Phase 2 metabolism

?
Promotes excretion and results in loose of biological activity (except morphine) and some conjugates can lead to immune responses:
UDP-GTs
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UDP-GTs are monomeric with a MW of?
50-60,000
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UGT1:
10 isoforms, products of the same gene
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UGT2:
isoforms are products of separate genes
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If a UDP-GT conjugate has a MW of .>400 where will it be excreted to?
Bile
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If a UDP-GT conjugate has a MW of .
Urine
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Enterohepatic recirculation can .......... half life of a drug?
increase
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UDP-GT-1 can be induced by:
phenobarbitone &PAH
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SULTs are found in the:
cytosol
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SULT found at highest levels in the liver:
SULT1A1
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SULT found at highest levels in the intestine:
SULT1A3
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glucuronidation of:
paracetamol, salicylic acid, disulphiram
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sulfation of:
isoprenaline, desipramine, paracetamol
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methylation of:
l-dopa, histamine, arsenic
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acetylation of:
sulfamethoxazole, sulfanilamide, isoniazid
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Sulfation use what as a source of sulphate:
PAPS
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What requires salvation for activity?
minoxidil
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The general product of sulfation:
ionised, polar, water soluble
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SULTs can be the AhR which are activated by?
dioxins
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methylation results in:
increased liphophilicity
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The co-factor used by methyltransferase enzymes?
SAM
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o-methylation of:
l-dopa
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n-methylation of:
histamine, nicotine
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n-methylation of:
mercaptopurine
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Arsenic is metabolised by?
methyltransferases
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NAT1 + NAT2 are located where in the cell?
cytosol
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acetyltransferases used what to donate an acetyl group?
acetyl coenzyme A
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Inactivation of isoniazid by NAT2 is related to?
slow acetylator
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The association with NAT2 and bladder cancer is due to inactivation of?
arylamine dyes
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NAT1 is found in most tissues but NAT2 is found mainly in the?
liver & intestine
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NATS are:
not inducible
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What percentage of the population is unable to acetylate?
50%
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Which statement is true?
NAT1-Monomorphic. NAT2-Polymorphic
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NAT drug substrates require a:
amino-group
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NAT1 substrate:
sulfamethoazole, sulfanilamide
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NAT2 substrate:
isoniazid
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The result of acetylation is?
decreased solubility
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amino-acid conjugation requires a:
carboxylic acid
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amino-acid conjugation is found where in the cell?
mitochondria
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2 examples which undergo amino-acid conjugation:
benzoic acid, salicylic acid
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2 enzymes involved in amino-acid conjugation are?
MACS and Acyl-CoA:glycine N-acetyltranserase
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Why are so few xenobiotics conjugated?
Acyl-CoA:glycine N-acetyltranserase is selective
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Glutathione is a:
tripeptide
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GSTs are found in the majority of tissue and are found at what concentration in human liver?
10mM
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GSTs consist of homo or hetrodimers of submits of:
25,000
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GSTs conjugate the reduced glutathione (GSH) to?
electrophillic compounds
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GSH reacts through:
neuclophillic cysteine thiol group
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GST subfamilies include?
Alpha, Mu, Pi, Theta
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Which subfamily prefers small molecules as substrates?
Theta
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Substrate for GST-Theta?
dichloromethane
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Genetic polymophisims of GSTs are found in which subfamilies?
GSTM1 & GSTT1
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GST enzymes can be induced by?
PAHs, barbiturates, antioxidants
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What group from the GSH takes part in the reaction?
suphydryl
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Which drug is not a substrate for glutathione conjugation?
disulphiram
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Other cards in this set

Card 2

Front

UDP-GTs are monomeric with a MW of?

Back

50-60,000

Card 3

Front

UGT1:

Back

Preview of the front of card 3

Card 4

Front

UGT2:

Back

Preview of the front of card 4

Card 5

Front

If a UDP-GT conjugate has a MW of .>400 where will it be excreted to?

Back

Preview of the front of card 5
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