Allosteric, Biased-Signaling Modulators of the Cannabinoid Receptor One

              I attend the seminar on modulators and receptors. The speaker, Dr. Debra Kendall,  started with the GPCR superfamily saying that it was the largest receptor family with over 1000 members and constitutes for approximately 3% of the human genome. The GPCR superfamily serves as sensors which convert extracellular signals to intracellular signals. GPCR's can conform when ligands stabilize different active conformations which results in distinct affinities for various G-proteins. In other words there is functional selectivity of biased agonism. Certain functions that are mediated by the GOCRs in the central nervous system are cognition, memory, mood, stress, appetite, and pain. There are also mutations in GPCR that can lead to disease. For example GnRHR results in familial Gonadotropin Deficiency. GPCR's have proved to be key drug targets for products such as Claritin and Allegra. Then the speaker talked about Cannabinoid Receptors specifically Cannabinoid Receptor One. The receptors can bind to G proteins. Cannabinoid Receptor One is found primarily in the central nervous system and when activated are thought to affect movement, coordination, memory, sensation of pain, and appetite. The conclusion of the speakers talk showed that CB1 alters finding affinity for agonist and incurs agonist. It also inhibits G protein coupling activity. The speaker said that therapeutic agents can target GPCRs to bring about highly specific responses. Overall the seminar was interesting and I learned a lot of new things.