Cannabinoid Receptor One
On Friday, November 21 2014, Dr. Debra Kendall of the University of Connecticut visited the UNCG campus to present a seminar about Cannabinoid Receptors. The seminar addressed research conducted by Dr. Kendall and her colleagues in regards to the Cannabinoid Receptor One and its physiological function in the human body. Her research, titled Allosteric, Biased-Signaling Modulators of the Cannabinoid Receptor One: Thinking Outside the Active Site, provided a very in-depth and insightful discussion about the cannabinoid CB1 receptor's binding patterns and effects on the body.
HIGHLIGHTS
- CB1 allosteric modulator ORG 27569, is a drug which acts as a allosteric modulator of the cannabinoid CB1 receptor. Its effects include alteration of the binding affinity for agonist and inverse agonist, inhibition of G protein coupling activity, and activation of downstream signaling of periodic mechanical stress activates MEK1/2-ERK1/2.
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| ORG 27569. Chemical formula C24H28ClN3O. |
- Ligand biased signaling of allosteric modulator LDK1258 inhibits feeding behavior in animals.
- Therapeutic agents can target GPCR's to bring about highly specific responses.
DISCUSSION
According to Dr. Kendall's research, the cannabinoid CB1 receptor is a class A, G protein-coupled receptor. GPCR's constitute one of the largest protein receptor families. They are known for being a family of receptors that are signaled from outside the cell, yet still activate inside the signal transduction pathway. GPCR's are also known as seven - trans membrane domain receptors due to the fact that they pass through the cell membrane seven times.
G protein-coupled receptors, including the cannabinoid CB1 receptor discussed in this seminar are found only in eukaryotes. Dr. Kendall's research particularly focused on the allosteric regulation. Allosteric regulation can be defined as a protein that binds to an effector molecule at a site other than the protein's active site. Orthosteric agonists bind to the GPCR, which causes a conformational change that results in signalling.
In conclusion, her research uncovered several interesting discoveries. I had never attended a Chemistry/Biochemistry seminar before this extra credit opportunity presented itself, but am glad I attended this one. Although I struggled with understanding some of the concepts addressed during the seminar, after some research based on the notes that I took while listening to Dr. Kendall, I can honestly say that I learned a great deal from her presentation. It is amazing just how much information was packed into her hour long seminar, but the hour spent learning about Cannabinoid Receptors was well worth it.
Hi Jessica,
ReplyDeleteVery detailed and well made blog. The lecture sounds very information but fun to have listened to. Once they are activated, what do MEK1/2-ERK1/2 do?