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- W2792696685 abstract "Large conductance Ca2+-activated K+ channels (BK channels) activate in response to both membrane voltage and intracellular Ca2+. Although the voltage sensor and Ca2+ binding sites have been identified, the coupling of the voltage sensor activation or Ca2+ binding to the opening of the activation gate is not clear. In a screening of compounds for BK channel modulators, we found BC1-5 as a candidate that alters BK channel function. Patch-clamp studies of mSlo1 BK channels expressed in the Xenopus oocyte membrane show that BC1-5 activates the channel at 0 [Ca2+]i by shifting the conductance-voltage (GV) relation to more negative voltages for up to 75 mV with a concentration at half-maximal response (EC50) of 4 μM. The shift of GV relation reduces when the channel is activated by increasing [Ca2+]i, In 100 μM [Ca2+]i, which is a saturating concentration for Ca2+ dependent activation of the channel, 100 µM BC1-5 cannot shift GV. This result suggests that BC1-5 promotes channel opening by interacting with the pathway for Ca2+ dependent activation. Although the BC1-5 effect depends on [Ca2+]i the compound can activate the mSlo1 Core-MT channel, in which the cytosolic domain containing Ca2+ binding sites is deleted. Molecular docking analysis and mutagenesis studies suggest that BC1-5 interacts with the cytosolic face of the voltage sensor domain to activate the channel. These results suggest that BC1-5 modulates the coupling between Ca2+ binding and channel opening and the voltage sensor domain is involved in this coupling mechanism." @default.
- W2792696685 created "2018-03-29" @default.
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- W2792696685 date "2018-02-01" @default.
- W2792696685 modified "2023-09-30" @default.
- W2792696685 title "Coupling between Sensors and the Activation Gate in BK Channels Probed by a Chemical Compound" @default.
- W2792696685 doi "https://doi.org/10.1016/j.bpj.2017.11.2635" @default.
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