Mechanism of pharmacochaperoning in a mammalian KATP channel revealed by cryo-EM
ATP-sensitive potassium (KATP) channels composed of a pore-forming Kir6.2 potassium channel and a regulatory ABC transporter sulfonylurea receptor 1 (SUR1) regulate insulin secretion in pancreatic β-cells to maintain glucose homeostasis.
Gregory M Martin +7 more
doaj +1 more source
Design, Synthesis, Activity and Docking Study of Sorafenib Analogs Bearing Sulfonylurea Unit
Two series of novel sorafenib analogs containing a sulfonylurea unit were synthesized and their chemical structures were confirmed by 1H-NMR, 13C-NMR, MS spectrum and elemental analysis.
Chunjiang Wu +6 more
doaj +1 more source
Stimulation of glucose utilization in 3T3 adipocytes and rat diaphragm in vitro by the sulphonylureas, glimepiride and glibenclamide, is correlated with modulations of the cAMP regulatory cascade [PDF]
The long-term hypoglycemic activity of sulphonylurea drugs has been attributed, in part at least, to the stimulation of glucose utilization in extra-pancreatic tissues. The novel sulphonylurea, glimepiride, gives rise to a longer lasting reduction in the
Wetekam, Eva-Marlen +5 more
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Natriuretic peptide receptor-C regulates coronary blood flow and prevents myocardial ischemia/reperfusion injury: novel cardioprotective role for endothelium-derived C-type natriuretic peptide [PDF]
Background: Ischemia/reperfusion (I/R) injury complicates myocardial infarction and stroke by exacerbating tissue damage and increasing risk of mortality.
Ramona Scotl +15 more
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The unusual stoichiometry of ADP activation of the KATP channel
KATP channels, oligomers of 4 pore-forming Kir6.2 proteins and 4 sulfonylurea receptors (SUR), sense metabolism by monitoring both cytosolic ATP, which closes the channel by interacting with Kir6.2, and ADP, which opens it via SUR.
Eric eHosy, Michel eVivaudou
doaj +1 more source
Neonatal diabetes is a rare disease, often caused by a monogenic abnormality. A male infant patient developed diabetic ketoacidosis at 2 months‐of‐age due to the heterozygous ABCC8 gene mutation (p.Pro1198Leu).
Shinsuke Uraki +14 more
doaj +1 more source
Determination of the molecular mass of the native beta-cell sulfonylurea receptor. [PDF]
In the present study we have determined the molecular mass of the beta-cell sulfonylurea receptor in its native form by two different experimental approaches; gel filtration chromatography and radiation inactivation analysis.
Ashcroft, SJ +18 more
core +1 more source
Treatment of type 2 diabetes: the stability of the effectiveness of hypoglycemic medications
This article is dedicated to the problem of glycaemic durability of drugs used in treatment of type 2 diabetes. The results of studies comparing durability of glycemic control as monotherapy or in combination of metformin with different drugs: dipeptidyl
Tat'yana Morgunova, Valentin Fadeev
doaj +1 more source
As a first step, the authors emphasise lifestyle changes (increased physical activity, stopping smoking), blood pressure control, and lowering cholesterol).
Giacomo Gastaldi +8 more
doaj +1 more source
Sulfonylurea is associated with higher risks of ventricular arrhythmia or sudden cardiac death compared with metformin: A population-based cohort study [PDF]
Background Commonly prescribed diabetic medications such as metformin and sulfonylurea may be associated with different arrhythmogenic risks. This study compared the risk of ventricular arrhythmia or sudden cardiac death between metformin and ...
Jeremy Man Ho Hui +13 more
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