G protein-coupled receptors Throughout this course you will have many opportunities to respond to other people’s opinions and comments by participating in the discussion. It is helpful to complete your reading prior to answering the discussion topics. Nearly half of all non-antibiotic prescriptions drugs target cell surface receptors called G protein-coupled receptors (Appling et al., 2019). After completion of the human genome project, studies suggest that there are at least 800 different G protein-coupled receptors (GPCRs), making them the largest and most diverse group of membrane receptors in eukaryotes. GPCRs bind a variety of signaling molecules, or ligands, and play an important role in a wide variety of functions in the human body, making them good targets for drugs. Resource: Appling, D. R., Mathews, C. K., & Anthony-Cahill, S. J. (2019). Biochemistry: Concepts and connections. Pearson. For this unit’s discussion you will need to respond to the following: Once bound to a signaling molecule or ligand, a GPCR undergoes a conformational change that then triggers an interaction with a nearby G protein. What are G proteins? How is a G protein activated? How is a G protein inactivated? Activation of a single G protein can result in the production of hundreds or even thousands of second messenger molecules. What is a second messenger? Provide an example of a second messenger and its role in the cell. GPCRs help regulate an enormous range of bodily functions and therefore are the targets of many pharmaceutical drugs. Do some research and identify a drug that targets GPCR. What is the name of the drug? What is the drug used to treat? What is the mechanism of action of the drug? Caffeine is consumed worldwide and elicits some of its effects by targeting adenosine receptors, which are GCPRs. What types of caffeinated beverages do you consume? Do some research on the effects of caffeine and share some pros and cons. Based on your research, do you think it is possible to consume too much caffeine? Why or why not?
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