Receptor Kinetics & Cell Signaling Flashcards
Pharmacodynamics
The effect of a drug on the body (as it binds to its target).
Pharmacokinetics
The availability of a drug within the body. (How a drug is carried/metabolized in body)
Main types of Receptors (4)
- Ligand-gated (ion channels; ionotropic receptors)
- Intracellular Receptors
- G-protein coupled Receptors
- Enzyme-linked receptors
A low Kd indicates…
A low Ka indicates…
…A high binding affinity
…A low binding affinity
Equation for Kd
[L] [R] / [LR]
Units: molar
Efficacy vs Effectiveness
How well the drugs works (regardless of patient) vs. How easy is it for a patient to use the drug?
GPCR Pathway (G-alpha)
Adenylyl Cyclase (AC) > (ATP>cAMP) .> PKA >further regulation
(GPCR) Phosphodiesterase function
Inhibitor. Converts cAMP to AMP
RTK Signaling Pathway
Enzymes Dimerize > Autophosphorylation of Tyr > PI3 Kinase (PIP 2>3) > PDK1 > AKT
Examples of RTK Receptors
EGF (Endothelial Growth Factor) & Insulin receptors