Final Exam (Lecture 22 - 26) Flashcards
Which of the following statements is incorrect?
A. Glucuronidation makes molecules more lipid soluble
B. The same molecule can have multiple sites of glucuronidation by UGT
C. UGT is superfamily, family is arabic numeral, subfamily is capital letter
D. UGT’s are only present in mammals
E. A & D
(A) Glucuronidation makes molecules more WATER soluble
*C - Ex. UGT1A
UGT = superfamily 1 = family A = subfamily
True or False UGT’s are members of a larger uridine diphosphoglycosyltransferase superfamily?
True - this superfamily exists in plants, animals, and bacteria
Which of the following statements about UGT is incorrect?
A. half of protein is coded by a unique first exon
B. second part of protein is identical but coded by a set of 4 exons downstream from exon 1
C. UGT is a membrane bound protein
D. Conserved C-terminal domain of UGT defines substrate specificity
E. Liver and GI tract are major sites of UGT expression
(D) The VARIABLE N-TERMINAL definse substrate specificity, not the C-terminal
*E - liver and GI tract are main sites of drug metabolism
Which of the following statements about UGT is correct?
A. Bilirubin is solely glucuronidated by UGT1A1
B. Crigler-Najjar Syndrome 1 & 2 are not associated with disorders of bilirubin glucuronidation
C. Irinotecan toxicity may be seen in UGT1A1*28 homozygotes
D. A & C
E. All of the above
(D) A & C are correct
*B - Crigler-Najjar Syndrome 1 & 2 ARE associated with disorders of bilirubin
Which of the following syndromes are associated with disorders of bilirubin glucuronidation?
A. Crigler-Najjar Syndrome type 1 B. Crigler-Najjar Syndrome type 2 C. Gilbert's syndrome D. A & B E. All of the above
(E) all of the above
Cytosolic sulfotransferases result in which of the following?
A. increased water solubility
B. decreased passive penetration of cell membranes
C. decreased urinary and biliary excretion
D. Only A & B
E. None of the above
(D) only A & B are correct
*C - cytosolic sulfotransferases result in INCREASED urinary and biliary excretion
Which of the following statements is incorrect?
A. Sulfonate group is ionized at physiologic pH
B. SULT1A1 catalyzes sulfating of small neutral phenols
C.
D.
E.
NEEDS MORE INFO
True or False - almost all sulfated xenobiotics and endobiotics are biologically active?
False - they are biologically INACTIVE!
How many SULT genes have been identified in humans? How many SULT families?
13 SULT genes
4 SULT families (SULT1, 2, 4, 6)
Which SULT family is correctly matched to its biological role?
A. SULT1 - simple phenols like estradiol, thyroid hormones, xenobiotics, drugs
B. SULT2 - hydroxy groups of steroids
C. SULT4 - no known substrate or function
D. SULT6 - testis specific
E. All are matched correctly
(E) all matched correctly
This term is defined as various forms of an enzyme that are coded by different alleles at the same locus?
allozymes
This term is defined as enzymes that perform the same function, but which are coded by genes located at different loci?
isozymes
What is the major xenobiotic SULT in the human liver?
SULT1A1 isoform
All of the following are substrates of SULT1A1, except?
A. Minoxidil B. APAP C. Ethinyl estradiol D. Metabolites of Tamoxifen E. Amiodarone
(E) Amiodarone is not a SULT1A1 substrate
Which SULT1A1 allele is responsible for thermostability differences observed in platelet SULT1A1 activity?
*2