Perturbing pro-survival proteins using quinoxaline derivatives: A structure-activity relationship study

RajuleR.; BryantV.C.; LopezH.LuoX.NatarajanA.

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Perturbing pro-survival proteins using quinoxaline derivatives: A structure-activity relationship study

机译：Perturbing pro-survival proteins using quinoxaline derivatives: A structure-activity relationship study

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In HeLa cells the combinatorial knockdown of Bcl-xL and Mcl-1 is sufficient to induce spontaneous apoptosis. Quinoxaline derivatives were screened for the induction of Mcl-1 dependent apoptosis using a cell line without functional Bcl-xL. Quinoxaline urea analog 1h was able to specifically induce apoptosis in an Mcl-1 dependent manner. We demonstrate that even small changes to 1h results in dramatic loss of activity. In addition, 1h and ABT-737 synergistically inhibit cell growth and induce apoptosis. Our results also suggest that 1h could have therapeutic potential against ABT-737 refractory cancer.

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《Bioorganic and medicinal chemistry》 |2012年第7期|2227-2234|共8页
作者
RajuleR.; BryantV.C.; LopezH.LuoX.NatarajanA.;
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作者单位

Eppley Institute for Cancer Research, University of Nebraska Medical Center, Omaha, NE 68198;

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原文格式 PDF
正文语种英语
中图分类药学;
关键词
ABT-737; Bcl-xL; Mcl-1; Quinoxaline; Structure-activity relationship;

Perturbing pro-survival proteins using quinoxaline derivatives: A structure-activity relationship study

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