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10.1085/jgp.201711942 http://scihub22266oqcxt.onion/10.1085/jgp.201711942 30002162!6080886!30002162     free     free     free Warning: file_get_contents(https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pubmed&id=30002162&cmd=llinks): Failed to open stream: HTTP request failed! HTTP/1.1 429 Too Many Requests in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 215 Deprecated: Implicit conversion from float 213.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 213.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 213.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 213.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 213.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 213.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534       J+Gen+Physiol 2018 ; 150 (8): 1215-1230 Nephropedia Template TP {{tp|p=30002162|t=2018. Biaryl sulfonamide motifs up- or down-regulate ion channel activity by activating voltage sensors |pdf=|usr=}}{{30002162}} gab.com Text Biaryl sulfonamide motifs up- or down-regulate ion channel activity by activating voltage sensors JO: J Gen Physiol http://www.kidney.de/pget.php?&tw=1&pmid=30002162 #FOAvip Voltage-gated ion channels are key molecules for the generation of cellular electrical excitability. Many pharmaceutical drugs target these channels by blocking their ion-conducting pore, but in many cases, channel-opening compounds would be more beneficial. Here, to search for new channel-opening compounds, we screen 18,000 compounds with high-throughput patch-clamp technology and find several potassium-channel openers that share a distinct biaryl-sulfonamide motif. Our data suggest that the negatively charged variants of these compounds bind to the top of the voltage-sensor domain, between transmembrane segments 3 and 4, to open the channel. Although we show here that biaryl-sulfonamide compounds open a potassium channel, they have also been reported to block sodium and calcium channels. However, because they inactivate voltage-gated sodium channels by promoting activation of one voltage sensor, we suggest that, despite different effects on the channel gates, the biaryl-sulfonamide motif is a general ion-channel activator motif. Because these compounds block action potential-generating sodium and calcium channels and open an action potential-dampening potassium channel, they should have a high propensity to reduce excitability. This opens up the possibility to build new excitability-reducing pharmaceutical drugs from the biaryl-sulfonamide scaffold. Twit Text FOAVip Biaryl sulfonamide motifs up- or down-regulate ion channel activity by activating voltage sensors ????J Gen Physiol http://www.kidney.de/pget.php?&tw=1&pmid=30002162 #FOAvip Twit Text # Free Paper on # # # # # LINK http://www.kidney.de/pget.php?&tw=1&pmid=30002162 #FOAvip English Wikipedia <ref>{{Cite pmid|30002162}}</ref> Biaryl sulfonamide motifs up- or down-regulate ion channel activity by activating voltage sensors #MMPMID30002162 Liin SI; Lund PE; Larsson JE; Brask J; Wallner B; Elinder F J Gen Physiol 2018[Aug]; 150 (8): 1215-1230 PMID30002162show ga Voltage-gated ion channels are key molecules for the generation of cellular electrical excitability. Many pharmaceutical drugs target these channels by blocking their ion-conducting pore, but in many cases, channel-opening compounds would be more beneficial. Here, to search for new channel-opening compounds, we screen 18,000 compounds with high-throughput patch-clamp technology and find several potassium-channel openers that share a distinct biaryl-sulfonamide motif. Our data suggest that the negatively charged variants of these compounds bind to the top of the voltage-sensor domain, between transmembrane segments 3 and 4, to open the channel. Although we show here that biaryl-sulfonamide compounds open a potassium channel, they have also been reported to block sodium and calcium channels. However, because they inactivate voltage-gated sodium channels by promoting activation of one voltage sensor, we suggest that, despite different effects on the channel gates, the biaryl-sulfonamide motif is a general ion-channel activator motif. Because these compounds block action potential-generating sodium and calcium channels and open an action potential-dampening potassium channel, they should have a high propensity to reduce excitability. This opens up the possibility to build new excitability-reducing pharmaceutical drugs from the biaryl-sulfonamide scaffold. |Animals[MESH] |CHO Cells[MESH] |Cricetulus[MESH] |High-Throughput Screening Assays[MESH] |Kinetics[MESH] |Shaker Superfamily of Potassium Channels/*drug effects[MESH] |Small Molecule Libraries[MESH]Biaryl sulfonamide motifs up- or down-regulate ion channel activity by(epmc).pdf DeepDyve Pubget Overpricing