Cui Yong-Mei, Yasutomi Eriko, Otani Yuko, Yoshinaga Takashi, Ido Katsutoshi, Sawada Kohei, Ohwada Tomohiko
Graduate School of Pharmaceutical Sciences, The University of Tokyo, 7-3-1 Hongo, Bunkyo-ku, Tokyo 113-0033, Japan.
Bioorg Med Chem Lett. 2008 Oct 1;18(19):5197-200. doi: 10.1016/j.bmcl.2008.08.081. Epub 2008 Aug 28.
We found that the podocarpic acid structure provides a new scaffold for chemical modulators of large-conductance calcium-activated K(+) channels (BK channels). Structure-activity analysis indicates the importance of both the arrangement (i.e., location and orientation) of the carboxylic acid functionality of ring A and the hydrophobic region of ring C for expression of BK channel-opening activity.
我们发现罗汉松酸结构为大电导钙激活钾通道（BK通道）的化学调节剂提供了一种新的支架。构效分析表明，A环羧酸官能团的排列（即位置和取向）以及C环的疏水区域对于BK通道开放活性的表达均很重要。
