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3,6-dibromocarbazole piperazine derivatives of 2-propanol as first inhibitors of cytochrome c release via Bax channel modulation.

Abstract：

: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.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Bombrun A,Gerber P,Casi G,Terradillos O,Antonsson B,Halazy S

doi

10.1021/jm034107j

keywords:

subject

Has Abstract

pub_date

2003-10-09 00:00:00

pages

4365-8

issue

21

eissn

0022-2623

issn

1520-4804

journal_volume

46

pub_type

信件

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