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- W3149795986 abstract "Antagonism of glucagon’s biological action is a proven strategy for decreasing glucose in diabetic animals and patients. To achieve full, potent, and selective suppression, we chemically optimized N-terminally truncated glucagon fragments for the identification and establishment of the minimum sequence peptide, [Glu9]glucagon(6–29) amide (11) as a full antagonist in cellular signaling and receptor binding (IC50 = 36 nM). Substitution of Phe6 with l-3-phenyllactic acid (Pla) produced [Pla6, Glu9]glucagon(6–29) amide (21), resulting in a 3-fold improvement in receptor binding (IC50 = 12 nM) and enhanced antagonist potency. Further substitution of Glu9 and Asn28 with aspartic acid yielded [Pla6, Asp28]glucagon amide (26), which demonstrated a further increase in inhibitory potency (IC50 = 9 nM), and improved aqueous solubility. Peptide 26 and a palmitoylated analogue, [Pla6, Lys10(γGluγGlu-C16), Asp28]glucagon(6–29) amide (31), displayed sustained duration in vivo action that successfully reversed glucagon-induced glucose elevation in mice." @default.
- W3149795986 created "2021-04-13" @default.
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- W3149795986 date "2021-04-06" @default.
- W3149795986 modified "2023-10-13" @default.
- W3149795986 title "Optimization of Truncated Glucagon Peptides to Achieve Selective, High Potency, Full Antagonists" @default.
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- W3149795986 doi "https://doi.org/10.1021/acs.jmedchem.0c02069" @default.
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