G-Protein Coupled Receptors (GPCRs)

by Kevin Ahern, PhD

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    So far I’ve talked about receptor systems that are functioning in fairly general terms. Let’s take a look up close and personal now at individual receptor system known as the G-protein coupled receptors, or as people refer them, the GPCRs. The GPCRs are G-protein coupled receptors, are a very abundant class of receptor proteins. There’s almost 800 genes in the human genome that are specifically in the form of G-protein coupled receptor sequences. Amazingly, almost 460 of these are olfactory, meaning that they’re involved in the process of smelling. So the GPCR depicted here is embedded in a lipid bilayer. And we’ve used color to identify the different regions of the protein projecting through the lipid bilayer. Though at the bilayer of course is shown in grey. The protein embedded in it has the different colors of blue, green, yellow and red. We see numbers associated with those and we see different colors associated with those. So each change of color represents a different portion of the protein that’s going from either down to up, or up to down, or down to up, and up to down, etcetera. This protein traverses the lipid bilayer by moving seven times up and down and up and down. So those are known as seven transmembrane domains and that’s where the name 7TM comes from. We can see that the protein has two distinct endings. One ending at the top that has a NH3+, that’s the amine end of the protein. And a carboxyl end of the protein in red at the bottom. Now, this orientation of the protein and lipid bilayer is specific for each individual protein. Now, the β-adrenergic receptor that I want to talk about is an example of one of the seven TMs, and it’s involved in working the process...

    About the Lecture

    The lecture G-Protein Coupled Receptors (GPCRs) by Kevin Ahern, PhD is from the course Hormones and Signal Transduction. It contains the following chapters:

    • G-Protein Coupled Receptors
    • GPCRs and G-Proteins
    • β-adrenergic Receptor Signaling – Creation of the Second Messenger

    Included Quiz Questions

    1. They often have seven transmembrane domains.
    2. They bind hormone with their intracellular domain.
    3. They are rare in the human genome.
    4. All of the answers are true.
    5. None of the answers are true.
    1. ...results in the production of cAMP by adenylate cyclase.
    2. ...causes the α subunit of a G-protein to become activated with GDP.
    3. ...stimulates the phosphatase activity of protein kinase A.
    4. All of the answers are true.
    5. None of the answers are true.

    Author of lecture G-Protein Coupled Receptors (GPCRs)

     Kevin Ahern, PhD

    Kevin Ahern, PhD

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