![Discovery of pyrrolo[1,2-a]quinoxalin-4(5H)-one derivatives as novel non-covalent Bruton's tyrosine kinase (BTK) inhibitors - PubMed](https://static-content-prd.skipta.com/public/skipta/skipta-post/2023-12/fileENEXh9 "Discovery of pyrrolo[1,2-a]quinoxalin-4(5H)-one derivatives as novel non-covalent Bruton's tyrosine kinase (BTK) inhibitors - PubMed")
Discovery of pyrrolo[1,2-a]quinoxalin-4(5H)-one derivatives as novel non-covalent Bruton's tyrosine kinase (BTK) inhibitors - PubMed
Source : https://pubmed.ncbi.nlm.nih.gov/35661525/
Bruton's tyrosine kinase (BTK) is a promising target in the treatment of B cell malignancies and autoimmune disorders. Developing selective non-covalent BTK inhibitors is an important strategy to overcome the...
Conclusion/Relevance: In all, we provided a new scaffold as non-covalent selective BTK inhibitors and the representative compounds exhibited potency both in vitro and in vivo.
Structural Feature Analyzation Strategies toward Discovery of Orally Bioavailable PROTACs of Bruton's Tyrosine Kinase for the Treatment of Lymphoma - PubMed
Source : https://pubmed.ncbi.nlm.nih.gov/35671249/
doi: 10.1021/acs.jmedchem.2c00324. Online ahead of print. 1 Hangzhou Institute of Innovative Medicine, Institute of Drug Discovery and Design, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310058, P. R. China. 2...
Conclusion/Relevance: Bruton's tyrosine kinase proteolysis-targeting chimeras (BTK-PROTACs) have emerged as a promising approach to address the limitations of BTK inhibitors. However, conducting the rational discovery of orally bioavailable BTK-PROTACs presents significant challenges. In this study, dimensionality reduction analysis and model...
Pirtobrutinib inhibits wild-type and mutant Bruton's tyrosine kinase-mediated signaling in chronic lymphocytic leukemia - Blood Cancer Journal
Source : https://www.nature.com/articles/s41408-022-00675-9
Pirtobrutinib (LOXO-305), a reversible inhibitor of Bruton's tyrosine kinase (BTK), was designed as an alternative strategy to treat ibrutinib-resistant disease that develops due to C481 kinase domain mutations. The clinical...
Conclusion: Collectively, these results demonstrate that pirtobrutinib is an effective BTK inhibitor for CLL harboring wild-type or mutant BTK as observed by changes in CCL3 and CCL4 biomarkers and suggest that alterations in BCR pathway signaling are the mechanism for its clinical effects. Long-term evaluation is needed for BTK gatekeeper...
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Leukemia and Lymphoma Connect3yrKey Points • Source: Blood Cancer Journal • Conclusion: “Pirtobrutinib appears to be an effective agent for lowering BCR-mediated signaling in cell lines as well as primary cells, including during therapy. Importantly, this drug Show More
Novel agents and regimens for hematological malignancies: recent updates from 2020 ASH annual meeting - Journal of Hematology & Oncology
Source : https://jhoonline.biomedcentral.com/articles/10.1186/s13045-021-01077-3
Antibodies and chimeric antigen receptor-engineered T cells (CAR-T) are increasingly used for cancer immunotherapy. Small molecule inhibitors targeting cellular oncoproteins and enzymes such as BCR-ABL, JAK2, Bruton tyrosine kinase, FLT3,...
Relevance: Antibodies and chimeric antigen receptor-engineered T cells (CAR-T) are increasingly used for cancer immunotherapy. Small molecule inhibitors targeting cellular oncoproteins and enzymes such as BCR-ABL, JAK2, Bruton tyrosine kinase, FLT3, BCL-2, IDH1, IDH2, are biomarker-driven chemotherapy-free agents approved for several major...
New Directions for Mantle Cell Lymphoma in 2022
Mantle cell lymphoma is a rare B-cell non-Hodgkin lymphoma that is clinically and biologically heterogeneous. Risk stratification at the time of diagnosis is critical. One of the most powerful prognostic...
0pubmed
Conclusion/Relevance: The therapeutic landscape is rapidly evolving in mantle cell lymphoma, including earlier use of novel biologically targeted therapies for frontline treatment. In addition, in relapsed/refractory mantle cell lymphoma, there are a number of promising therapies beyond covalent BTK inhibitors, including novel...