Binding of sulphonylureas to plasma proteins – A KATP channel perspective
نویسندگان
چکیده
منابع مشابه
Independent trafficking of KATP channel subunits to the plasma membrane.
KATP channels are unique in requiring two distinct subunits (Kir6.2, a potassium channel subunit) and SUR1 (an ABC protein) for generation of functional channels. To examine the cellular trafficking of KATP channel subunits, green fluorescent protein (GFP) was tagged to the cytoplasmic N or C terminus of SUR1 and Kir6. 2 subunits and to the C terminus of a dimeric fusion between SUR1 and Kir6.2...
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The hepcidin hormone of 25 amino acid residues (hepcidin25) is a key regulator of iron homeostasis (1 ). Hepcidin has been shown to bind in vitro to 2macroglobulin ( 2M) and albumin in human plasma (2 ). It is not known, however, to what extent hepcidin is bound to proteins in vivo. For purposes of clinical interpretation, it is critical to know whether protein-bound or free hepcidin is being q...
متن کاملMolecular action of sulphonylureas on KATP channels: a real partnership between drugs and nucleotides
Sulphonylureas stimulate insulin secretion from pancreatic β-cells primarily by closing ATP-sensitive K(+) channels in the β-cell plasma membrane. The mechanism of channel inhibition by these drugs is unusually complex. As direct inhibitors of channel activity, sulphonylureas act only as partial antagonists at therapeutic concentrations. However, they also exert an additional indirect inhibitor...
متن کاملCorrection: Molecular action of sulphonylureas on KATP channels: a real partnership between drugs and nucleotides.
“IC is the current in drug free solution obtained by averaging the current before and after application, IC50 is the drug concentration at which the inhibition is half maximal, h is the Hill coefficient, L is a scaling factor reflecting the difference between channel activity in control and MgATPcontaining solution (L = 1 in the absence of the nt) and a is the fraction of KATP current remaining...
متن کاملLeptin-stimulated KATP channel trafficking
Insulin secretion from pancreatic β-cells is initiated by the closure of ATP-sensitive K+ channels (KATP) in response to high concentrations of glucose, and this action of glucose is counteracted by the hormone leptin, an adipokine that signals through the Ob-Rb receptor to increase KATP channel activity. Despite intensive investigations, the molecular basis for KATP channel regulation remains ...
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ژورنال
عنوان ژورنال: PLOS ONE
سال: 2018
ISSN: 1932-6203
DOI: 10.1371/journal.pone.0197634