A hormone made up of one alpha chain and one beta chain connected by disulfide bonds and released by the pancreas
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What are rapid acting insulins?
Cause changes to prevent the formation of insulin dimers so more effective at stimulating the receptor
These are used for injection after eating or in pumps
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What are some examples of rapid acting insulins?
Lispro- lysine and proline residues reversed on the C-terminal end of the beta-chain.
Aspart - substitution of a prolie for aspartic acid.
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What are long acting insulins?
Percipitate in the subcutaneous tissue allowing for slow release or increase affinity for serum albumin which extend their life span in serum.
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What are some examples of long acting insulins?
Degludec - deletion of threonine in the position B30, percipitates in tissue
LY2605541 - insulin glargine, percipitates in tissue
Detemir - deletion of threonine at B30, binds to albumin
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What do insulin secretagogues do?
Stimulate the release of inuslin from beta cells
Rapid acting given just before a main meal
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What do insulin secretagogues need to work?
Active pancreatic beta cells so thats why its only prescribed to type 2 diabetics in combination with insulin sensitisers
Act on the sulphonylurea receptor (SUR)
SUR proteins are subunits of the inward-rectifier potassium ion channels Kir6.1/6.2
Four Kir6.1/6.2 and four SUR subunits from the KATP channel
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How do sulphonylureas work?
They cause K+ channels to close independent of ATP causing depolarisation leading to insulin synthesis and release
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What are some key features of Glinides?
Similar route as sulphonylureas - rapid onset and short duration of action but they have: Weaker binding affinity and faster dissociation from the SUR1 binding site.
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Other cards in this set
Card 2
Front
What are rapid acting insulins?
Back
Cause changes to prevent the formation of insulin dimers so more effective at stimulating the receptor
These are used for injection after eating or in pumps
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