20-03-2012, 04:30 PM
Drug-Receptor Interactions
Drug-Receptor interactions.ppt (Size: 618.5 KB / Downloads: 115)
What are receptors?
Traditional model was a rigid “Lock and Key”
Lock Receptor surface
Key Drug or Ligand
Drug-Receptor Interactions
Receptors fluid, flexible surfaces or pockets
Can change 3-D structure as ligand docks
Most receptors are sites for natural ligands
Small portion or surface of a macromolecule
Includes: Enzymes, components of cell membranes, intracellular protein or nucleic acid, antibodies, DNA, RNA
Ligand - Receptor docking structure changes
Changes “function”
Drug-Receptor Interactions
Membrane bound receptors
Receptors of membranes are primarily proteins
If the gene sequence is known: site directed mutagenesis
Alter one or more amino acids in the receptor
Has this changed the biological responses to a particular ligand?
How has altering the amino acid within the receptor altered the intramolecular forces that hold the ligand in the receptor?
Number of internal hydrogen bonds amide bonds
Number of hydrophobic interactions
van der Waal’s forces
Ionic interactions
Small molecule interaction with a membrane receptor
Can result in a large change in protein conformations
Structural and physical properties of membrane changes