Sandbox Reserved 1180: Difference between revisions
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Class B GPCRs contain 15 distinct receptors for peptide hormones and generate their signal pathway through the activation of adenylate cyclase (AC) which increases concentration of cAMP, inositol phosphate, and calcium levels in cyto. <ref>DOI 10.1111/bph.12689</ref> These signals are essential elements of intracellular signal cascades for human diseases including type II diabetes mellitus, osteoporosis, obesity, cancer, neurological degeneration, cardiovascular diseases, headaches, and psychiatric disorders; making their regulation through drug targeting of particular interest to companies developing novel molecules. <ref name= "Hollenstein 2014">DOI 10.1016/j.tips.2013.11.001</ref> Structurally based approaches to the development of small-molecule agonists and antagonists have been hampered by the lack of accurate Class B TMD visualizations until recent crystal structures of corticoptropin-releasing factor receptor 1 and human glucagon were realized. <ref name= "Hollenstein 2013">DOI 10.1038/nature12357</ref> <ref name= "Siu 2013">DOI 10.1038/nature12393</ref> | Class B GPCRs contain 15 distinct receptors for peptide hormones and generate their signal pathway through the activation of adenylate cyclase (AC) which increases concentration of cAMP, inositol phosphate, and calcium levels in cyto. <ref>DOI 10.1111/bph.12689</ref> These signals are essential elements of intracellular signal cascades for human diseases including type II diabetes mellitus, osteoporosis, obesity, cancer, neurological degeneration, cardiovascular diseases, headaches, and psychiatric disorders; making their regulation through drug targeting of particular interest to companies developing novel molecules. <ref name= "Hollenstein 2014">DOI 10.1016/j.tips.2013.11.001</ref> Structurally based approaches to the development of small-molecule agonists and antagonists have been hampered by the lack of accurate Class B TMD visualizations until recent crystal structures of corticoptropin-releasing factor receptor 1 and human glucagon were realized. <ref name= "Hollenstein 2013">DOI 10.1038/nature12357</ref> <ref name= "Siu 2013">DOI 10.1038/nature12393</ref> | ||
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The glucagon class B GPCR (GCGR) is involved in glucose homeostasis through the binding of the signal peptide glucagon. | The glucagon class B GPCR (GCGR) is involved in glucose homeostasis through the binding of the signal peptide glucagon. | ||
