AI-based discovery and cryoEM structural elucidation of a KATP channel pharmacochaperone [PDF]
eLifePancreatic KATP channel trafficking defects underlie congenital hyperinsulinism (CHI) cases unresponsive to the KATP channel opener diazoxide, the mainstay medical therapy for CHI. Current clinically used KATP channel inhibitors have been shown to act as
Assmaa Elsheikh +7 more
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The ATP sensitive potassium channel (KATP) is a novel target for migraine drug development
Frontiers in Molecular Neuroscience, 2023 Migraine is one of the leading causes of disability worldwide, affecting work and social life. It has been estimated that sales of migraine medicines will reach 12.9 billion USD in 2027.
Amalie Clement +5 more
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KATP channels and cardioprotection [PDF]
Arhiv za farmacijuThis review discusses ATP-sensitive potassium (KATP) channels, which connect intracellular energy metabolism to cellular electrical activity and play crucial roles in various physiological processes, particularly in the pancreas and cardiovascular system.
Taskin Eylem +5 more
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15727 KATP channel prodrugs as therapeutics for chronic pain and substance abuse disorders [PDF]
Journal of Clinical and Translational Science, 2021 IMPACT: Pharmacological activation of KATP channels may provide analgesia and attenuate opioid tolerance and withdrawal OBJECTIVES/GOALS: Our long term goal is to develop therapeutics for the treatment of the overuse of opioids.
Alexis Doucette +3 more
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Structural insights into the mechanism of pancreatic KATP channel regulation by nucleotides [PDF]
Nature Communications, 2022 KATP channels are energy sensors. Here, authors report the Cryo-EM structures of pancreatic KATP in both the closed state and the pre-open state. These structures illuminate the mechanism of KATP channel regulation by the intracellular nucleotides.
Mengmeng Wang +3 more
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The Structural Basis for the Binding of Repaglinide to the Pancreatic KATP Channel
Cell Reports, 2019 Summary: Repaglinide (RPG) is a short-acting insulin secretagogue widely prescribed for the treatment of type 2 diabetes. It boosts insulin secretion by inhibiting the pancreatic ATP-sensitive potassium channel (KATP).
Dian Ding +4 more
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KATP channel dependent heart multiome atlas [PDF]
Scientific Reports, 2022 Plasmalemmal ATP sensitive potassium (KATP) channels are recognized metabolic sensors, yet their cellular reach is less well understood. Here, transgenic Kir6.2 null hearts devoid of the KATP channel pore underwent multiomics surveillance and systems ...
D. Kent Arrell +8 more
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Structure of an open KATP channel reveals tandem PIP2 binding sites mediating the Kir6.2 and SUR1 regulatory interface [PDF]
Nature CommunicationsATP-sensitive potassium (KATP) channels, composed of four pore-lining Kir6.2 subunits and four regulatory sulfonylurea receptor 1 (SUR1) subunits, control insulin secretion in pancreatic β-cells.
Camden M. Driggers +4 more
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Dynamic duo: Kir6 and SUR in KATP channel structure and function [PDF]
ChannelsKATP channels are ligand-gated potassium channels that couple cellular energetics with membrane potential to regulate cell activity. Each channel is an eight subunit complex comprising four central pore-forming Kir6 inward rectifier potassium channel ...
Bruce L. Patton +4 more
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Pathophysiological Consequences of KATP Channel Overactivity and Pharmacological Response to Glibenclamide in Skeletal Muscle of a Murine Model of Cantù Syndrome [PDF]
Frontiers in Pharmacology, 2020 Cantù syndrome (CS) arises from mutations in ABCC9 and KCNJ8 genes that lead to gain of function (GOF) of ATP-sensitive potassium (KATP) channels containing SUR2A and Kir6.1 subunits, respectively, of KATP channels.
Rosa Scala +10 more
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