BY2EN2 Endocrinology Week 2 Each week, I will provide an overview of what will happen asynchronously (in your own time, at your own pace) and synchronously (live with me). Please make sure you have done any of the asynchronous work required before the synchronous session to make the most of it! When you are watching recordings, please do pause and make notes as well as clarifying things that you don't understand. The slides are all available on Blackboard. Asynchronously before the session Watch the recording entitled "G Protein-Coupled Receptors". Read Lim p.184- 186. Watch the recording entitled "G Proteins". Read Lim p.65-75. ? Research how cholera and pertussis toxins cause disease. Watch the recording entitled "GPCR Second Messengers".
Read Lim p.140-145. v v Write two MCQs based on the module so far and upload them to Blackboard using the Excel sheet provided. This will form the basis of a revision quiz for you. Synchronous session - Thursday 8th October 3-4pm Attend the synchronous session (and take part!).
2.1 G-protein coupled receptors lecture What are GPCRs? · Largest class of human cell surface receptors- over 1000 different types. · Involved in smell, taste, vision, hormone detection. . Characterised by 7 transmembrane domain- N terminal of a GCPR is on the outside of the cell and it passes through the membrane 7 times and end in the C terminal which is inside the cell. . There are many types of drugs that target GPCRS. Brand Name Generic Name Zyprexa Risperdal Claritin Imigran Cardura Tenormin Serevent Duragesic Imodium Cozaar Zantac Cytotec Zoladex Requip Atrovent Olanzapine Risperidone Loratidine Histamine H1 Sumatriptan Doxazosin Atenolol Salmeterol Fentanyl Loperamide Opioid Losartan Ranitidine Misoprostol Goserelin Gonadotrophin-releasing factor Ropinirole Ipratropium G-protein coupled receptor(s) Serotonin 5-HT2 and dopamine Serotonin 5-HT2 Serotonin 5-HT1B/1D a-adrenoceptor 81-adrenoceptor B2-adrenoceptor Opioid Angiotensin II Histamine H2 Prostaglandin PGE1 Dopamine Muscarinic Indication Schizophrenia, Antipsychotic Schizophrenia Rhinitis, Allergies Migraine Prostate hypertrophy Coronary heart disease Asthma Pain Diarrhea Hypertension Peptic ulcer Ulcer Prostate cancer Parkinson's disease Chronic obstructive pulmonary disease (COPD) · About 50% of pharmaceuticals target GPCRs, about 25% of them are top selling drugs. GPCR ligandstt . Photons . Taste and smell molecules . Pheromones · Histamines Hormones · And many more GPCR taxonomytt Large family of proteins. They are usually classified by phylogenetic analysis (aligning gene and protein structure with each other and looking for commonalities and building a family tree out of the GCPRs to give an overview of what the families look like. The GCPR super-family are divided into 5 distinct families based upon homology within the proteinstt · Glutamate-like GPCRs · Rhodopsin-like GPCRs · Adhesion-like GPCRs Frizzled-like GPCRs · Secretin-like GPCRS This is known as the GRAFTS system.