A competitive inhibitor that is converted to an irreversible inhibitor at the active site of the enzyme.
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What makes suicide substrates dangerous?
They are converted within the enzyme active site to a highly reactive species, which can form covalent bonds to amino acids in the active site.
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Define a receptor?
Protein molecules embedded within the cell membrane, with part of its structure on the outside of the cell.
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How is a receptor activated?
Receptors have selective binding sites for chemical messengers. The binding of messenger to receptor results in an induced fit.
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What is the structure and function of ion channel receptors?
This controls the movement ions across the cell membrane . It is made up of protein subunits. The lock gate controls movement through the channel.
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What is the structure and function of ligand-gated ion channel receptors?
Ligand-gated receptors are constructed of 5 kinked alpha helices which rotate when neurotransmitter binds.
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What is the structure and function of G-Protein coupled receptors?
Contain G-Proteins which are able to bind to the binding site when messenger binds by induced fit.
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What is the structure and function of kinase-linked receptor?
These are receptors that can activate enzymes directly. There is both a receptor and enzyme binding site.
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What is the function of an agonist?
They mimic the natural substrate and need to bind to the receptor in such a way to activate it.
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What key points must you consider when thinking about how an against should bind?
Drugs must have the correct binding groups, binding must be in the correct position, drugs must be the correct size for binding site
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Explain why agonists need binding groups?
Binding groups are needed so that binding interactions are able to form. Lack of binding interactions could lead to the neurotransmitters leaving the binding site slower.
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Explain why the position of binding groups in agonists is important?
If the binding groups are not positioned correctly then receptor activation will fail
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Explain why the size of the molecules in agonists is important?
Molecules must be the correct size to fit the space available and allow binding groups to align with binding regions within the target.
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What is the function of an antagonist?
They bind to the receptor in such a way that does NOT activate it. This will inhibit binding of the natural messenger
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What factors must be considered in antagonist binding?
Must have enhanced binding over natural substrate, uses extra binding regions causing an induced fit that deactivates the receptor, inhibits co-activator binding
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What bonds and interactions form between oestradiol and the oestrogen receptor?
Hydrogen bonds, VDW and hydrophobic interactions
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What is the umbrella effect?
Antagonists can bind to a site near the active site and provide an 'umbrella' over the active site.
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What is a partial agonist?
Exhibit both antagonist and agonist character. Binding may result in a conformational change and may lead to partial opening of an ion channel.
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What is an inverse agonist?
An inverse agonist has the same effect as the antagonist but can also prevent the activity associated with the natural equilibrium.
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Describe the structure and function of transport proteins?
This works by engulfing the polar molecule and releasing it across the membrane. The binding site recognises the polar molecules.
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Explore the therapeutic potential of targeting transport proteins?
You can develop drug molecules to mimic guest molecule, bind strongly to transport protein and block activity. This will increase levels neurotransmitters at nerve synapses.
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WhY is it necessary to target structural proteins?
Applications of anti-viral and anti-cancer drugs. Drugs can target receptors on the host cell wall.
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why is it necessary to target protein-protein interactions?
Many important processes involve the interaction between two proteins. Targeting these interactions could inhibit certain biological processes. However, for this large drug molecules would have to be used which would be hard to cross the membrane.
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Other cards in this set
Card 2
Front
What makes suicide substrates dangerous?
Back
They are converted within the enzyme active site to a highly reactive species, which can form covalent bonds to amino acids in the active site.
Card 3
Front
Define a receptor?
Back
Card 4
Front
How is a receptor activated?
Back
Card 5
Front
What is the structure and function of ion channel receptors?
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