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XIE Weiquan, DAI Wen, WANG Shuzhen, CHEN Yijun. A novel peptide and its mechanism overcoming imatinib-resistance chronic myeloid leukemia[J]. Journal of China Pharmaceutical University, 2014, 45(3): 368-372. DOI: 10.11665/j.issn.1000-5048.20140321
Citation: XIE Weiquan, DAI Wen, WANG Shuzhen, CHEN Yijun. A novel peptide and its mechanism overcoming imatinib-resistance chronic myeloid leukemia[J]. Journal of China Pharmaceutical University, 2014, 45(3): 368-372. DOI: 10.11665/j.issn.1000-5048.20140321
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A novel peptide and its mechanism overcoming imatinib-resistance chronic myeloid leukemia

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    • Abstract
  • COG133, a peptide inhibitor of SET, can enhance PP2A activity to treat imatinib-resistant CML by T315I mutation. Based on this fact, a peptide designated as SP2 showed the best anti-tumor activity among nine newly-designed Apolipoprotein E-mimetic peptides compared to COG133. The IC50 of SP2 against BaF3-p-210(T315I)cells was(2. 9±0. 1)μmol/L at 72 h, 10% of that of COG133(26. 5±1. 2 μmol/L). Further studies indicated that SP2 antagonizes SET protein to increase the activity of PP2A, thereby dephosphorylating p-BCR-ABL to induce cell apoptosis.
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    • References (19)
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