{"id":782,"date":"2026-04-15T13:14:18","date_gmt":"2026-04-15T13:14:18","guid":{"rendered":"https:\/\/citations.tools.bio-logic.fr\/?p=782"},"modified":"2026-04-15T13:14:18","modified_gmt":"2026-04-15T13:14:18","slug":"pharmaco-topology-of-sulfonylurea-receptors","status":"publish","type":"post","link":"https:\/\/citations.tools.bio-logic.fr\/?p=782","title":{"rendered":"Pharmaco-topology of Sulfonylurea Receptors"},"content":{"rendered":"<h4>DOI:<\/h4>\n<p><a href=\"https:\/\/doi.org\/10.1074\/jbc.275.2.717\" target=\"_blank\" rel=\"noopener\">10.1074\/jbc.275.2.717<\/a><\/p>\n<h4>Authors:<\/h4>\n<p>Andrey P. Babenko, Gabriela Gonz\u00e1lez, Joseph Bryan<\/p>\n<h4>Abstract:<\/h4>\n<p>The differential responsiveness of (SUR1\/K(IR)6.2)(4) pancreatic beta-cell versus (SUR2A\/K(IR)6.2)(4) sarcolemmal or (SUR2B\/K(IR)6. 0)(4) smooth muscle cell K(ATP) channels to K(+) channel openers (KCOs) is the basis for the selective prevention of hyperinsulinemia, myocardial infarction, and acute hypertension. KCO-stimulation of K(ATP) channels is a unique example of functional coupling between a transport ATPase and a K(+) inward rectifier. KCO binding to SUR is Mg-ATP-dependent and antagonizes the inhibition of (K(IR)6.0)(4) pore opening by nucleotides. Patch-clamping of matched chimeric human SUR1-SUR2A\/K(IR)6.2 channels was used to identify the SUR regions that specify the selective response of sarcolemmal versus beta-cell channels to cromakalim or pinacidil versus diazoxide. The SUR2 segment containing the 12th through 17th predicted transmembrane domains, TMD12-17, confers sensitivity to the benzopyran, cromakalim, and the pyridine, pinacidil, whereas an SUR1 segment which includes TMD6-11 and the first nucleotide-binding fold, NBF1, controls responsiveness to the benzothiadiazine, diazoxide. These data are incorporated into a functional topology model for the regulatory SUR subunits of K(ATP) channels.<\/p>\n","protected":false},"excerpt":{"rendered":"<p>DOI: 10.1074\/jbc.275.2.717 Authors: Andrey P. Babenko, Gabriela Gonz\u00e1lez, Joseph Bryan Abstract: The differential responsiveness of (SUR1\/K(IR)6.2)(4) pancreatic beta-cell versus (SUR2A\/K(IR)6.2)(4) sarcolemmal or (SUR2B\/K(IR)6. 0)(4) smooth muscle cell K(ATP) channels to K(+) channel openers (KCOs) is the basis for the selective prevention of hyperinsulinemia, myocardial infarction, and acute hypertension. KCO-stimulation of K(ATP) channels is a unique [&hellip;]<\/p>\n","protected":false},"author":1,"featured_media":0,"comment_status":"open","ping_status":"open","sticky":false,"template":"","format":"standard","meta":{"footnotes":""},"categories":[21],"tags":[],"class_list":["post-782","post","type-post","status-publish","format-standard","hentry","category-rsc-200"],"_links":{"self":[{"href":"https:\/\/citations.tools.bio-logic.fr\/index.php?rest_route=\/wp\/v2\/posts\/782","targetHints":{"allow":["GET"]}}],"collection":[{"href":"https:\/\/citations.tools.bio-logic.fr\/index.php?rest_route=\/wp\/v2\/posts"}],"about":[{"href":"https:\/\/citations.tools.bio-logic.fr\/index.php?rest_route=\/wp\/v2\/types\/post"}],"author":[{"embeddable":true,"href":"https:\/\/citations.tools.bio-logic.fr\/index.php?rest_route=\/wp\/v2\/users\/1"}],"replies":[{"embeddable":true,"href":"https:\/\/citations.tools.bio-logic.fr\/index.php?rest_route=%2Fwp%2Fv2%2Fcomments&post=782"}],"version-history":[{"count":0,"href":"https:\/\/citations.tools.bio-logic.fr\/index.php?rest_route=\/wp\/v2\/posts\/782\/revisions"}],"wp:attachment":[{"href":"https:\/\/citations.tools.bio-logic.fr\/index.php?rest_route=%2Fwp%2Fv2%2Fmedia&parent=782"}],"wp:term":[{"taxonomy":"category","embeddable":true,"href":"https:\/\/citations.tools.bio-logic.fr\/index.php?rest_route=%2Fwp%2Fv2%2Fcategories&post=782"},{"taxonomy":"post_tag","embeddable":true,"href":"https:\/\/citations.tools.bio-logic.fr\/index.php?rest_route=%2Fwp%2Fv2%2Ftags&post=782"}],"curies":[{"name":"wp","href":"https:\/\/api.w.org\/{rel}","templated":true}]}}