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Drug Biotransformation
Acetylation
10
Pharmacology
Graduate
11/08/2010

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Cards

Term
What types of substrates to NAT's work with?
Definition
xenobiotic amines, hydrazines

hydroxy gps of N-hydroxylated compounds

endogenous amines and hydroxyls

(Special case- amino gp of cysteine conjugates in cysteine conjugate NAT in Mercapturic Acid pathway)
Term
What is the cosubstrate of NAT? which group is acetylated?
Definition
Acetyl CoEnzyme A
thiol group of coenzyme A is acetylated
Term
MW of NAT?
Definition
33,500
Term
What are the two most important NATs in the acetylation of xenobiotics?
Definition
NAT1 and NAT2
Term
Where is NAT2 mostly found?
Definition
Liver
some expression in extrahepatic tissues
Term
Where is NAT1 mostly found?
Definition
Blood, intestine, and bladdar
(Low expression in liver)
Term
Expression levels of ______ do not seem to be changed by inducing agents.
Definition
NATs
Term
What do all NATs have in common that allows them to attack Acetyl Coenzmyme A?
Definition
Conserved cysteine residue at the 68 position... this is called the ping-pong bi-bi mechanism where enzyme acetylates itself and then the drug enters and gets acetylated
Term
What is the name of the mechanism for acetylation?
Definition
Ping-Pong Bi-Bi mechanism
Term
What was the first enzyme shown to exhibit polyorphism?
Definition
NAT2
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