Modulation of somatostatin receptors
After somatostatin binds to its receptor (SSTR5 complex), a chain of molecular events leads to decrease in insulin secretion (green circles) to the blood. In order to increase insulin release, somatostatin receptor can be blocked with a specifically designed substance (pink circles).
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Somatostatin regulates alpha- and beta-cells
Somatostatin is a hormone produced by delta cells in the pancreatic islets of Langerhans. This hormone has various functions in an organism, among others effective regulation of beta- and alpha-cells, secreting insulin and glucagon, respectively.
Somatostatin antagonist for higher insulin release
In pharmacological terms, antagonists are drugs which block a receptor from executing its function. When somatostatin binds to its receptor on beta-cells, there is a decrease in insulin production. An antagonist to somatostatin receptor will stimulate insulin release at high glucose levels.
Somatostatin agonist for lower glucagon release
In contrast to antagonist, an agonist binds to a receptor to stimulate its activity. When somatostatin binds to its receptor on alpha-cells, there is a decrease in glucagon production. An agonist to somatostatin receptor on alpha-cells will lead to prevention of glucagon release at high glucose levels.
Targeting receptors on both beta and alfa cells
It is possible to produce an attractive drug that would inhibit the beta-cell somatostatin receptor, while activating the alpha-cell somatostatin receptor. Today, Biocrine evaluates beta-cell and alpha-cell somatostatin receptor as potential novel drugable targets in the treatment of diabetes.
Suad Efendic