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competition for the enzyme is dependent on the concentration of the substrate and the inhibitor
competition for the enzyme is not dependent on the concentration of the enzyme
What CYP isoforms are responsible for the bioactivation of most carcinogens?
CYP1A1/2, CYP1B1, CYP2E1 and CYP3A
Is CYP1A1 or CYP1A2 constitutively expressed in the liver? Where is the other one expressed?
CYP1A1 is expressed in the lung, intestine and skin
Describe the mechanism through which induction of CYP1A1 occurs.
depression of the repressor protein that suppresses CYP1A1 activity and activation of CYP1A1 gene transcription
What is responsible for both constitutive and inducible expression of CYP1B1?
aryl hydrocarbon receptor
What are the four results of a genetic polymorphism in the CYP2D6 enzyme?
ultrarapid metaboliser, extensive metaboliser, intermediate metaboliser and poor metaboliser
What can CYP2E1 alone cause the formation of? Why? Example
ROS causing oxidative stress
CYP2E1 is an easily coupled enzyme
Ethanol causes oxidative stress through CYP2E1 induction
What does overexpression of CYP2E1 in hepatic cells increase?
intracellular hydrogenperoxide (40-50%)
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