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The therapeutic agents that target ATP-sensitive potassium channels
- Source :
- Acta Pharmaceutica, Vol 66, Iss 1, Pp 23-34 (2016), Acta Pharmaceutica, Volume 66, Issue 1
- Publication Year :
- 2016
- Publisher :
- Walter de Gruyter GmbH, 2016.
-
Abstract
- ATP-sensitive potassium (KATP) channels are a major drug target for the treatment of type-2 diabetes. KATP channels are ubiquitously expressed and link the metabolic state to electrical excitability. In pancreatic β-cells, KATP channels are crucial in the regulation of glucose-induced insulin secretion. Also, KATP channels are involved in the protection against neuronal seizures and ischaemic stress in the heart, brain and in the regulation of vascular smooth muscle tone. Functional KATP channels are hetero-octamers composed of two subunits, a pore forming Kir6, which is a member of the inwardly rectifying potassium channels family, and a regulatory sulphonylurea receptor (SUR). In response to nucleotides and pharmaceutical agonists and antagonists, SUR allosterically regulates channel gating. The allosteric communication pathways between these two heterologus proteins in KATP channels are still poorly understood. This review will highlight the therapeutic agents that target KATP channels and are used to treat diabetes and cardiovascular diseases.
- Subjects :
- 0301 basic medicine
endocrine system
Vascular smooth muscle
Potassium
Allosteric regulation
Pharmaceutical Science
chemistry.chemical_element
Sulfonylurea Receptors
therapeutic agents
03 medical and health sciences
Drug Delivery Systems
0302 clinical medicine
KATP Channels
Humans
Nucleotide
Receptor
Pharmaceutical industry
Pharmacology
chemistry.chemical_classification
diabetes
Chemistry
Inward-rectifier potassium ion channel
cardiovascular
General Medicine
atp-sensitive potassium channels
inwardly rectifying potassium channels
Potassium channel
Cell biology
sulphonylurea receptor
030104 developmental biology
Diabetes Mellitus, Type 2
Pharmaceutical Preparations
Cardiovascular Diseases
Sulfonylurea receptor
HD9665-9675
Ion Channel Gating
hormones, hormone substitutes, and hormone antagonists
030217 neurology & neurosurgery
ATP-sensitive potassium channels
Subjects
Details
- ISSN :
- 18469558 and 13300075
- Volume :
- 66
- Database :
- OpenAIRE
- Journal :
- Acta Pharmaceutica
- Accession number :
- edsair.doi.dedup.....61dd0c977a180b960c689541e0937f8f