A novel microtubule independent effect of paclitaxel: the inhibition of peptidylarginine deiminase from bovine brain

摘要: Although the principal effect of paclitaxel (taxol) is in preventing depolymerization microtubules, other effects have been described recently. In present manuscript, we demonstrate an inhibitory on enzyme peptidylarginine deiminase (PAD) which converts peptidyl bound arginine to citrulline. To study mechanism action drug PAD, a number studies were carried out with purified enzyme. With synthetic substrate benzoyl-arginine ethyl ester (BAEE), almost total inhibition activity was observed at 12. 5 mM. myelin basic protein (MBP) as substrate, deimination arginyl residues prevented by 0.5 mM paclitaxel. The velocity-substrate curve unusual since enhancement BAEE. These data suggested presence two binding sites Inhibition non-competitive for both sites.