semanticscholar.org/paper/9ed1ae73f403540be166af99cc9211ed88400c3c
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In Genetics
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In Radiology, Nuclear Medicine and Imaging
Citations in the corpus
- The Bruton tyrosine kinase inhibitor PCI-32765 blocks B-cell activation and is efficacious in models of autoimmune disease and B-cell malignancy (2010, background): “We previously reported the discovery and characterization of a series of Btk-selective irreversible inhibitors that bind covalently to a noncatalytic Cys (Cys481) residue in Btk (17).”
- Role of Bruton’s tyrosine kinase in B cells and malignancies (2018, background): “the kinase domain and thereby blocks kinase activity [184].”
- Kinase-targeted cancer therapies: progress, challenges and future directions (2018, background): “Various covalent kinase inhibitors target kinases such as BTK [143], Fes [144], VEGF-R2 [145], and RSK2 [146] through their ability to bind to a cysteine residue.”
- Targeting the PI5P4K lipid kinase family in cancer using covalent inhibitors (2020, background): “There has been a resurgence of interest in covalent inhibitors, especially with recent clinical successes of cysteine-directed covalent BTK inhibitor ibrutinib (Pan et al., 2007), EGFR inhibitors neratinib (Rabindran et al.”