Specific Btk inhibition suppresses B cell- and myeloid cell-mediated arthritis

Di Paolo, Julie A, Huang, Tao, Balazs, Mercedesz, Barbosa, James, Barck, Kai H, Bravo, Brandon J, Carano, Richard A D, Darrow, James +23 more·2011·Nature Chemical Biology

Cited by (394)

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  2. Efficacy and safety of branebrutinib (BMS-986195), an irreversible Bruton's tyrosine kinase inhibitor, for the treatment of rheumatoid arthritis: a phase 2a, randomised, double-blind, placebo-controlled study
    Mikkel Østergaard, Espen Andre Haavardsholm, Miroslawa Nowak, Yi Luo, Jessica Landis, Aberra Fura, Chahin Pachaï, Duncan Rotich, Yanlin Wang-Fischer, Leonidas N. Carayannopoulos et al. · 2026 · The Lancet Rheumatology
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  4. Mechanisms of resistance to BTK inhibitors in B cell malignancies and emerging targeted strategies
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  5. Small-Molecule Drugs Approved by the FDA in 2025
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  6. Targeting DAMP Activation of Toll-Like Receptors: Novel Pathways to Treat Rheumatoid Arthritis?
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  7. Harnessing the Immune Regulatory Balance of Toll-like Receptor 9 Agonists in Cancer Immunotherapy.
    Cui J, Bai L, Li Zhou, Weihsuan Chen, J Chen · 2017
  8. Innate and adaptive immunomodulation by Bruton’s tyrosine kinase (BTK) inhibitors: An emerging treatment for multiple sclerosis
    Dejan Jakimovski, Bianca Weinstock‐Guttman, Robert Zivadinov · 2023 · Elsevier eBooks
  9. Development of 7H-pyrrolo[2,3-d]pyrimidin-4-amine Derivatives Using QSARINS Tool as BTK Inhibitors for the Treatment of Rheumatoid Arthritis
    Shital Manoj Patil, Kalyani Dhirendra Asgaonkar, Pradnya Magdum, Vaishnavi Chinde, Aishwarya M. Edake, Akshata Parashram Naik · 2023 · Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry
  10. Small Molecule Immunosuppressants in Inflammatory Disease
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  11. Adaptive and Innate Immune Systems
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  12. Resistance to Bruton’s Tyrosine Kinase Signaling Pathway Targeted Therapies
    Yaya Chu, Mitchell Stuart Cairo, Auke Beishuizen · 2019 · Resistance to targeted anti-cancer therapeutics
  13. Bayesian machine learning to discover Bruton’s tyrosine kinase inhibitors
    Jian Wang, Ting Ran, Yadong Chen, Tao Lu · 2019 · Chemical Biology & Drug Design
  14. Development of piperidinyl dipyrrrolopyridine-based dual inhibitors of Janus kinase and Bruton’s tyrosine kinase: a potential therapeutic probability to deal with rheumatoid arthritis
    Neelam Pery, Nayab Batool Rizvi, Muhammad Imtiaz Shafiq · 2020 · Journal of Molecular Modeling
  15. Ibrutinib: a strong candidate for the future of mantle cell lymphoma treatment
    Liang Zhang, Kate Juliet Newberry, Michael L. Wang · 2013 · Expert Review of Clinical Immunology
  16. Reply
    Lindsay E. Nyhoff, Leslie J. Crofford, Peggy L. Kendall · 2016 · Arthritis & Rheumatology
  17. Comprehensive Characterization of BTK Inhibitor Specificity, Potency, and Biological Effects: Insights into Covalent and Non-covalent Mechanistic Signatures
    Antonia C. Darragh, Andrew M. Hanna, Justin Lipner, Nicole B. Servant, Alastair J. King, Mirza Jahic · 2024 · bioRxiv (Cold Spring Harbor Laboratory)
  18. Use of Signaling Pathways as Therapeutic Targets for Blood Cancer
    Johanna Mondésir, Pierre Sujobert, Mark Alan Murakami, Marie‐Anne Hospital, Didier Bouscary, Jérôme Tamburini · 2014 · International Journal of Hematologic Oncology
  19. Novel Potent and Selective Bruton's Tyrosine Kinase (BTK) Inhibitor
    Lichuan Liu, Jason S. Halladay, Susan Wong, Melis Coraggio, Matthew Baumgardner, Sashi V. Gopaul, Jason W. Boggs, Peter Kuebler, Xiang Liao, Joseph W. Lubach et al. · 2011
  20. Investigation of the roles of acid sensing proteins in rheumatoid arthritis
    Fawaz Albloui · 2016 · White Rose eTheses Online (University of Leeds, The University of Sheffield, University of York)
  21. Protein Kinase Inhibitors for the Treatment of Multiple Sclerosis
    Ana Martı́nez, Carmen Gil · 2019 · Royal Society of Chemistry eBooks
  22. Development of Small Molecule Kinase Degraders as Chemical Biology Probes and Cancer Therapies
    Dennis Dobrovolsky · 2018 · Digital Access to Scholarship at Harvard (DASH) (Harvard University)
  23. Discovery and Process Development of BIIB068: A Reversible Bruton’s Tyrosine Kinase (BTK) Inhibitor for the Treatment of Autoimmune Diseases
    Bin Ma, Chaomin Li, Brian T. Hopkins, Lloyd C. Franklin, Robbie Chen, Tamera Mack, Daniel B. Patience, William F. Kiesman, Erin M. O’Brien · 2020 · ACS symposium series
  24. Allosteric regulation of BTK by the PHTH domain and small molecules
    Neha Amatya · 2021
  25. Medicinal Attributes of Heterocyclic Compounds in Rheumatoid Arthritis: Recent Developments and SAR Studies
    Vikram Jeet Singh, Bharti Sharma, Pooja A. Chawla · 2022 · Current Topics in Medicinal Chemistry
  26. Literature Search and Review
    Doug Auld, Wendy Lea, Mindy I. Davis, Anton M. Simeonov · 2011 · Assay and Drug Development Technologies
  27. Caracterização genética e funcional do NLRP3 em linfócitos e monócitos de indivíduos cronicamente infectados por HIV-1
    Vinícius Nunes Cordeiro Leal · 2021
  28. Drug Properties
    Siamak Cyrus Khojasteh, Harvey Wong, Donglu Zhang, Cornelis E. C. A. Hop · 2022 · Springer eBooks
  29. A structure-based approach to kinase inhibition based on the natural product (-)-TAN-2483B
    Jordan A. J. McCone · 2020
  30. Pharmacologic Features of Drugs Targeting Bruton's Tyrosine Kinase ( BTK )
    Joel McCay and, John G. Gribben · 2023
  31. Recent Progress of Irreversible BTK Inhibitors
    Wenxi Zhao · 2024 · Transactions on Materials Biotechnology and Life Sciences
  32. Structure-based design of novel pyrrolo[1,2-a]quinoxalin-4(5H)-one derivatives as potent noncovalent Bruton's tyrosine kinase (BTK) inhibitors
    Chaoquan Tian, Wenjie Liao, Zhixiao Yu, Hongguang Du, Haoming Song, Wenyi Mei, Zhenjiang Zhao, Yanyan Diao, Zhuo Chen, Honglin Li · 2025 · Bioorganic & Medicinal Chemistry Letters
  33. Molecular regulation of IL-2 inducible T-cell kinase (Itk) and the Tec kinases: A combined experimental and computational study, with emphasis on the N-terminal Pleckstrin Homology domain
    Scott E. Boyken · 2013
  34. Linker attachment points: “finishing touch” in PROTAC design
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  35. Targeting Bruton’s Tyrosine Kinase in CLL: Selectivity, Resistance Mechanisms, and Emerging Therapeutic Strategies
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  36. Tearing Down Scientific Boundaries: Frontiers in Medicinal Chemistry 2026
    Pascal Heitel, Philipp Barbie, Alessia Gambardella, Marta Pinto, Felix Pape, Anika Tarasewicz, Gerhard Heßler, Bernhard Wünsch, Matthias Schiedel, Christina Lamers · 2026 · ChemMedChem
  37. Bruton's Tyrosine Kinase Inhibitors: Mechanisms, Efficacy, Toxicities and Applications for the Treatment of Human Diseases
    Miao Sun, Dengju LI, Jia Wei · 2026 · MedComm
  38. Neuron myelination is accelerated by Bruton’s tyrosine kinase inhibition via microglial extracellular vesicles
    Matteo Tartaglia, Arianna Ioni, Mariassunta De Luca, Laura Vilardo, Igea D’Agnano, Antonella Conte, Cristina Limatola, Myriam Catalano · 2026 · Frontiers in Cellular Neuroscience
  39. BindingDB Entry 50002514: Design and Synthesis of Novel Amino-triazine Analogues as Selective Bruton's Tyrosine Kinase Inhibitors for Treatment of Rheumatoid Arthritis.
    BindingDB · 2020 · UC San Diego
  40. BindingDB Entry 50000272: Discovery of GDC-0853: A Potent, Selective, and Noncovalent Bruton's Tyrosine Kinase Inhibitor in Early Clinical Development.
    BindingDB · 2019 · UC San Diego
  41. BindingDB Entry 50001805: The development of Bruton's tyrosine kinase (BTK) inhibitors from 2012 to 2017: A mini-review.
    BindingDB · 2020 · UC San Diego
  42. BindingDB Entry 50017377: Emerging small-molecule inhibitors of the Bruton's tyrosine kinase (BTK): Current development.
    BindingDB · 2023 · UC San Diego
  43. BindingDB Entry 50023582: Design, Synthesis, and Biological Evaluation of Pyrrolo[1,2-a]quinoxalin-4(5H)-one Derivatives as Potent and Orally Available Noncovalent Bruton's Tyrosine Kinase (BTK) Inhibitors.
    BindingDB · 2026 · UC San Diego
  44. BindingDB Entry 7945: Discovery of a Potent BTK Inhibitor with a Novel Binding Mode by Using Parallel Selections with a DNA-Encoded Chemical Library.
    BindingDB · 2017 · UC San Diego
  45. BindingDB Entry 50016662: Optimization of a novel piperazinone series as potent selective peripheral covalent BTK inhibitors.
    BindingDB · 2023 · UC San Diego
  46. BindingDB Entry 50011293: Medicinal Chemistry Strategies for the Development of Kinase Inhibitors Targeting Point Mutations.
    BindingDB · 2022 · UC San Diego
  47. BindingDB Entry 50045492: Potent and selective Bruton's tyrosine kinase inhibitors: discovery of GDC-0834.
    BindingDB · 2016 · UC San Diego
  48. BindingDB Entry 50008819: Optimization of novel reversible Bruton's tyrosine kinase inhibitors identified using Tethering-fragment-based screens.
    BindingDB · 2021 · UC San Diego
  49. BindingDB Entry 50046859: Discovery of highly potent and selective Bruton's tyrosine kinase inhibitors: Pyridazinone analogs with improved metabolic stability.
    BindingDB · 2017 · UC San Diego
  50. BindingDB Entry 50007921: The Exploration of Chirality for Improved Druggability within the Human Kinome.
    BindingDB · 2021 · UC San Diego
  51. BindingDB Entry 50010916: Stereochemical Differences in Fluorocyclopropyl Amides Enable Tuning of Btk Inhibition and Off-Target Activity.
    BindingDB · 2021 · UC San Diego
  52. BindingDB Entry 50008415: Discovery of Evobrutinib: An Oral, Potent, and Highly Selective, Covalent Bruton's Tyrosine Kinase (BTK) Inhibitor for the Treatment of Immunological Diseases.
    BindingDB · 2021 · UC San Diego
  53. BindingDB Entry 50012032: Discovery of BIIB068: A Selective, Potent, Reversible Bruton's Tyrosine Kinase Inhibitor as an Orally Efficacious Agent for Autoimmune Diseases.
    BindingDB · 2022 · UC San Diego
  54. BindingDB Entry 50011454: Driving Potency with Rotationally Stable Atropisomers: Discovery of Pyridopyrimidinedione-Carbazole Inhibitors of BTK.
    BindingDB · 2022 · UC San Diego
  55. BindingDB Entry 50008045: Discovery and structure-activity relationship of novel diphenylthiazole derivatives as BTK inhibitor with potent activity against B cell lymphoma cell lines.
    BindingDB · 2021 · UC San Diego
  56. BindingDB Entry 50002240: Discovery of 4,7-Diamino-5-(4-phenoxyphenyl)-6-methylene-pyrimido[5,4- b]pyrrolizines as Novel Bruton's Tyrosine Kinase Inhibitors.
    BindingDB · 2020 · UC San Diego
  57. BindingDB Entry 50045472: Discovery of novel Bruton's tyrosine kinase (BTK) inhibitors bearing a pyrrolo[2,3-d]pyrimidine scaffold.
    BindingDB · 2016 · UC San Diego
  58. BindingDB Entry 50007980: Discovery of LOU064 (Remibrutinib), a Potent and Highly Selective Covalent Inhibitor of Bruton's Tyrosine Kinase.
    BindingDB · 2021 · UC San Diego
  59. BindingDB Entry 50000297: Discovery of N-(3-(5-((3-acrylamido-4-(morpholine-4-carbonyl)phenyl)amino)-1-methyl-6-oxo-1,6-dihydropyridin-3-yl)-2-methylphenyl)-4-(tert-butyl)benzamide (CHMFL-BTK-01) as a highly selective irreversible Bruton's tyrosine kinase (BTK) inhibitor.
    BindingDB · 2019 · UC San Diego
  60. BindingDB Entry 50047871: Discovery of 6-Fluoro-5-(R)-(3-(S)-(8-fluoro-1-methyl-2,4-dioxo-1,2-dihydroquinazolin-3(4H)-yl)-2-methylphenyl)-2-(S)-(2-hydroxypropan-2-yl)-2,3,4,9-tetrahydro-1H-carbazole-8-carboxamide (BMS-986142): A Reversible Inhibitor of Bruton's Tyrosine Kinase (BTK) Conformationally Constrained by Two Locke
    BindingDB · 2018 · UC San Diego
  61. BindingDB Entry 50012914: Discovery and Evaluation of Pyrazolo[3,4-
    BindingDB · 2022 · UC San Diego
  62. BindingDB Entry 50018849: Discovery of BGB-8035, a Highly Selective Covalent Inhibitor of Bruton's Tyrosine Kinase for B-Cell Malignancies and Autoimmune Diseases.
    BindingDB · 2024 · UC San Diego
  63. BindingDB Entry 50009603: Discovery of Zanubrutinib (BGB-3111), a Novel, Potent, and Selective Covalent Inhibitor of Bruton's Tyrosine Kinase.
    BindingDB · 2021 · UC San Diego
  64. BindingDB Entry 50018682: 4-Aminopyrazolopyrimidine scaffold and its deformation in the design of tyrosine and serine/threonine kinase inhibitors in medicinal chemistry.
    BindingDB · 2024 · UC San Diego
  65. BindingDB Entry 50003050: Optimization of the efflux ratio and permeability of covalent irreversible BTK inhibitors.
    BindingDB · 2020 · UC San Diego
  66. BindingDB Entry 50046425: Discovery of thieno[3,2-c]pyridin-4-amines as novel Bruton's tyrosine kinase (BTK) inhibitors.
    BindingDB · 2016 · UC San Diego
  67. BindingDB Entry 50015799: Design, synthesis, and biological evaluation of pyrrolopyrimidine derivatives as novel Bruton's tyrosine kinase (BTK) inhibitors.
    BindingDB · 2023 · UC San Diego
  68. BindingDB Entry 50040780: Rational design of highly selective spleen tyrosine kinase inhibitors.
    BindingDB · 2013 · UC San Diego
  69. BindingDB Entry 50040034: Bruton's tyrosine kinase inhibitors: approaches to potent and selective inhibition, preclinical and clinical evaluation for inflammatory diseases and B cell malignancies.
    BindingDB · 2013 · UC San Diego
  70. BindingDB Entry 50013934: Discovery of potent and selective reversible Bruton's tyrosine kinase inhibitors.
    BindingDB · 2022 · UC San Diego
  71. BindingDB Entry 50049042: Discovery of novel BTK inhibitors with carboxylic acids.
    BindingDB · 2019 · UC San Diego
  72. BindingDB Entry 50046650: Design and synthesis of carbazole carboxamides as promising inhibitors of Bruton's tyrosine kinase (BTK) and Janus kinase 2 (JAK2).
    BindingDB · 2016 · UC San Diego
  73. BindingDB Entry 50001941: Discovery and evaluation of 1H-pyrrolo[2,3-b]pyridine based selective and reversible small molecule BTK inhibitors for the treatment of rheumatoid arthritis.
    BindingDB · 2020 · UC San Diego
  74. BindingDB Entry 50011285: Design of Potent and Selective Covalent Inhibitors of Bruton's Tyrosine Kinase Targeting an Inactive Conformation.
    BindingDB · 2022 · UC San Diego
  75. BindingDB Entry 50045011: Design, synthesis and evaluation of novel 5-phenylpyridin-2(1H)-one derivatives as potent reversible Bruton's tyrosine kinase inhibitors.
    BindingDB · 2016 · UC San Diego
  76. BindingDB Entry 50044550: Discovery of a series of 2,5-diaminopyrimidine covalent irreversible inhibitors of Bruton's tyrosine kinase with in vivo antitumor activity.
    BindingDB · 2015 · UC San Diego
  77. BindingDB Entry 50003054: Discovery of a novel series of pyridine and pyrimidine carboxamides as potent and selective covalent inhibitors of Btk.
    BindingDB · 2020 · UC San Diego
  78. BindingDB Entry 50002048: Design and synthesis of novel pyrimidine analogs as highly selective, non-covalent BTK inhibitors.
    BindingDB · 2020 · UC San Diego
  79. BindingDB Entry 50016410: Review of the development of BTK inhibitors in overcoming the clinical limitations of ibrutinib.
    BindingDB · 2023 · UC San Diego
  80. BindingDB Entry 50046550: Synthesis and biological evaluation of novel 7-substituted 3-(4-phenoxyphenyl)thieno[3,2-c]pyridin-4-amines as potent Bruton's tyrosine kinase (BTK) inhibitors.
    BindingDB · 2016 · UC San Diego
  81. BindingDB Entry 50007714: Design, synthesis and evaluation of novel 7H-pyrrolo[2,3-d]pyrimidin-4-amine derivatives as potent, selective and reversible Bruton's tyrosine kinase (BTK) inhibitors for the treatment of rheumatoid arthritis.
    BindingDB · 2021 · UC San Diego
  82. BindingDB Entry 50046163: Fragment-Based Discovery of a Small Molecule Inhibitor of Bruton's Tyrosine Kinase.
    BindingDB · 2016 · UC San Diego
  83. BindingDB Entry 50034114: Imidazo[1,5-a]quinoxalines as irreversible BTK inhibitors for the treatment of rheumatoid arthritis.
    BindingDB · 2012 · UC San Diego
  84. BindingDB Entry 50002854: Discovery of potent, highly selective covalent irreversible BTK inhibitors from a fragment hit.
    BindingDB · 2020 · UC San Diego
  85. BindingDB Entry 50017556: Discovery of selective irreversible inhibitors of B-Lymphoid tyrosine kinase (BLK).
    BindingDB · 2023 · UC San Diego
  86. BindingDB Entry 50017353: Small-Molecule Kinase Inhibitors for the Treatment of Nononcologic Diseases.
    BindingDB · 2023 · UC San Diego
  87. BindingDB Entry 50015211: Discovery and Preclinical Characterization of BIIB091, a Reversible, Selective BTK Inhibitor for the Treatment of Multiple Sclerosis.
    BindingDB · 2023 · UC San Diego
  88. BindingDB Entry 50013640: Novel irreversible covalent BTK inhibitors discovered using DNA-encoded chemistry.
    BindingDB · 2022 · UC San Diego
  89. BindingDB Entry 50044301: Purine derivatives as potent Bruton's tyrosine kinase (BTK) inhibitors for autoimmune diseases.
    BindingDB · 2015 · UC San Diego
  90. BindingDB Entry 50010667: Discovery of Branebrutinib (BMS-986195): A Strategy for Identifying a Highly Potent and Selective Covalent Inhibitor Providing Rapid in Vivo Inactivation of Bruton's Tyrosine Kinase (BTK).
    BindingDB · 2021 · UC San Diego
  91. BindingDB Entry 50007369: Discovery of 4-Aminoquinoline-3-carboxamide Derivatives as Potent Reversible Bruton's Tyrosine Kinase Inhibitors for the Treatment of Rheumatoid Arthritis.
    BindingDB · 2021 · UC San Diego
  92. BindingDB Entry 50000587: Discovery of Potent and Selective Tricyclic Inhibitors of Bruton's Tyrosine Kinase with Improved Druglike Properties.
    BindingDB · 2019 · UC San Diego
  93. BindingDB Entry 50045572: TR-FRET binding assay targeting unactivated form of Bruton's tyrosine kinase.
    BindingDB · 2016 · UC San Diego
  94. BindingDB Entry 50000744: Structure-Activity Relationship Study of QL47: A Broad-Spectrum Antiviral Agent.
    BindingDB · 2020 · UC San Diego