Lecture 4 Drug Receptor Interaction

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11 Apr 2012
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Lecture 4 PCL201 Drug-Receptor Interactions
Drug interactions occur with biological proteins
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
Model Enzyme Substrate Interaction
The Lock and Key Model
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
oEnantiomers (mirror images)
Different enantiomers may interact differently, can affect doses
Can be inhibited (blocked through other molecules)
Reversible
Saturated
Nature of the interaction
One of the characteristics of living cells is the ability to recognize extracellular
stimuli and to respond by modifying their cellular physiology.
Multicellular organisms signal by one of two mechanisms:
oElectrical signals
oChemical signals
o
D+RDR Biological Response
Receptors are proteins that participate in intracellular
communication via chemical signals
Ligands are signaling molecules
Endogenous (natural to body) or exogenous
Neurotransmitter/Hormone or Drug (can change a signaling
process)
Effector molecules are those that are activated by the signaling
cascade and begin the biological response
G-protein adenylyl cyclase is effector
Drug-Receptor interaction
1. Have an effective concentration range
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