Pharmacology - L2

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  • Created by: Jess
  • Created on: 20-04-15 09:22
What is a receptor?
A molecule inside or on the surface of a cell that binds a specific ligand to produce a consistent physiological effect.
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What is an agonist?
A molecule that mimics the effect of the endogenous ligand at that receptor
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What is an antagonist?
A molecule that blocks the effects of the endogenous ligand.
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What is the orthosteric binding site?
The binding site of the endogenous ligand
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What is an allosteric modulator?
A molecule that regulates the function of a receptor but acts at a site distinct from the orthosteric binding site.
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What are the 4 main receptor types?
Ligand gated ion channels, kinase linked receptors, G protein coupled receptors and nuclear receptors.
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What are the main stages in receptor tyrosine kinase activation?
Dimerisation on ligand binding.Autophosphorylation of the C-terminal domains at specific tyrosine residues. Produces docking sites for proteins possessing SH2 domains. Forms a signalling cascade scaffold.
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What are the main structural features of a GPCR?
7 transmembrane domains. Extracellular N-terminus. Intracellular C-terminus. Single polypeptide chain.
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What are the 3 GPCR families?
Family A - rhodopsin-like. Family B - glucagon/secretin-like. Family C - metabotropic glutamate-like.
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What is the GRAFS classification?
Classification of GPCRs. G = Glutamate. R = Rhodopsin. A = Adhesion. F = Frizzled. S = Secretin.
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Describe the ligand binding site of family A GPCRs.
Specific residues within the transmembrane domains form the ligand binding site.
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Describe the ligand-receptor interaction at family B GPCRs.
Ligands are generally polar and bind via a two point attachment in the extracellular N-terminus.
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What are RAMPs?
Receptor activity-modifying proteins that selectively interact with some family B GPCRs to modify their properties (most commonly to form the functional receptor).
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What is the native form of a GPCR?
Dimeric or higher order oligomeric structures. Can be homomeric or heteromeric.
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What is the evidence that GPCRs are higher order oligomeric?
High weight bands on SDS-PAGE. Co-immunoprecipitation of epitope-tagged GPCRs. Live imaging of interactions using FRET. High power microscopy to visualise GPCR arrays.
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Does each GPCR monomer function independently?
Evidence suggests each dimer interacts with a single G protein.
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Card 2

Front

What is an agonist?

Back

A molecule that mimics the effect of the endogenous ligand at that receptor

Card 3

Front

What is an antagonist?

Back

Preview of the front of card 3

Card 4

Front

What is the orthosteric binding site?

Back

Preview of the front of card 4

Card 5

Front

What is an allosteric modulator?

Back

Preview of the front of card 5
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