GPCRs!

I went to a department seminar and it was about allosteric modulators and biased-signaling modulators of the cannabinoid reception one. The speaker was Dr. Debra Kendall and she works in the pharmacy school at the University of Connecticut. She started the lecture by introducing the GPCR (G-protein coupled receptor)  protein receptor. It’s the largest receptor family and it makes up three percent of the human genome. There are good and bad things about the GPCR. She was saying that the good was that it’s so heavily integrated into human physiology and are really important for science and the bad is that there are only a few GPCR receptors we can target. Dr. Kendall mentioned that she really wants to contribute to science by finding more ways to modify them so they are more easily targeted.  

                GPCRs are involved in many things including drug discovery, the central nervous system, and diseases. Forty percent of the central nervous system is targeted by the GPCR making it the most targeted area. The functions mediated by the GPCRs in the central nervous system are cognition, memory attention, movement, mood, stress, appetite, and pain. Mutations in the GPCRs can lead to diseases like Rhodopsin which causes blindness. Some common drugs that are targeted by GPCRs are Claritin, Allegra, and Zyprexa. At this point in the lecture she was showing various structures of molecules dealing with proteins. I got really excited because I knew how to name and identity parts of the structures! I knew all about the stereochemistry and the benzene molecules involved!

                To wrap up the lecture, Dr. Kendall went into allosteric modulation. Pretty much, allosteric modulation are compounds that bind to an allosteric site that is topographically distinct from the orthostatic site and modulate the binding and/or signaling of an orthosteric ligand. They are valuable to therapeutics because they decrease toxicity or side effects, fine tune pharmacological responses, and they have more pharmacophore diversity than orthosteric ligands. She even went on to discuss weed! She briefly went into how the THC receptors bind to the cannabinoid receptors. Overall I think the lecture was way over my head, but I appreciate the opportunity to hear about great things going on in science.