Phospholipid-sensitive Ca2+-dependent protein kinase inhibition by R-24571, a calmodulin antagonist.

@article{Mazzei1984PhospholipidsensitiveCP,
  title={Phospholipid-sensitive Ca2+-dependent protein kinase inhibition by R-24571, a calmodulin antagonist.},
  author={Gonzalo J. Mazzei and Randall C. Schatzman and Raymond Scott Turner and William Ralph Vogler and Jacqueline Kuo},
  journal={Biochemical pharmacology},
  year={1984},
  volume={33 1},
  pages={125-30}
}
R-24571 (calmidazolium), a derivative of the antimycotic agent miconazole, inhibited phospholipid-sensitive Ca2+-dependent protein kinase (PL-Ca-PK), with an IC50 (the concentration causing 50% inhibition) of 5.3 microM. It also inhibited the calmodulin/Ca2+-stimulated enzymes, with IC50 values of 1.6 and 0.1 microM for myosin light chain kinase (MLCK) and phosphodiesterase respectively. Analysis of inhibition by R-24571 of PL-Ca-PK and MLCK revealed complex kinetics, suggesting that the agent… CONTINUE READING