AUTHOR=Starke Ilka , Glick Gary D. , Börsch Michael 

TITLE=Visualizing Mitochondrial FoF1-ATP Synthase as the Target of the Immunomodulatory Drug Bz-423

JOURNAL=Frontiers in Physiology

VOLUME=9

YEAR=2018

URL=https://www.frontiersin.org/journals/physiology/articles/10.3389/fphys.2018.00803

DOI=10.3389/fphys.2018.00803

ISSN=1664-042X

ABSTRACT=<p>Targeting the mitochondrial enzyme F<sub>o</sub>F<sub>1</sub>-ATP synthase and modulating its catalytic activities with small molecules is a promising new approach for treatment of autoimmune diseases. The immunomodulatory compound Bz-423 is such a drug that binds to subunit OSCP of the mitochondrial F<sub>o</sub>F<sub>1</sub>-ATP synthase and induces apoptosis <italic>via</italic> increased reactive oxygen production in coupled, actively respiring mitochondria. Here, we review the experimental progress to reveal the binding of Bz-423 to the mitochondrial target and discuss how subunit rotation of F<sub>o</sub>F<sub>1</sub>-ATP synthase is affected by Bz-423. Briefly, we report how Förster resonance energy transfer can be employed to colocalize the enzyme and the fluorescently tagged Bz-423 within the mitochondria of living cells with nanometer resolution.</p>