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논문 기본 정보

자료유형
학술대회자료
저자정보
Ha, Tal-Soo (Lab. of Molecular Neurobiology, Dept. of Life Science Kwangju Institute of Science and Technology [K-JIST]) Kim, Yong-Chul (Lab. of Drug Discovery, Dept. of Life Science Kwangju Institute of Science and Technology [K-JIST]) Park, Chul-Seung (Lab. of Molecular Neurobiology, Dept. of Life Science Kwangju Institute of Science and Technology [K-JIST])
저널정보
한국생물물리학회 한국생물물리학회 학술발표회 한국생물물리학회 2003년도 정기총회 및 학술발표회
발행연도
2003.1
수록면
42 - 42 (1page)

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Large-conductance $Ca^{2+}$-activated potassium channels ($BK_{Ca}$ are a widely distributed and play key roles in various cell functions. In nerve cells, $BK_{Ca}$ channels shorten the duration of action potentials and block $Ca^{2+}$ entry thereby repolarizing excitable cells after excitation. $BK_{Ca}$ channel opening has been postulated to confer neuroprotection during stroke, and has attracted attention as a means for therapeutic intervention in asthma, hypertension, convulsions, and traumatic brain injury. Several natural and synthetic compounds including a steroid hormone, $\beta$-estradiol, have been identified as the activators of $BK_{Ca}$ channels. Based on the structural features of the previously reported activators of $BK_{Ca}$ channels, we designed several lead compounds, synthesized chemically, and tested their functional activity on cloned $BK_{Ca}$ channels. The $\alpha$ subunit of rat $BK_{Ca}$ channel was expressed alone or with different $\beta$ subunits in Xenopus oocytes and the effects of the compounds were tested electrophysiological means. One of the lead compounds affected the activity of the $\alpha$ subunit of $BK_{Ca}$ channel in a $\beta$ subunit-specific manner. While the activity of B $K_{ca}$ channel $\alpha$ subunit was Potentiated, the channel composed of $\alpha$ and $\beta$1 subunits were inhibited by this compound. We are currently investigating the mechanism of the $\beta$ subunit-dependent effects and planning to localize the receptor site of the lead compound.f the lead compound.

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