PCL201H1 Lecture 4: Lecture 4 Drug Receptor Interaction
Document Summary
Most drug-receptor interactions are: reversible, via weak chemical bonds. Irreversible drug-receptor interactions are: rare, via strong chemical bonds (aspirin or anti-tumor drugs, undesirable, e. g. aspirin cox bind irreversibly. Natural compound/agonist binds to receptor to initiate signaling cascade. Drug mimics natural compound (similar chemical interactions), activates signaling cascade. Drug-receptor interaction similar to substrate-enzyme reaction: specific, enantiomers (mirror images, can be inhibited (blocked through other molecules, reversible, saturated. Different enantiomers may interact differently, can affect doses. Drug-receptor interaction: have an effective concentration range, e. g. Minimal concentration to initiate, maximum concentration to saturate: have biological specificity physiological response. Mechanisms to convey chemical signal from outside to inside the cell. Ion channels (ligand gated or ionotropic and voltage gated) 1: g-protein coupled receptors (gpcr or metabotropic, transmembrane enzyme receptors (receptor tyrosine kinases, nuclear hormone receptors (lipid soluble, water soluble signals, these bind to specific plasma membrane receptors, receptor-ligand complex activates/alters a cascade of events in cell, e. g.
