What is an Inverse Agonist? - ✔✔Shift equilibrium towards inactive state
What is the Cubic Ternary Complex? - ✔✔G proteins bind to inactive receptor
Amplification is _______ ______ and _______________________ - ✔✔System Dependent
a Function of Distance
MOD2-✔✔
What are the 4 types of binding assays? - ✔✔Radioactive Assay
Fluorescence Assay
Polarization Assay
FRET Assay
What is Scintillation proximity? - ✔✔a radio-isotopic technology format used to measure a wide
range of biological interactions, including drug-target binding affinity studies
What is Surface Plasmon Resonance? - ✔✔a phenomenon where the electrons in the metal
surface layer are excited by photons of incident light with a certain angle of incidence, and then
propagate parallel to the metal surface
What are the three types of binding experiments? - ✔✔Saturation binding
, Displacement binding
Kinetics
What are the two types of binding that happen in binding experiments? - ✔✔Specific binding -
Drug bound to target site
What is the formula for specific binding? - ✔✔[A]/[A] + Kd
What is the formula for nonspecific binding? - ✔✔nsb = k*[A]
What is the formula for total binding? - ✔✔([A]*Bmax /[A] + Kd ) + k * [A]
What is a Scatchard Plot? - ✔✔plots the total amount of bound ligand divided by its
free concentration (B/[L]) against the total bound ligand, B.
What are the three types of displacement binding? (3) What is there impact on IC50? -
✔✔Competitive - As the concentration of radioligand goes up, IC50 goes up.
Noncompetitive - IC50 does not change with increasing radioligand
Allosteric - IC50 goes up with increasing radioligand Complete inhibition is not possible at
high concentrations of radioligand (saturable)
What are the first 4 criteria for Binding Experiments? - ✔✔1. The binding is saturable
2. The binding is reversible and able to be displaced by other ligands
3. There is a ligand available to determine non-specific binding.
4. There is sufficient biological binding material to yield a good signal-to-noise ratio but no too much so
as to cause depletion of the tracer ligand.
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