Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 46, Issue 21, Pages 4365-4368Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm034107j
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There is compelling evidence that Bax channel activity stimulates cytochrome c release leading ultimately to cell death, which is a key event in ischemic injuries and neurodegenerative diseases. Here 3,6-dibromocarbazole piperazine derivatives of 2-propanol are described as the first small and potent modulators of the cytochrome c release triggered by Bid-induced Bax activation in a mitochondrial assay. Furthermore, a mechanism of action is proposed, and fluorescent derivatives allowing the localization of such inhibitors are reported.
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