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Lectures 2 3 (receptors)
- 3. • Cell Membrane Lipids • Proteins • Receptors • Enzymes • Carrier proteins • Structural proteins • Nucleic acids • DNA • RNA • Carbohydrates • Cell surface carbohydrates • Antigen and recognition molecules Drug Targets Konrad H. Bleicher, Hans-Joachim Böhm, Klaus Müller & Alexander I. Alanine Nature Reviews Drug Discovery 2, 369-378 (May 2003)
- 4. Receptors
- 5. Drug-Receptor Interactions 1. Ionic (Electrostatic) Interactions
- 6. Drug-Receptor Interactions Ion-Dipole and Dipole- Dipole Interactions
- 11. Drug-Receptor Interactions Charge-Transfer Hydrophobic Interactions
- 12. Drug-Receptor Interactions π- π stacking Cation- π Interation
- 17. Theories of Drug-Receptor Interactions • Occupancy Theory –The intensity of the body’s response to the drug is directly related to the number of receptors occupied by the drug. –The maximum response occurs when all of the receptors have drug molecules attached.
- 18. Theories of Drug-Receptor Interactions • Rate Theory • Pharmacological response is not dependent on drug-receptor complex concentration but rather depends upon rate of association of drug and receptor.
- 19. Drug-Receptor Interactions • Two-state (Multi-state) Receptor Model • R and R* are in equilibrium (equilibrium constant L), which defines the basal activity of the receptor. • Full agonists bind only to R* • Partial agonists bind preferentially to R* • Full inverse agonists bind only to R • Partial inverse agonists bind preferentially to R • Antagonists have equal affinities for both R and R* (no effect on basal activity) • In the multi-state model there is more than one R state to account for variable agonist and inverse agonist behavior for the same receptor type.
- 20. Drug Chirality
- 23. Diastereomers
- 24. Receptor Chirality Roger A.H. Adan. Nature, Volume 27, Issue 4, 2006, 183–186
Notes de l'éditeur
- Intramolecular H. bonding becomes important if involved in stabilizing the conformation necessary for binding and activity
- Intramolecular H. bonding becomes important if involved in stabilizing the conformation necessary for binding and activity Ortho is a wek antibacterial while the para is a strong antibacterial
- Intramolecular H. bonding becomes important if involved in stabilizing the conformation necessary for binding and activity Ortho is a wek antibacterial while the para is a strong antibacterial
- Intramolecular H. bonding becomes important if involved in stabilizing the conformation necessary for binding and activity Ortho is a wek antibacterial while the para is a strong antibacterial