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Chronic myeloid leukemia (CML) results from the formation of the BCR-ABL1 chimeric protein which serves as a target for clinically used tyrosine kinase inhibitors (TKIs), such as imatinib mesylate (IM). Although very efficient, the development of resistance to TKIs remains a critical issue for a subset of patients. In our study we aimed to identify one aspect of IM resistance in K-562 cells, a cell line used as a model for CML. Secreted from all cell types, extracellular vesicles (EVs) are nanoparticles that function as mediators of cell-cell communication. Upon engulfment by other cells they may modulate their phenotype. IM is linked to changes in oxidative metabolism in K-562 cells. Our study explored the putative involvement of EVs secreted from K-562 cells in providing protection from oxidative stress and resistance to IM in these cells. The results of our study showed that the protection from oxidative stress provided by previously exposed K-562 cell, derived EVs is only partial. Similarly, these EVs provided intact K-562 cells with some resistance to IM treatment. These results may suggest that resistance to IM may develop and expand to other cells by EVs that are secreted from already resistant cells, similar to a horizontal transfer of resistance provided by plasmids in bacteria.
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http://dx.doi.org/10.3390/cimb47080666 | DOI Listing |
Curr Issues Mol Biol
August 2025
The Felsenstein Medical Research Center, Rabin Medical Center, Petah-Tikva 4941492, Israel.
Chronic myeloid leukemia (CML) results from the formation of the BCR-ABL1 chimeric protein which serves as a target for clinically used tyrosine kinase inhibitors (TKIs), such as imatinib mesylate (IM). Although very efficient, the development of resistance to TKIs remains a critical issue for a subset of patients. In our study we aimed to identify one aspect of IM resistance in K-562 cells, a cell line used as a model for CML.
View Article and Find Full Text PDFRSC Adv
August 2025
Pharmaceutical Medicinal Chemistry& Drug Design Department, Faculty of Pharmacy (Boys), Al-Azhar University Cairo 11884 Egypt
A novel series of quinazoline-based compounds were designed and synthesized as modified analogues to certain known VEGFR-2 inhibitors, as an extension of our work on the design and synthesis of new VEGFR-2 inhibitors. The anti-proliferative properties of the synthesized compounds were assessed against three tumor cell lines (MCF-7, HepG-2, and K-562). Compounds 8a (IC = 0.
View Article and Find Full Text PDFMolecules
July 2025
Institute of Organic Chemistry with Centre of Phytochemistry, Bulgarian Academy of Sciences, Acad. G. Bontchev Str. Bl. 9, 1113 Sofia, Bulgaria.
Ferrocene (Fc), a redox-active organometallic scaffold, has attracted significant attention in medicinal chemistry due to its favorable physicochemical and pharmacological properties. The present study explores the therapeutic potential of novel Fc-functionalized analogues of imatinib and nilotinib, aimed at targeting BCR-ABL1+ chronic myeloid leukemia (CML) cells. A series of Fc-based derivatives (compounds , , , and ) were synthesized by systematically substituting key pharmacophoric regions of the parent tyrosine kinase inhibitors with Fc units.
View Article and Find Full Text PDFMed Oncol
July 2025
Laboratory of Veterinary Pharmacology and Toxicology, Faculty of Veterinary Medicine, University of Thessaly, Trikalon 224, 43100, Karditsa, Thessaly, Greece.
Natural products (NPs) have long been used in traditional medicine and continue to be explored for their chemopreventive and therapeutic properties. Many of their biological effects are mediated through redox-sensitive pathways, such as the nuclear factor erythroid 2-related factor 2 (Nrf2), a key regulator of antioxidant responses and cellular defense mechanisms. This study aimed to evaluate the antioxidant capacity, cytotoxicity, pro-apoptotic activity, and Nrf2-modulating effects of 22 natural product extracts traditionally used in ethnomedicine in a human leukemic K-562 cell model.
View Article and Find Full Text PDFBioorg Med Chem
November 2025
Stem Cells and Regenerative Medicine Innovation Center, Kerman University of Medical Sciences, Kerman, Iran.
Despite advances in antibody-based therapies for leukemia, significant limitations persist, including immunogenicity, toxicity, and resistance development. To address these challenges, we pursued an innovative peptide-based targeting strategy against CD33, a well-validated surface marker in leukemia. This study establishes a comprehensive pipeline integrating computational design with experimental validation to develop novel CD33-targeting peptides with optimal therapeutic properties.
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