Anthracenedione–methionine conjugates are novel topoisomerase II-targeting anticancer agents with favorable drug resistance profiles

Structure-associated drug resistance and DNA-unwinding abilities have greatly limited the clinical usage of anthracenediones, including mitoxantrone (MX) and ametantrone (AT), which intercalate into DNA and induce topoisomerase II (TOP2)-mediated DNA break. We studied a series of 1,4-bis(2-amino-eth...

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Veröffentlicht in:	Biochemical pharmacology 2012-05, Vol.83 (9), p.1208-1216
Hauptverfasser:	Lee, Chieh-Hua, Hsieh, Mei-Yi, Hsin, Ling-Wei, Chen, Hsiang-Chin, Lo, Su-Chi, Fan, Jia-Rong, Chen, Wan-Ru, Chen, Hung-Wei, Chan, Nei-Li, Li, Tsai-Kun
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Anthracenedione Anthraquinones - chemistry Anthraquinones - pharmacology anticarcinogenic activity Antigens, Neoplasm - genetics Antigens, Neoplasm - metabolism antineoplastic agents Antineoplastic Agents - chemistry Antineoplastic Agents - pharmacology Antitumor agents Apoptosis ATP Binding Cassette Transporter, Sub-Family B ATP-Binding Cassette, Sub-Family B, Member 1 - metabolism Cancer Cell culture Cleavable complex Cytotoxicity DNA DNA Breaks DNA Damage DNA topoisomerase (ATP-hydrolysing) DNA Topoisomerases, Type II - genetics DNA Topoisomerases, Type II - metabolism DNA-Binding Proteins - genetics DNA-Binding Proteins - metabolism Drug resistance Drug Resistance, Neoplasm Drug Screening Assays, Antitumor HL-60 Cells Humans Isoenzymes isozymes Male Methionine - chemistry Methionine - pharmacology Mice Mice, SCID Mitoxantrone Mitoxantrone - chemistry Mitoxantrone - pharmacology Multi-drug resistance P-Glycoprotein Poly-ADP-Ribose Binding Proteins proteins Structure-Activity Relationship Topoisomerase
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