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September 10, 2025British Journal of Haematology

Differential modulation of Bruton's tyrosine kinase inhibitor selectivity on platelet GPVI and integrin αIIbβ3 bidirectional signalling via BTK/PLCγ2/PKCθ affects haemostasis and thrombosis

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Authors

TZTeng ZhangSDShan DuGHGongwei Han

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Overview

Exploration of BTK inhibitors' impact on thrombus formation in relation to GPVI and integrin signaling pathways.

Key Points

  • Ibrutinib significantly inhibits platelet activation and integrin αIIbβ3 more than zanubrutinib, impacting haemostasis.
  • Collagen-induced GPVI signalling is differentially regulated by both BTK inhibitors, revealing distinct pathways.
  • Observational analysis of clot retraction and platelet spreading shows greater inhibitory effects of ibrutinib via integrin αIIbβ3.
  • Differential modulation in the BTK/PLCγ2/PKCθ pathway can increase bleeding risk, emphasizing therapeutic implications.

Cite This Study

Zhang et al. (2025) studied this question.

synapsesocial.com/papers/68c1a26154b1d3bfb60dd408https://doi.org/10.1111/bjh.70029
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Also Consider

Synapse has enriched 5 closely related papers on similar clinical questions. Consider them for comparative context:

  1. 1498 Bruton’s tyrosine kinase (BTK) inhibitors impede platelet aggregation but not adhesion to collagen.2024
  2. 2Comparison of variably specific Bruton tyrosine kinase inhibitors on platelet aggregation mediated by Fcγ receptor (FcγR) IIa, glycoprotein VI, and platelet endothelial aggregation receptor (PEAR) 1: implications for Bruton tyrosine kinase inhibitors as antithrombotic therapy2026
  3. 3Involvement of Btk in Cardiovascular Disease and Its Therapeutic Targeting2026 · 2 citations
  4. 4Selective Btk inhibition by PRN1008/PRN473 blocks human CLEC-2 & PRN473 reduces venous thrombosis formation in mice.2024 · 18 citations
  5. 5BTK Inhibition in Hematology: From CLL/SLL to Emerging Applications Across B-Cell and Immune Disorders2026 · 5 citations