标题：Small-Molecule Bcl2 BH4 Antagonist for Lung Cancer Therapy

作者：Han B1, Park D1, Li R1, Xie M1, Owonikoko TK2, Zhang G2, Sica GL3, Ding C4, Zhou J4, Magis AT5, Chen ZG2, Shin DM2, Ramalingam SS2, Khuri FR2, Curran WJ1, Deng X6.

网址:http://www.ncbi.nlm.nih.gov/pubmed/26004684

求助者：omt05

• 求助时间：2015/6/12 11:45:53
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• 文献摘要：

The BH4 domain of Bcl2 is required for its antiapoptotic function, thus constituting a promising anticancer target. We identified a small-molecule Bcl2-BH4 domain antagonist, BDA-366, that binds BH4 with high affinity and selectivity. BDA-366-Bcl2 binding induces conformational change in Bcl2 that abrogates its antiapoptotic function, converting it from a survival molecule to a cell death inducer. BDA-366 suppresses growth of lung cancer xenografts derived from cell lines and patient without significant normal tissue toxicity at effective doses. mTOR inhibition upregulates Bcl2 in lung cancer cells and tumor tissues from clinical trial patients. Combined BDA-366 and RAD001 treatment exhibits strong synergy against lung cancer in vivo. Development of this Bcl2-BH4 antagonist may provide a strategy to improve lung cancer outcome.

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