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Di-2-pyridylketone 4,4-dimethyl-3-thiosemicarbazone (Dp44mT) overcomes multidrug resistance by a novel mechanism involving the hijacking of lysosomal P-glycoprotein (Pgp).
Jansson PJ, Yamagishi T, Arvind A, Seebacher N, Gutierrez E, Stacy A, Maleki S, Sharp D, Sahni S, Richardson DR. Jansson PJ, et al. Among authors: seebacher n. J Biol Chem. 2015 Apr 10;290(15):9588-603. doi: 10.1074/jbc.M114.631283. Epub 2015 Feb 26. J Biol Chem. 2015. PMID: 25720491 Free PMC article.
Lysosomal membrane stability plays a major role in the cytotoxic activity of the anti-proliferative agent, di-2-pyridylketone 4,4-dimethyl-3-thiosemicarbazone (Dp44mT).
Gutierrez EM, Seebacher NA, Arzuman L, Kovacevic Z, Lane DJ, Richardson V, Merlot AM, Lok H, Kalinowski DS, Sahni S, Jansson PJ, Richardson DR. Gutierrez EM, et al. Biochim Biophys Acta. 2016 Jul;1863(7 Pt A):1665-81. doi: 10.1016/j.bbamcr.2016.04.017. Epub 2016 Apr 19. Biochim Biophys Acta. 2016. PMID: 27102538 Free article.
Novel second-generation di-2-pyridylketone thiosemicarbazones show synergism with standard chemotherapeutics and demonstrate potent activity against lung cancer xenografts after oral and intravenous administration in vivo.
Lovejoy DB, Sharp DM, Seebacher N, Obeidy P, Prichard T, Stefani C, Basha MT, Sharpe PC, Jansson PJ, Kalinowski DS, Bernhardt PV, Richardson DR. Lovejoy DB, et al. Among authors: seebacher n. J Med Chem. 2012 Aug 23;55(16):7230-44. doi: 10.1021/jm300768u. Epub 2012 Aug 3. J Med Chem. 2012. PMID: 22861499
26 results