Professor Debra Kendall from the University of Connecticut gave a lecture about Allosteric Modulators and their pharmaceutical uses. She specifically spoke about the uses of cannabis in medicine and where it binds in the brain. The receptors come from a super family called GPCRs or G protein-coupled receptors. This is the largest receptor, checking in at over 1,000 members. That accounts for 3% of the human genome and 40% of current FDA approved. All of this considered only roughly 50 GPCRs are regularly targeted. GPCRs serve as sensors, converting extra-cellular signals to intracellular signals.
GPCRs also share conserved 2D secondary structure topology & 3D structural fold for the 7 transmembrane helices. Of all the medicines developed for targeting GPCRs, oncology is the field that is most provided for. Oncology accounts for 16% of medicines targeted for GPCRs.
She also said that different protein are meant to help in different areas, such as dopamine being helpful for movement or glutamate helping with retaining information. Professor Kendall spoke about why allosteric ligands are valuable in therapeutics. She pointed out the decreased toxicity and chances of side effects, the enahced physiological specificity, and functional selectivity. I admit that to fully understand a large portion of Professor Kendall's seminar, I would need more experience with chemistry, but I do think it was really quite interesting.
Her research seems pretty interesting. I wonder how this would impact the way medicines are made in order to stimulate particular parts of the brain.
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