Direct inhibition of a PKA inhibitor, H-89 on K-V channels in rabbit coronary arterial smooth muscle cells
Özet
We examined the effects of the protein kinase A (PKA) inhibitor H-89 on voltage-dependent K+ (Kv) currents in freshly isolated rabbit coronary arterial smooth muscle cells, using a whole-cell patch clamp technique. H-89 inhibited the Kv current in a concentration-dependent manner, with a K-d value of 1.02 mu M. However, the PKA inhibitors KT 5720 and Rp-8-CPT-cAMPS did not significantly alter the Kv current or the inhibitory effects of H-89 on the Kv current. Moreover, H-85, a structurally similar but inactive analog of H-89, showed similar inhibitory effects on the Kv channel. H-89 had no effect on the voltage-dependency of activation or inactivation, or on recovery kinetics. These results suggest that in rabbit coronary arterial smooth muscle cells, H-89 inhibits the Kv current directly by blocking the pore cavity, an effect independent of PKA inhibition. (c) 2006 Elsevier Inc. All rights reserved.
Anahtar kelimeler
Atıf için künye
Son, Y., Park, W., Kim, S., Earm, Y., Kim, N., Youm, J., Warda, M. A. A., Kim, E., & Han, J. (2006). Direct inhibition of a PKA inhibitor, H-89 on K-V channels in rabbit coronary arterial smooth muscle cells. Biochemical and Biophysical Research Communications, 341(4), 931–937. https://doi.org/10.1016/j.bbrc.2006.01.053
BibTeX
@article{son2006-250711,
author = {Son, YK and Park, WS and Kim, SJ and Earm, YE and Kim, N and Youm, JB and Warda, Mohamad Alı Ahmad and Kim, E and Han, J},
title = {Direct inhibition of a PKA inhibitor, H-89 on K-V channels in rabbit coronary arterial smooth muscle cells},
journal = {Biochemical and Biophysical Research Communications},
year = {2006},
volume = {341},
number = {4},
pages = {931--937},
issn = {0006-291X},
doi = {10.1016/j.bbrc.2006.01.053},
url = {https://akademik.atauni.edu.tr/yayinlar/250711-direct-inhibition-of-a-pka-inhibitor-h-89-on-k-v-channels-in-rabbit-coronary}
}