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32 Cards in this Set
- Front
- Back
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What are the two types of receptors? |
Membrane Bound Receptors and intracellular receptors. |
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What is a GPCR? |
G-Protein Coupled Receptors, sometimes referred to as 7TM or 7 Trans-Membrane protein. Usually has a G-Protein inside the cell. Most common receptors and the biggest. |
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Explain what it means when someone refers to a GPCR as a 7TM or 7 Trans-Membrane protein. |
The protein has 7 different instances where the protein crosses the membrane before you ultimately have one side of the protein that sits inside the cell, and one side that its outside the cell. Usually N terminus is inside the cell, and the C terminus is outside the cell. It doesn't always have to be that way. |
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What is a G-protein? |
A GTP binding protein, which turns the receptor on. The receptor is closed by the bound GTP becoming hydrolyzed once turning it into GDP which turns off the receptor. |
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In order for a G-Protein bound to GDP to activate the corresponding receptor what has to happen? |
GDP must be removed from the protein and the G-Protein must bind to a new GTP molecule. |
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Can you have a partial agonist/antagonist to achieve partial activation/deactivation? |
Yes. |
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Two main nucleophiles to remember. Amino Acids... |
Cystine and Lysine. |
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What are two types of membrane bound receptors? |
GPCR aka 7TM, and ion channels. |
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What are two types of intracellular receptors? |
Nuclear receptors and secondary receptors. |
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What is an Assay? |
An examination or determination of characteristics |
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What is an IC50? |
The concentration at which 50% inhibition takes place. Plot looks like a titration curve. |
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What is an IC90? |
The concentration at which 90% inhibition takes place |
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When is an IC90 typically performed? |
It is typically determined when evaluating infectious diseases/disease targets |
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Is there more or less error associated with an IC90 vs an IC50. |
There is often less error associated with an IC90. |
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What is an EC50? |
The concentration at which 50% of the targeted activity is observed. Plot looks like a titration curve. |
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What is an ED50? |
The dose at which 50% of the targeted activity is observed |
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What is an LC50? |
The concentration at which 50% of the targeted population is killed |
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What is an LD50? |
The dose at which 50% of the targeted population is killed |
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How is Therapeutic Index calculated? |
LD50/ED50 = TI |
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A colorimetric assay is really a measurement of ________ _______. Using a particular __________ allows for selectivity. |
Light absorption. Using a particular wavelength (color) allows for selectivity |
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A fluorometric assay typically has increased _________-_____-________ ratio because incidental interference is decreased |
Signal-to-Noise. |
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A chemiluminescent assay accurately measures ______ given off as a result of a ________. |
A chemiluminescent assay accurately measures light given off as a result of a reaction |
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A radiometric assay measures the presence of a _____________ _____________. |
A radiometric assay measures the presence of a radioactive element |
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What is GFP? |
GFP (Green Fluorescent Protein) stems from a relatively small (27 kDa) protein originally isolated from jellyfish. |
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What does ELISA stand for? What does ELISA use for detection? |
ELISA (Enzyme-Linked ImmunoSorbent Assay) uses a specific antigen/antibody relationship for detection |
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True or False? The presence of just about any molecule can be detected and quantified if an antibody is available or can be found in an ELISA assay? |
True. |
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What does FRET stand for? What does it measure? |
FRET (Fluorescence Resonance Energy Transfer) is a measurement of fluorescence between two different molecules and depends on distance. |
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What are 3 key things to have for assay design? |
1.) Good controls, you have to be able to show that the process occurs AND that it can be stopped. 2.) Good reproducibility, reagents are reliably available and don’t have batch-to-batch variability. 3.) It can't be cost prohibitive. |
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What is the definition of Pharmacokinetics? |
The characteristic interactions of a drug candidate and the body in terms of its Absorption, Distribution, Metabolism and Excretion. (ADME) |
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What is Pharmacodynamics? |
A branch of pharmacology dealing with the reactions between drugs and living systems. |
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What is the simple definition of Pharmacokinetics? |
What the body does to the drug. |
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What is the simple definition of Pharmacodynamics? |
What the drug does to the body. |
