3,6-Dibromocarbazole Piperazine Derivatives of 2-Propanol as First Inhibitors of Cytochrome c Release via Bax Channel Modulation

A Bombrun, P Gerber, G Casi… - Journal of medicinal …, 2003 - ACS Publications
A Bombrun, P Gerber, G Casi, O Terradillos, B Antonsson, S Halazy
Journal of medicinal chemistry, 2003ACS Publications
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 …
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.
ACS Publications