Q-VD-OPh, a Broad Spectrum Caspase Inhibitor with Potent Antiapoptotic Properties
Document Type
Article
Publication Date
8-1-2003
Abstract
In recent years, several inhibitors that prevent caspase activation and apoptosis have emerged. At high doses, however, these inhibitors can have nonspecific effects and/or become cytotoxic. In this study, we determined the effectiveness of broad spectrum caspase inhibitors to prevent apoptosis. A carboxy terminal phenoxy group conjugated to the amino acids valine and aspartate (Q-VD-OPh) potently inhibited apoptosis. Q-VD-OPh was significantly more effective in preventing apoptosis than the widely used inhibitors, ZVAD-fmk and Boc-D-fmk, and was also equally effective in preventing apoptosis mediated by the three major apoptotic pathways, caspase 9/3, caspase 8/10, and caspase 12. In addition to the increased effectiveness, Q-VD-OPh was not toxic to cells even at extremely high concentrations. Our data indicate that the specificity, effectiveness, and reduced toxicity of caspase inhibitors can be significantly enhanced using carboxyterminal o-phenoxy groups and may have important uses in vivo.
Repository Citation
Caserta, T. M.,
Smith, A. N.,
Gultice, A. D.,
Reedy, M. A.,
& Brown, T. L.
(2003). Q-VD-OPh, a Broad Spectrum Caspase Inhibitor with Potent Antiapoptotic Properties. Apoptosis, 8 (4), 345-352.
https://corescholar.libraries.wright.edu/ncbp/52
