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UGT aka
UDP-Glucuronosyltransferase
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UGT transfers ___________ to substrate
β-D-glucuronide
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What is UDPGA and what isoforms utilize it?
- Uridine-5-diphosphate-a-D-glucuronic acid
- UGT1, UGT2A and UGT2B
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What are UGT GI forms? What are they important for?
- UGT1A7, 1A8, 1A10
- 1st pass metabolism and affects bioavailability
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___________ is the major enzyme for codeine glucuronidation
UGT2B7
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What disease is associated with mutation of UGT1A1 gene?
Crigler-Najjar syndrome
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Mutation in UGT1A1 gene will cause what biological effect(ie.HTN is a biological effect)?
Hyperbilirubinemia
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UGT1A1 mutation causes __________ which produces ___________ in the serum.
- Crigler-Najjar syndrome
- High bilirubin
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Mutation in UGT1A1 (increase/decrease) in glucuronidation acivity that leads to ____ and ___?
- decrease
- congenital nonhemolytic jaundice
- unconjugated hyperbilirubinemia
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UGT1A1*28 allege mutation is associated with what disease?
Glibert Syndrome
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Glibert syndrome causes __________ in blood serum due to mutation in _________ allele.
- increase in unconjugated bilirubin
- UGT1A1*28
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Glibert syndrom is a mutation in what region of the gene?
TATA box
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Treating UGT1A1*28 mutation with _______ drug leads to severe delayed diarrhea and _________.
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House cats have lots their ability to glucuronidate certain agents due to what characteristic?
Hypercarnivore
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Due to hypercarnivorous characteristic of house cats, they have lost _______ enzyme.
UGT1A6
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Loss of _________, cats can not glucuronidate ___&___ due to its increase in toxicity and slow clearance.
- UGT1A6
- APAP & acetysalicylic acid
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During fetal development, __________ is the enzyme that is responsible for biotransformation of retinol?
Sulfotransferases
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Sulfotransferases are responsible for biotransfering what anticoagulant drug?
heparin
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________ SULTs are located in the Golgi.
Membrane bound
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________ SULTs are mainly responsible for biotransfering sulfonate xenobiotics, bile acids.
Cytosolic
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What subfamily of GST is responsible for metabolism of inflammatory agents such as protaglandins.
Microsomal
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Which isoform of GST causes a null mutation that leads to colon cancer.
Null mutation (GSTM1*0)
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Which null mutation of GST subfamily leads to increase in chemotherapy side effects
GSTT1*0
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Increase in incidence of asthma is associated with what polymorphism?
Null GST polymorphism
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Overexpression ___________ leads to increase in resistance to nitrogen mustards binding to DNA.
GST
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______&______ isoforms of are known as fast acetylators which is responsible for ________ drug used for tuberculosis.
- NAT2*12 and NAT2*13
- Isoniazid
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Slow acetylators can do lead to what when hydralazine is given?
tachycardia or hypotension
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Poor metabolism of what drug by NAT lead to severe cadiogenic effects?
Hydralazine
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Inactivation of neurotransmittors is associated with what enzyme?
COMT
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Polymorphisms in the enzyme resposible for metabolizing neurotransmittor can lead to what disease. (Name one)
- Schizophrenia
- Parkinson's
- alcoholism
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What enzyme metabolizes antineoplastic and immunosupressive agents?
Thiopurine S-methyltransfersase
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activation of _______ drug by ___________ into 6-MP.
- Azathiprine
- Glutathione S-transferase
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6-MP is metabolized by ___________.
Thiopurine S-methyltransferase
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Polymorphisms in TPMT leads to what severe pathophysiologic effect, due to increased concentration of drug that are metabolized by TPMT.(Name one)
- Hepatotoxicity
- life-threatening myelosuppression
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