Novel pharmacological approach for the prevention of multidrug resistance (MDR) in a human leukemia cell line

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dc.contributor.authorGupta, Sonu Kumar
dc.contributor.authorSingh, Priyanka
dc.contributor.authorChhabra, Ravindresh
dc.contributor.authorVerma, Malkhey
dc.date.accessioned2024-01-16T14:23:08Z
dc.date.accessioned2024-08-13T10:34:06Z
dc.date.available2024-01-16T14:23:08Z
dc.date.available2024-08-13T10:34:06Z
dc.date.issued2021-06-11T00:00:00
dc.description.abstractBackground: Drug resistance mechanisms are the regulatory factors associated with drug metabolism and drug transport to inward and outward of the target cells. Maybridge fragment (MBF) library is a collection of pharmacophore rich compounds having affinity with membrane transporters. This study has been designed to evaluate the efficacy of MBFs in overcoming the leukemic cells� resistance to imatinib. Methods: Imatinib resistant cells (K562-R) were prepared using myelogenous leukemia cell line (K562) by titration method. The four MBFs were prioritized for determining their effect on imatinib resistance. The cells were treated with imatinib and MBFs and the MTT assay was performed to evaluate the efficacy of MBFs in enhancing the imatinib mediated cell death. The transcript levels of Bcr-Abl1 gene and efflux transporter genes were determined by RT-qPCR analysis. Results: The MBFs enhanced the imatinib mediated cell death of K562-R cells. There was also a significant decrease in the mRNA levels of the major drug efflux genes (ABCB1, ABCB10, ABCC1 and ABCG2) when treated with a combination of imatinib and MBF in comparison to imatinib treatment alone. Conclusion: The drug efflux is one of the mechanisms of multidrug resistance in cancer cells and the MBFs used in this study were all found to significantly overcome the imatinib resistance by limiting the expression of efflux genes. This study, therefore, highlights the potential of Maybridge compounds in treating the drug resistant leukemia. � 2021 Elsevier Ltden_US
dc.identifier.doi10.1016/j.leukres.2021.106641
dc.identifier.issn1452126
dc.identifier.urihttps://doi.org/10.1016/j.leukres.2021.106641
dc.identifier.urihttp://10.2.3.109/handle/32116/2851
dc.language.isoen_USen_US
dc.publisherElsevier Ltden_US
dc.subjectBcr-Abl1en_US
dc.subjectChronic Myeloid Leukemiaen_US
dc.subjectDrug efflux pumpsen_US
dc.subjectImatinib Mesylateen_US
dc.subjectMaybridge compoundsen_US
dc.subjectRT-qPCRen_US
dc.titleNovel pharmacological approach for the prevention of multidrug resistance (MDR) in a human leukemia cell lineen_US
dc.title.journalLeukemia Researchen_US
dc.typeArticleen_US
dc.type.accesstypeClosed Accessen_US

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