Home > Publications database > Targeting sensitive and multidrug resistant leukemia cells with a novel benzofuran-isatin conjugate. > print |
001 | 300114 | ||
005 | 20250408150503.0 | ||
024 | 7 | _ | |a 10.1016/j.ejphar.2025.177538 |2 doi |
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037 | _ | _ | |a DKFZ-2025-00612 |
041 | _ | _ | |a English |
082 | _ | _ | |a 610 |
100 | 1 | _ | |a Jin, Chunmei |b 0 |
245 | _ | _ | |a Targeting sensitive and multidrug resistant leukemia cells with a novel benzofuran-isatin conjugate. |
260 | _ | _ | |a New York, NY [u.a.] |c 2025 |b Elsevier |
336 | 7 | _ | |a article |2 DRIVER |
336 | 7 | _ | |a Output Types/Journal article |2 DataCite |
336 | 7 | _ | |a Journal Article |b journal |m journal |0 PUB:(DE-HGF)16 |s 1744117463_4304 |2 PUB:(DE-HGF) |
336 | 7 | _ | |a ARTICLE |2 BibTeX |
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336 | 7 | _ | |a Journal Article |0 0 |2 EndNote |
500 | _ | _ | |a 2025 Mar 22:997:177538 |
520 | _ | _ | |a Benzofuran-isatin conjugates are considered as promising compounds in cancer prevention and treatment. However, it is not known yet whether these compounds are useful to effectively treat multidrug-resistant tumors. In this study, we investigated the activity of G-5e, a novel benzofuran-isatin conjugate in a panel of cell lines exhibiting well-known drug resistance mechanisms (P-gp, BCRP, TP53, EGFR). P-glycoprotein overexpressing CEM/ADR5000 cell line displayed notable hypersensitivity (collateral sensitivity) to G-5e, which was mediated through autophagic cell death activation including downregulation of the autophagy suppressor RND2, upregulation of the autophagy inducer LC3B, and G0/G1 phase arrest during cell cycle progression. Independent of collateral sensitivity, transcriptomic analyses also revealed that G-5e caused downregulation of NF-κB and ERK1/2 pathways. Our findings highlight the potential of benzofuran-isatin conjugates to combat multidrug resistance and the role of RND2 for collateral sensitivity. |
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650 | _ | 7 | |a Autophagic cell death |2 Other |
650 | _ | 7 | |a Benzofuran-isatin conjugate |2 Other |
650 | _ | 7 | |a Collateral sensitivity |2 Other |
650 | _ | 7 | |a Multidrug resistance |2 Other |
650 | _ | 7 | |a P-glycoprotein |2 Other |
700 | 1 | _ | |a Emam, Mahmoud |b 1 |
700 | 1 | _ | |a Klauck, Sabine M |0 P:(DE-He78)514f8ac681adb9f76d5de4b07ccd143b |b 2 |u dkfz |
700 | 1 | _ | |a Ali, Nadeen T |b 3 |
700 | 1 | _ | |a Salem, Rofaida |b 4 |
700 | 1 | _ | |a Eldehna, Wagdy M |b 5 |
700 | 1 | _ | |a Efferth, Thomas |b 6 |
700 | 1 | _ | |a Hegazy, Mohamed-Elamir F |b 7 |
700 | 1 | _ | |a Dawood, Mona |b 8 |
773 | _ | _ | |a 10.1016/j.ejphar.2025.177538 |g p. 177538 - |0 PERI:(DE-600)1483526-5 |p 177538 |t European journal of pharmacology |v 997 |y 2025 |x 0014-2999 |
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