desHis1Glu9-glucagon-[mPEG] and desHis1Glu9(Lys30PAL)-glucagon: Long-acting peptide-based PEGylated and acylated glucagon receptor antagonists with potential antidiabetic activity.

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Abstract

Glucagon is hormone secreted from the pancreatic alpha-cells that is involved in blood glucose regulation. As such, antagonism of glucagon receptor signalling represents an exciting approach for treating diabetes. To harness these beneficial metabolic effects, two novel glucagon analogues, desHis1Glu9-glucagon-[mPEG] and desHis1Glu9(Lys30PAL)-glucagon, has been evaluated for potential glucagon receptor antagonistic properties. Both novel peptides were completely resistant to enzymatic breakdown and significantly (P
LanguageEnglish
Pages43-51
JournalEuropean Journal of Pharmacology
Volume709
Issue number1-3
DOIs
Publication statusPublished - 2 Apr 2013

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Glucagon Receptors
Glucagon
Hypoglycemic Agents
Peptides
Glucagon-Secreting Cells
Blood Glucose
Hormones

Cite this

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abstract = "Glucagon is hormone secreted from the pancreatic alpha-cells that is involved in blood glucose regulation. As such, antagonism of glucagon receptor signalling represents an exciting approach for treating diabetes. To harness these beneficial metabolic effects, two novel glucagon analogues, desHis1Glu9-glucagon-[mPEG] and desHis1Glu9(Lys30PAL)-glucagon, has been evaluated for potential glucagon receptor antagonistic properties. Both novel peptides were completely resistant to enzymatic breakdown and significantly (P",
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AU - Irwin, Nigel

AU - Franlin, ZJ

AU - O'Harte, Finbarr

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