Irreversible enzyme inhibitors are compounds that permanently deactivate enzymes by forming stable bonds, typically covalent, at the active site. Unlike reversible inhibitors, they do not dissociate, leading to a lasting loss of enzymatic activity. These inhibitors are crucial in regulating metabolic pathways, serving as pharmaceuticals, and are used in agriculture and sanitation. The text explores their potency, measurement, and examples like DFP and DFMO in medical treatments.
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1
Nature of bond in irreversible enzyme inhibitors
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2
Common reactive groups in irreversible inhibitors
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3
Amino acid residues targeted by irreversible inhibitors
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4
Irreversible inhibitors modify the ______ of an enzyme, while preserving its overall ______.
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5
Irreversible inactivation can be caused by extreme ______, high ______, or certain ______, which may lead to protein denaturation.
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6
Processes like protein aggregation or dissociation into ______ are often non-specific and can affect many ______, not just enzymes.
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7
Difference between IC50 and kobs/[I] in inhibitor potency measurement.
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8
Significance of kobs reaching kinact.
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9
Condition for kobs/[I] as a valid potency measure.
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10
Initially, the enzyme and inhibitor may form a ______ complex, which later becomes a covalently bonded, inactive complex (EI*).
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11
The ______ of enzyme inactivation (kinact) is calculated by fitting the loss of activity over time to a specific ______ equation.
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rate rate
12
______, such as MALDI-TOF, can be used to detect the enzyme's mass increase due to inhibitor binding, shedding light on the ______ of their interaction.
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13
Characteristic of slow-binding inhibitors initial interaction
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14
Conformational change in enzyme due to slow-binding inhibitors
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15
Examples of slow-binding inhibitors
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16
______, used to combat African sleeping sickness, becomes active by the enzyme it targets and subsequently renders it inactive.
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17
Quinacrine mustard demonstrates a ______ inhibition of trypanothione reductase, with one molecule binding in a reversible manner and another covalently.
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18
Natural role of enzyme inhibitors
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19
Synthetic enzyme inhibitors usage
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20
Enzyme inhibition in metabolic regulation
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