Friday, July 13, 2012

Exendin - A New Incretin?

ADA June 2012 Conference


Alpha cells and the origin of glucagon-like sequences and their receptors

David M. Irwin, Department of Laboratory Medicine and Pathobiology, University of Toronto


Summary of presentation:

Incretin Hormones – 2 known human incretin hormones
-          Glucagon-like peptide 1 (GLP-1)
-          Glucose-dependent insulinotropic peptide (GIP)

Other incretins = Exendin
-          Long acting GLP-1 analogue
o   Acts through the GLP-1 receptor
o   Have increased circulating half-life
o   Synthetic version marketed
-          From the venom of a lizard (Gila monster)
-          No known orthologs in vertebrates, not a product of the proglucagon gene
-          Anole Lizard Exendin – sequence of peptides are not similar to GLP-1 or GIP (human genome)
-          Other animals had similar exendin to lizard (chicken, turkey, duck, zebra finch, xenopus)
-          Exendin 1, 2, 3,and 4 sequences – exendin 3 and 4 are GLP-1 like in their sequence and function; exendin 1 and 2 similar to the are GIP-like in sequence and function
-          Expression of the exendin gene in the chicken and xenopus brain – who knows what it is duing there?
-          No exendin gene in human genome!
-          Exendin genes are found in birds, reptiles and frogs
-          No obvious candidate receptor for exendin; glucagon, GLP1, GLP2, and GIP act through related receptors
-          There are novel group of receptors present in fish, reptiles, birds that are NOT present in mammals – why do mammals not have this gene?
-          GLP1 receptors not found in fish
-          GCGR – duplicated in fish (glucagon receptors)
-          GLP2R – single copy in all species
-          GIPR – no intact gene found in birds
-          GRLR – not found in mammals (glucagon-receptor-like-receptors

Conclusion
o   Genomic data useful for identifying new genes
o   Continues to yield surprises
o   Hormone and receptor families are larger and more complex
-          Open questions
o   What does exendin do in other vertebrates?
o   Is GRLR the receptor for exendin?
o   Why do humans (all mammals) not have Exendin/GRLR?
o   What ligand/receptor has replace the function of Exendin/GRLR in mammals?


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