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Inhibition of the mitochondrial F1F0-ATPase by ligands of the peripheral benzodiazepine receptor.

Abstract：

:Although PK11195 binds to the peripheral benzodiazepine receptor with nanomolar affinity, significant data exist which suggest that it has another cellular target distinct from the PBR. Here we demonstrate that PK11195 inhibits F(1)F(0)-ATPase activity in an OSCP-dependent manner, similar to the pro-apoptotic benzodiazepine Bz-423. Importantly, our data indicate that cellular responses observed with micromolar concentrations of PK11195, which are commonly attributed to modulation of the PBR, are likely a direct result of mitochondrial F(1)F(0)-ATPase inhibition.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Cleary J,Johnson KM,Opipari AW Jr,Glick GD

doi

10.1016/j.bmcl.2006.12.102

subject

Has Abstract

pub_date

2007-03-15 00:00:00

pages

1667-70

issue

6

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(07)00023-6

journal_volume

17

pub_type

杂志文章

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