Drug Targets (Important) | Cheat Sheet - Edubirdie

University:
University of Wolverhampton
Course:
4PY019 | Pharmacy
Academic year:

2024
Views:

357

Pages:

2
Author:

Sara

1. How do ligand-gated ion channels work? 1) ligand binds to an allosteric complementary site on the ion channel /receptor 2) ion channel undergoes conformational change + opens so ions can enter/leave the cell 3) ion permeability increases generating a possible AP, by depolarising the inside of the membrane 4) ion channel closes when ligand unbinds 2. What binds to nicotinic receptors? - nicotine - ACh 3. Describe acetyl- acetyl groups are donated by acetyl coenzyme A, which choline synthe- are then covalently bonded to choline to form ACh sis: 4. What does acetylcholinesterase hydrolyse ACh into? choline + acetic acid 5. Why can beta because they are both very hydrophobic + gamma subunits freely move about in the cell's plasma membrane? 6. Describe how targeted muscarinic receptors cause the parasympathetic nervous system to relax: 1) muscarinic receptors in the heart are stimulated by ACh 2) this activates G proteins to open K channels 3) K+ ions diffuse out of the cell down their conc grad 4) this hyperpolarisation makes it harder for muscle cells in the heart to become depolarised + contract 7. Describe the ac- 1) ligand binds to extracellular site on the receptor tivation of ki2) this results in dimerization 3) this allows for autophosphorylation of the tyrosine ki1/2 nase-linked receptors: nase enzyme 4) intracellular proteins containing SH2 domains bind to the phosphorylated tyrosine in the intracellular domain 5) these bound SH2 domain-containing proteins now become activated + influence transcription + translation of proteins 8. What is dimeriza- where 2 receptors pair to form a dimer tion? 9. Describe a phosphate group is donated to the receptor by the bound autophosphoryla- ATP tion of tyrosine kinase enzyme: 2/2

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