Exendin-4
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Overview
Exendin-4 is a naturally occurring 39-amino acid GLP-1 receptor agonist isolated from the saliva of the Gila monster lizard (Heloderma suspectum). It served as the basis for the development of exenatide (Byetta), the first GLP-1 receptor agonist approved for diabetes treatment. Exendin-4 has approximately 53% sequence homology with human GLP-1 but is resistant to DPP-IV degradation.
Mechanism of Action
Exendin-4 activates GLP-1 receptors with similar efficacy to native GLP-1 but with dramatically extended half-life due to DPP-IV resistance. This produces sustained appetite suppression, glucose-dependent insulin secretion, and slowed gastric emptying.
Key Research Areas
Considerations for Researchers
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