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- || Review, Journal: Fyn, Blk, and Lyn kinase inhibitors: A mini-review on medicinal attributes, research progress, and future insights. (Pubmed Central) - Mar 18, 2024
The discussion encompasses the design strategies, SAR analysis, and chemical characteristics of effective inhibitors, shedding light on their specificity and potency. Furthermore, it explores the progress of clinical trials of these inhibitors, emphasizing their potential therapeutic applications.
- | Journal, Cancer stem: Transcriptomic analysis identifies B-lymphocyte kinase as a therapeutic target for desmoplastic small round cell tumor cancer stem cell-like cells. (Pubmed Central) - Jan 4, 2024
BLK inhibition and knockdown reduced CSC-like properties, including abrogation of tumorsphere formation and stemness marker expression. Importantly, BLK knockdown reduced DSRCT CSC-like cell chemoresistance, making its inhibition a promising target for future combination therapy.
- | dasatinib / Generic mfg.
Journal: Discovery of promising B lymphocyte kinase inhibitors using structure-guided virtual screening. (Pubmed Central) - Sep 9, 2023
The control molecule for this study was the known BLK inhibitor, Dasatinib...Both proposed molecules remained bound to the binding pocket of BLK, as indicated by the molecular dynamics (MD) simulation study. Taken together, these findings provide valuable insights for guiding future research endeavors and translational efforts in developing therapeutics for different complex diseases, such as autoimmune disorders, lymphomas, and leukemias.Communicated by Ramaswamy H. Sarma.
- M7583 / EMD Serono, Telios Pharma
CHARACTERIZATION OF TL-895: A NOVEL BRUTON TYROSINE KINASE INHIBITOR (BTKI) IN CLINICAL DEVELOPMENT FOR CHRONIC LYMPHOCYTIC LEUKEMIA (CLL) AND MYELOFIBROSIS (MF) (Poster area) - May 12, 2023 - Abstract #EHA2023EHA_1267;
P1/2, P2
In pts with CLL and MF, the 150mg BID doseachieved complete and sustained BTK occupancy throughout the dosing interval, despite faster BTK resynthesis in myeloid cells. TL-895 holds therapeutic promise by modulating key signaling nodes of cell activation, reducing stromal support, and downregulating proinflammatory cytokines in pts with CLL and MF.
- PROTEOMIC PROFILING UNCOVERS THERAPEUTIC VULNERABILITIES FOR TCF3 TRANSLOCATED B-CELL ACUTE LYMPHOBLASTIC LEUKEMIAS (Poster area) - May 12, 2023 - Abstract #EHA2023EHA_963;
We suggest that exploring the protein expression landscape of genetic subtypes of B-ALL is a promising approachfor the discovery of putative biomarkers and promising novel therapeutic strategies. Proteomics, Acute lymphoblastic leukemia, ALL