ArticleThe Journal of general physiology2010
Glycine311, a determinant of paxilline block in BK channels: a novel bend in the BK S6 helix.
Article in The Journal of general physiology, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 23 papers.
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Who cites it
23 citing papers in PubMed, 30 citations in OpenAlex.
- Targeting the Cav1.2-KCa1.1 axis prevents rabies virus internalization and protects against lethal infection.PLoS pathogens · 2026Article
- Electrophysiological characterization of human KCNT1 channel modulators and the therapeutic potential of hydroquinine and tipepidine in KCNT1 mutation-associated epilepsy mouse model.Acta pharmacologica Sinica · 2025Article
- Transmembrane determinants of voltage-gating differences between BK (Slo1) and Slo3 channels.Biophysical journal · 2024Article
- Subunit-specific inhibition of BK channels by piperine.Biophysical journal · 2024Article
- Pharmacological Evidence Suggests That Slo3 Channel Is the Principal KInternational journal of molecular sciences · 2023Article
- Small molecule modulation of the Drosophila Slo channel elucidated by cryo-EM.Nature communications · 2021Article
- Roles of LRRC26 as an auxiliary γ1-subunit of large-conductance CaAmerican journal of physiology. Lung cellular and molecular physiology · 2020Article
- The functionally relevant site for paxilline inhibition of BK channels.Proceedings of the National Academy of Sciences of the United States of America · 2020Article
- Elucidating the Role of KInternational journal of molecular sciences · 2019Article
- Article
- Distinct mechanisms underlying cholesterol protection against alcohol-induced BK channel inhibition and resulting vasoconstriction.Biochimica et biophysica acta · 2016Article
- An old probe sheds new light on BK channel pore structure.The Journal of general physiology · 2014Article
- Paxilline inhibits BK channels by an almost exclusively closed-channel block mechanism.The Journal of general physiology · 2014Article
- Impact of heme and heme degradation products on vascular diameter in mouse visual cortex.Journal of the American Heart Association · 2014Article
- Structural determinants of phosphatidylinositol 4,5-bisphosphate (PIP2) regulation of BK channel activity through the RCK1 Ca2+ coordination site.The Journal of biological chemistry · 2014Article
- A point mutation in the human Slo1 channel that impairs its sensitivity to omega-3 docosahexaenoic acid.The Journal of general physiology · 2013Article
- Article
- Single-channel biophysical and pharmacological characterizations of native human large-conductance calcium-activated potassium channels in freshly isolated detrusor smooth muscle cells.Pflugers Archiv : European journal of physiology · 2013Article
- Role of the BK channel (KCa1.1) during activation of electrogenic K+ secretion in guinea pig distal colon.American journal of physiology. Gastrointestinal and liver physiology · 2012Article
- Article
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Authors and funding
4 authors at 1 institution in 1 country.
Funding
Abstract
The tremorogenic fungal metabolite, paxilline, is widely used as a potent and relatively specific blocker of Ca(2+)- and voltage-activated Slo1 (or BK) K(+) channels. The pH-regulated Slo3 K(+) channel, a Slo1 homologue, is resistant to blockade by paxilline. Taking advantage of the marked differences in paxilline sensitivity and the homology between subunits, we have examined the paxilline sensitivity of a set of chimeric Slo1/Slo3 subunits. Paxilline sensitivity is associated with elements of the S5-P loop-S6 module of the Slo1 channel. Replacement of the Slo1 S5 segment or the second half of the P loop results in modest changes in paxilline sensitivity. Replacing the Slo1 S6 segment with the Slo3 sequence abolishes paxilline sensitivity. An increase in paxilline affinity and changes in block kinetics also result from replacing the first part of the Slo1 P loop, the so-called turret, with Slo3 sequence. The Slo1 and Slo3 S6 segments differ at 10 residues. Slo1-G311S was found to markedly reduce paxilline block. In constructs with a Slo3 S6 segment, S300G restored paxilline block, but most effectively when paired with a Slo1 P loop. Other S6 residues differing between Slo1 and Slo3 had little influence on paxilline block. The involvement of Slo1 G311 in paxilline sensitivity suggests that paxilline may occupy a position within the central cavity or access its blocking position through the central cavity. To explain the differences in paxilline sensitivity between Slo1 and Slo3, we propose that the G311/S300 position in Slo1 and Slo3 underlies a structural difference between subunits in the bend of S6, which influences the occupancy by paxilline.
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