GPCRs – structures, actions, drugs 1200-RGPRC-OG

GPCRs form a very large family of membranous transmitters of signals consisting of about 800 of various types of these receptors. Despite of participating in completely different signaling cascades which are influencing divergent cell processes their structures are uniform and consist of seven transmembrane helices. GPCRs are activated by enormous number of various ligands from photons and ions up to lipids, neurotransmitters, hormones, and small proteins. Because GPCRs pursue most of cell signaling they participate in many physiological and pathological processes and are molecular targets for 30%-50% of all currently used drugs.
In the lecture the structures of known complexes of GPCR-ligand (blocking or activating the receptor) as well as activation and signaling mechanisms on molecular and atomic levels will be shown. Also the connections of GPCRs with various diseases will be described. The following receptors will be presented among others: adrenergic receptors (adrenaline, cardiac and antiasthmatic drugs), dopamine receptors (dopamine, lack in Parkinson’s disease), 5-HT receptors (serotonin, LSD), muscarinic receptors (acetylcholine, lack in Alzheimer’s disease), opioid receptors (morphine and analgesics), cannabinoid receptors (anadamide, THC), histamine receptors (histamine and anti-allergic drugs).
Since GPCRs are molecular targets for “popular” hormones: acetylcholine (memory, learning), dopamine (love, passions), serotonin (happiness, satisfaction) they have their place in pop culture. These receptors are also targets for many narcotics. The structure of the first GPCR, rhodopsin, was determined only in 2000, and since then the interests in studying of GPCRs and substances they bind increased greatly.