The potential of pirtobrutinib in multiple B-cell malignancies - PubMed
Source : https://pubmed.ncbi.nlm.nih.gov/35747462/
Bruton's tyrosine kinase (BTK) is a critical downstream signaling element from the B-cell receptor (BCR) that has been effectively inhibited in B-cell cancers by irreversible, covalent inhibitors including ibrutinib and...
Relevance: Here, we review the pharmacologic rationale for pursuing non-covalent BTK inhibitors, the clinical need for such inhibitors, existing safety, and resistance mechanism data for pirtobrutinib, and the forthcoming clinical trials that seek to define the clinical utility of pirtobrutinib, which has the potential to fulfill multiple areas...
Integrin Signaling Shaping BTK-Inhibitor Resistance - PubMed
Source : https://pubmed.ncbi.nlm.nih.gov/35883678/
Integrins are adhesion molecules that function as anchors in retaining tumor cells in supportive tissues and facilitating metastasis. Beta1 integrins are known to contribute to cell adhesion-mediated drug resistance in...
Conclusion/Relevance: Bruton's tyrosine kinase (BTK) is a component of B cell receptor signaling and BTK inhibitors such as ibrutinib are highly successful; however, their limitations include indefinite drug administration, the development of therapy resistance, and toxicities. VLA-4 might be activated independently of BTK, resulting in an...
Risk of bleeding associated with BTK inhibitor monotherapy: a systematic review and meta-analysis of randomized controlled trials
Source : https://www.tandfonline.com/doi/abs/10.1080/17512433.2022.2106968?journalCode=ierj20
Abstract The risk of bleeding associated with Bruton's tyrosine kinase inhibitor (BTKi) monotherapy remains to be understood. This systematic review aims to evaluate BTKi monotherapy related bleeding risk. PubMed, Embase,...
Conclusions: Ibrutinib and acalabrutinib (vs. control drugs or placebo) have a higher risk of bleeding and overall bleeding, respectively. Limited evidence suggests that ibrutinib (vs. acalabrutinib) significantly increases overall bleeding risk, but the differences are not observed in other comparisons.
Dual Targeting of Anti-Apoptotic Proteins Enhances Chemosensitivity of the Acute Myeloid Leukemia Cells
Source : https://journal.waocp.org/article_90207.html
Document Type : Research Articles Authors 1 Immunology Research Center, Tabriz University of Medical sciences, Tabriz, Iran. 2 Department of Immunology, Faculty of Medicine, Shahrekord University of Medical Sciences, Shahrekord,...
Conclusions: Our investigation suggests that suppression of Mcl-1 and survivin by siRNA can effectually inhibit cell growth and overcome chemoresistance of AML cells. Therefore siRNAs may be an important adjuvant in chemotherapy for AML patients.
Bruton's Tyrosine Kinase phosphorylates scaffolding and RNA-binding protein G3BP1 to induce stress granule aggregation during host sensing of foreign ribonucleic acids
Source : https://www.jbc.org/article/S0021-9258(22)00673-1/fulltext
The Ras-GTPase activating protein SH3 domain-binding protein 1 (G3BP1) plays a critical role in the formation of classical and anti-viral stress granules in stressed and virus-infected eukaryotic cells, respectively. While...
Conclusion: Taken together, our data indicate that BTK phosphorylation of G3BP1 induces G3BP1 oligomerization and facilitates the condensation of ribonucleoprotein complexes into macromolecular aggregates.