Exenatide
Exendin-4 Recombinant
Exendin-4 Recombinant produced in E.Coli is a non-glycosylated polypeptide chain containing 39 amino acids and having a molecular mass of approximately 4.2kDa. Exendin-4 is purified by proprietary chromatographic techniques.
Exendin, specifically Exendin-4, is a peptide hormone originally isolated from the saliva of the Gila monster. It is a glucagon-like peptide-1 (GLP-1) receptor agonist and shares approximately 50% sequence homology with the human GLP-1 hormone . Exendin-4 is classified as a GLP-1 receptor agonist and is used in its synthetic form, exenatide, for therapeutic purposes .
Key Biological Properties: Exendin-4 is known for its ability to stimulate insulin secretion, inhibit glucagon secretion, and slow gastric emptying . It has a longer half-life compared to human GLP-1, making it more stable and effective in therapeutic applications .
Expression Patterns and Tissue Distribution: Exendin-4 is not naturally occurring in humans but is derived from the Gila monster. In therapeutic applications, it is administered exogenously and acts on GLP-1 receptors distributed in various tissues, including the pancreas, brain, and gastrointestinal tract .
Primary Biological Functions: Exendin-4 primarily functions to regulate blood glucose levels by enhancing insulin secretion in response to meals, reducing glucagon secretion, and delaying gastric emptying .
Role in Immune Responses and Pathogen Recognition: While Exendin-4’s primary role is in glucose metabolism, recent studies suggest it may also have anti-inflammatory properties and could influence immune responses .
Mechanisms with Other Molecules and Cells: Exendin-4 binds to the GLP-1 receptor, mimicking the action of the endogenous GLP-1 hormone . This binding activates adenylate cyclase, increasing cyclic AMP (cAMP) levels, which in turn stimulates insulin secretion from pancreatic beta cells .
Binding Partners and Downstream Signaling Cascades: Upon binding to the GLP-1 receptor, Exendin-4 activates several downstream signaling pathways, including the cAMP/PKA pathway, which enhances insulin gene transcription and insulin secretion .
Regulatory Mechanisms Controlling Expression and Activity: The activity of Exendin-4 is regulated by its interaction with the GLP-1 receptor and subsequent activation of downstream signaling pathways .
Transcriptional Regulation and Post-Translational Modifications: As Exendin-4 is administered exogenously, its regulation is primarily at the level of receptor interaction and downstream signaling rather than transcriptional regulation .
Biomedical Research: Exendin-4 is extensively used in research to study glucose metabolism, insulin secretion, and potential neuroprotective effects .
Diagnostic Tools: While not commonly used as a diagnostic tool, Exendin-4’s effects on insulin secretion make it a valuable research tool for studying pancreatic function .
Therapeutic Strategies: Exendin-4, in its synthetic form exenatide, is used to treat type 2 diabetes by improving glycemic control . It is also being investigated for its potential neuroprotective effects and its role in weight management .
Role Throughout the Life Cycle: Exendin-4 plays a crucial role in managing blood glucose levels in individuals with type 2 diabetes, particularly in adults. Its potential neuroprotective effects are being explored for age-related cognitive decline . Additionally, its role in weight management may have implications for obesity treatment across different life stages .