PeptidePedia The community reference

Exenatide (revision 2)

Old revision·16:15, 28 Sep 2024·SecretagogueSol

This is an old revision of this page, as it stood at 16:15, 28 Sep 2024, saved by SecretagogueSol with the summary expand §Origin and sequence. It may differ substantially from the current revision, and any error it contains may since have been corrected.
Exenatide
INNexenatide
ClassGLP-1 receptor agonist
OriginSynthetic exendin-4
First approval2005
Compound infobox · conventions

Exenatide is a synthetic version of exendin-4, a 39-residue peptide isolated from the venom of the Gila monster, Heloderma suspectum. It shares approximately 53% sequence identity with human Glucagon-like peptide-1 and is a full agonist at the GLP-1 receptor. Approved in 2005, it was the first GLP-1 receptor agonist to reach the market.[1]

Its therapeutic relevance rests on an accident of sequence: exendin-4 carries glycine rather than alanine at position 2, so DPP-4 does not cleave it. No engineering was required to obtain protease resistance — the peptide is naturally resistant, and this is why a venom peptide became a diabetes drug.[1]

References

  1. ^ a b Nielsen LL, Young AA, Parkes DG. "Pharmacology of exenatide (synthetic exendin-4): a potential therapeutic for improved glycemic control of type 2 diabetes." Regulatory Peptides 117(2):77–88 (2004). PMID 14700743.