Drug Metabolism in Drug Design and Development Basic Concepts and Practice
3.1.1 Location Within the Cell The active site of the UGTs face the lumen of the endoplasmic reticulum (Fig. 3.2), whereas the a ...
substrate kinetics, it appears that there may be multiple glucuronide transporters on the ER membrane to move the glucuronide pr ...
UGT1A1 binding pocket, the carboxyl groups appear to be accessible to glucuronidation. Monoglucuronides at the 8 or 12 position ...
.UGT1various forms catalyze conjugation of planar phenols, bulky phenols, amines, tertiary amines, and bilirubin. (Nine active ...
A highly conserved N-terminal region containing the UDPGA binding site is found in both gene families. For the UGT1 family, the ...
TABLE 3.1 UGT1A nomenclature:seehttp://som.flinders.edu.au/FUSA/ ClinPharm/UGT/. UGT1 gene Trivial names Endogenous substrates T ...
TABLE 3.2 UGT2B nomenclature:seehttp://som.flinders.edu.au/FUSA/ ClinPharm/UGT/. UGT1 gene Species Endogenous substrates Tissue ...
3.1.4.4 Glucocorticoid Activation A glucocorticoid response element was identified near the CAR/PXR binding site in human UGT1A1 ...
TABLE 3.3 Selective substrates for individual UGT1A isozymes.Isoenzyme Endogenous substrates Reported K m Drug or xenobiotic sub ...
Carboxyl group : clofibrate, ciprofibrate, etodolac,fenoprofen, ibuprofen,ketoprofen, naproxen(racemic > S), valproic acid an ...
TABLE 3.3 ( Continued ) Isoenzyme Endogenous substrates Reported Km Drug or xenobiotic substrates Inducers Inhibitors UGT1A6 Ser ...
Drugs: acetaminophen, beta blocking adrenergicagents (low activity) suchas atenolol, labetolol,metoprolol, pindolol,propranolol, ...
TABLE 3.3 ( Continued ) Isoenzyme Endogenous substrates Reported Km Drug or xenobiotic substrates Inducers Inhibitors 2-hydroxy, ...
3-ethylphenol,4-methylphenol,4-nitrophenol,4- tert -butylphenol (low), methylsalicylate,salicylate, mono(ethylhexyl)phthalate, B ...
TABLE 3.3 ( Continued ) Isoenzyme Endogenous substrates Reported Km Drug or xenobiotic substrates Inducers Inhibitors ibuprofen, ...
UGT1A11 UGT1A12 UGT1A8 and UGT1A9 were previously mislabeled. The old UGT1A8 is now UGT1A9 and vice versa.AhR ...
TABLE 3.4 Selective substrates for individual UGT2B isozymes.Isoenzyme Endogenoussubstrates Reported Km Drug or xenobiotic subst ...
Bile acids: hyodexycholic acid Estrogens: Estriol, estradiol (17 b-hydroxy), 4-hydroxy estrone (high) 2- hydroxy estrone,2- hydr ...
evidence of an ARE in rat UGT1A6 but were able to show that oltipraz, which normally activates AREs was acting through an XRE (A ...
Unfortunately, detergents may differentially affect the individual enzymes and there is often a sharp concentration optimum for ...
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