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Questions and Answers
What is a characteristic of uncompetitive inhibitors?
What is a characteristic of uncompetitive inhibitors?
- They bind to the enzyme-substrate complex. (correct)
- They can be overcome by increasing the substrate concentration.
- They are more effective at low substrate concentrations.
- They are more common than competitive inhibitors.
What is the purpose of designing drugs that mimic the transition state of an enzyme-catalysed reaction?
What is the purpose of designing drugs that mimic the transition state of an enzyme-catalysed reaction?
- To mimic the substrate or product.
- To increase the substrate concentration.
- To bind more strongly to the enzyme. (correct)
- To inhibit the enzyme's activity.
What is the result of renin inhibitors blocking the synthesis of angiotensin I and II?
What is the result of renin inhibitors blocking the synthesis of angiotensin I and II?
- Decreased blood pressure. (correct)
- Unchanged blood pressure.
- Increased blood pressure.
- No effect on blood pressure.
What is the role of angiotensin II in the body?
What is the role of angiotensin II in the body?
What is the mechanism by which renin inhibitors lower blood pressure?
What is the mechanism by which renin inhibitors lower blood pressure?
What is the purpose of designing transition-state analogues?
What is the purpose of designing transition-state analogues?
What is the role of renin in the body?
What is the role of renin in the body?
What is the result of increasing the substrate concentration in the presence of an uncompetitive inhibitor?
What is the result of increasing the substrate concentration in the presence of an uncompetitive inhibitor?
What is a possible reason why drugs with a different skeleton to the substrate can act as competitive inhibitors?
What is a possible reason why drugs with a different skeleton to the substrate can act as competitive inhibitors?
What type of inhibitors can resemble the product of an enzyme-catalyzed reaction more closely than the substrate?
What type of inhibitors can resemble the product of an enzyme-catalyzed reaction more closely than the substrate?
What is the mechanism of action of competitive inhibitors that do not compete with the substrate?
What is the mechanism of action of competitive inhibitors that do not compete with the substrate?
What is a characteristic of irreversible inhibitors?
What is a characteristic of irreversible inhibitors?
Why do irreversible inhibitors block the affected enzyme permanently?
Why do irreversible inhibitors block the affected enzyme permanently?
What type of functional group is commonly found in effective irreversible inhibitors?
What type of functional group is commonly found in effective irreversible inhibitors?
What happens to the substrate when an irreversible inhibitor binds to the active site?
What happens to the substrate when an irreversible inhibitor binds to the active site?
Why does increasing substrate concentration not reverse the inhibition of irreversible inhibitors?
Why does increasing substrate concentration not reverse the inhibition of irreversible inhibitors?
What is the function of the hydroxyethylene transition-state mimic in Aliskiren?
What is the function of the hydroxyethylene transition-state mimic in Aliskiren?
What is the characteristic of the transition-state inhibitor Aliskiren?
What is the characteristic of the transition-state inhibitor Aliskiren?
What is the role of the tetrahedral intermediate in enzyme-catalyzed reactions?
What is the role of the tetrahedral intermediate in enzyme-catalyzed reactions?
Which of the following is an example of a transition-state inhibitor?
Which of the following is an example of a transition-state inhibitor?
What is the function of the two aspartyl residues in enzyme-catalyzed reactions?
What is the function of the two aspartyl residues in enzyme-catalyzed reactions?
What is the mechanism of inhibition of ACE inhibitors?
What is the mechanism of inhibition of ACE inhibitors?
What is the mechanism by which clavulanic acid functions?
What is the mechanism by which clavulanic acid functions?
What is the bond formed between the enzyme and the suicide substrate?
What is the bond formed between the enzyme and the suicide substrate?
What is the name of the enzyme inhibited by clavulanic acid?
What is the name of the enzyme inhibited by clavulanic acid?
What is the outcome of the reaction between the enzyme and the suicide substrate?
What is the outcome of the reaction between the enzyme and the suicide substrate?
What is the byproduct of the condensation reaction?
What is the byproduct of the condensation reaction?
What is the function of the CH3 group in the suicide substrate?
What is the function of the CH3 group in the suicide substrate?
What is the type of inhibition exhibited by clavulanic acid?
What is the type of inhibition exhibited by clavulanic acid?
What is the role of the fluorine atom in the suicide substrate?
What is the role of the fluorine atom in the suicide substrate?
What is the outcome of the reaction between the enzyme and the substrate in the absence of the suicide substrate?
What is the outcome of the reaction between the enzyme and the substrate in the absence of the suicide substrate?
What type of inhibitors are converted to irreversible inhibitors by the enzyme-catalysed reaction?
What type of inhibitors are converted to irreversible inhibitors by the enzyme-catalysed reaction?
What is the purpose of using clavulanic acid in antibacterial medication?
What is the purpose of using clavulanic acid in antibacterial medication?
What is the function of Trifluoroalanine in the context of enzyme inhibition?
What is the function of Trifluoroalanine in the context of enzyme inhibition?
What is the product of the reaction between pyridoxal phosphate and alanine?
What is the product of the reaction between pyridoxal phosphate and alanine?
What is the role of the enzyme transaminase in the reaction between pyridoxal phosphate and alanine?
What is the role of the enzyme transaminase in the reaction between pyridoxal phosphate and alanine?
What is the structure of the molecule shown in the figure?
What is the structure of the molecule shown in the figure?
What is the functional group of the molecule shown in the figure?
What is the functional group of the molecule shown in the figure?
What is the type of inhibition that occurs when a suicide substrate reacts with an enzyme?
What is the type of inhibition that occurs when a suicide substrate reacts with an enzyme?
What is the purpose of using transition-state inhibitors?
What is the purpose of using transition-state inhibitors?
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Study Notes
Competitive Inhibitors
- Can bind to a combination of binding regions within the active site, some used by the substrate and some not
- Can resemble the structure of the product more closely than the substrate
- Some competitive inhibitors bind to the active site but do not compete with the substrate, instead occupying the binding region normally occupied by the cofactor
Irreversible Inhibitors
- Bind irreversibly to the active site, forming a covalent bond
- Block the substrate from the active site
- Increasing substrate concentration does not reverse inhibition
- Likely to be similar in structure to the substrate
Transition-state Analogues
- Designed to mimic the transition state of an enzyme-catalyzed reaction
- Bind more strongly than drugs mimicking the substrate or product
- High energy, transient species that cannot be isolated or synthesized
- Drug design is based on reaction intermediates closer to transition states than substrates or products
- Examples: renin inhibitors, statins, ACE inhibitors, protease inhibitors
Renin Inhibitors
- Renin is a protease enzyme responsible for hydrolyzing a specific peptide bond in angiotensinogen to form angiotensin I
- Angiotensin I is converted to angiotensin II, which raises blood pressure
- Renin inhibitors should act as antihypertensives by preventing the first stage of this process
- Examples: aliskiren, which contains a hydroxyethylene transition-state mimic
Suicide Substrates
- Agents converted to irreversible inhibitors by the enzyme-catalyzed reaction
- React with the target enzyme once formed
- Example: trifluoroalanine as a suicide substrate of alanine transaminase
- Inhibition mechanism: irreversible alkylation of the enzyme
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