ライフサイエンスコーパス: glucuronidation

1 I metabolites, particularly those undergoing glucuronidation.

2 al bioavailability and rapid clearance via O-glucuronidation.

3 yunsaturated fatty acids increased substrate glucuronidation.

4 mes and screened for effective inhibitors of glucuronidation.

5 metabolites) undergoes clearance by Phase II glucuronidation.

6 enzyme is a major UGT involved in estradiol glucuronidation.

7 nsformation of oxidized products of atRA via glucuronidation.

8 UGT1A1 is the isoform responsible for SN-38 glucuronidation.

9 indicating the role of UGT1 isoform in SN-38 glucuronidation.

10 contribute to the diversity of extrahepatic glucuronidation.

11 , the extent of which is determined by SN-38 glucuronidation.

12 he specific isoform of UGT involved in SN-38 glucuronidation.

13 cy of acetaminophen (AAP) to phenotype SN-38 glucuronidation.

14 tion to DCF modified by 4' hydroxylation and glucuronidation.

15 AAP was a poor predictor of SN-38 glucuronidation.

16 ely, these inducible modifications go beyond glucuronidation.

17 ucuronosyltransferase 1A1 (UGT1A1)-catalyzed glucuronidation.

18 target PXR as a positive regulator of human glucuronidation.

19 which inactivate and solubilize androgens by glucuronidation.

20 mor cell growth, HA production, and androgen glucuronidation.

21 PKC agonists verified a central PKC role in glucuronidation.

22 infolding by hydrogen bonding seems to favor glucuronidation.

23 line capillary electrophoresis monitoring of glucuronidation.

24 egulatory and functional properties of human glucuronidation.

25 ver microsomes were the most active in 4-ABP glucuronidation (344.1 pmol/min/mg) followed by rats (30

26 UGTs eliminate by glucuronidation a broad variety of endobiotic and xenobi

27 is the sole enzyme responsible for bilirubin glucuronidation, a rate-limiting step necessary for bili

28 Glucuronidation activities of 14 substrates were measure

29 one and beta-naphthoflavone, cellular UGT1A1 glucuronidation activities were increased.

30 overexpressing HEK293 cells exhibited high N-glucuronidation activity against both nicotine and cotin

31 man liver microsomes (HLM) were analyzed for glucuronidation activity against SAHA and compared with

32 ant exhibited a 3-fold (P<0.005) decrease in glucuronidation activity against SAHA compared with wild

33 3Ala/277Tyr) variant exhibited no detectable glucuronidation activity against the trans isomers of ei

34 T2B17*2 exhibited a 45% (P<0.01) decrease in glucuronidation activity and a 75% (P<0.002) increase in

35 Conserved glucuronidation activity attributed to the Ugt1 locus ca

36 Differences of glucuronidation activity between human liver and colon s

37 ed in Ugt1(-/-) mice, because UGT2-dependent glucuronidation activity is unaffected.

38 sensitive method for determination of the N-glucuronidation activity of mouse, rat, and human liver

39 e developed method was used to determine the glucuronidation activity of mouse, rat, and human liver

40 es alternate isoforms UGT1A_i2s that control glucuronidation activity through protein-protein interac

41 samples directly correlated with functional glucuronidation activity toward androgens and the antica

42 In addition, the selective induction of glucuronidation activity toward lamotrigine, ethinyl est

43 ation activity; a similar lack of detectable glucuronidation activity was observed for the UGT1A10p.G

44 ssociated with reduced nicotine and cotinine glucuronidation activity, but intriguingly is not associ

45 8p.Cys277Tyr variant exhibited no detectable glucuronidation activity; a similar lack of detectable g

46 an liver microsomal specimens, the rate of O-glucuronidation against trans-4-OH-TAM and trans-endoxif

47 cular shape is less important in the hepatic glucuronidation and biliary excretion of bilirubin and o

48 The enzyme is essential for glucuronidation and biliary excretion of bilirubin, and

49 These inhibitors are impervious to glucuronidation and demonstrate allosteric inhibition.

50 rphisms may be associated with altered rates glucuronidation and detoxification of NNAL in vivo.

51 ridine 5'-diphosphoglucuronic acid-dependent glucuronidation and NADPH-dependent oxidation of estradi

52 Glucuronidation and oxidation studies of selected fluori

53 In contrast, ATP-dependent glucuronidation and sulfation of acetaminophen, deemed "

54 hepatic enzyme involved in nicotine/cotinine glucuronidation and that the UGT2B10*2 variant significa

55 Glucuronidation and transporter-mediated efflux into bil

56 Other compounds underwent glucuronidation and were not hypercholeretic.

57 oordinate induction of proteins for storage, glucuronidation, and canalicular transport of bilirubin.

58 apidly metabolized in the sole by oxidation, glucuronidation, and ethoxylate chain shortening.

59 carried out in the endoplasmic reticulum by glucuronidation, and most likely plays an important role

60 e excreted directly in bile or require prior glucuronidation are poorly understood.

61 liver microsomes established enantiospecific glucuronidation as a likely mechanism for the observed d

62 mutants nearly or completely inactivated all glucuronidation at both pH levels.

63 atio of 2-3-fold more activity for bilirubin glucuronidation at pH 6.4 versus 7.6 was established, an

64 ines the role and diversity of physiological glucuronidation at the distal end of the digestive tract

65 ) for the competitive inhibition of morphine glucuronidation by codeine, IC50 (on-line) = 170 vs 580

66 that bilirubin is metabolized solely through glucuronidation by UDP-glucuronosyltransferase (UGT) 1A1

67 AalphaC and HONH-AalphaC underwent glucuronidation by UGTs to form, respectively, N(2)-(bet

68 PXR is a key regulator of pregnancy induced glucuronidation capacity in addition to modulating the s

69 Glucuronidation capacity in humans is not a factor excep

70 In human prostate cancer cells, androgen glucuronidation, catalyzed by the two UDP-glucuronosyltr

71 etely or partially abolish hepatic bilirubin glucuronidation, causing Crigler-Najjar syndrome type 1

72 biosynthetic enzymes of the glutathione and glucuronidation conjugation pathways.

73 ydroxytestosterone generation and irinotecan glucuronidation correlated with the pattern of genetic v

74 Low levels of glucuronidation could also be detected in the resistant

75 tive to that of liver, suggesting that renal glucuronidation could be a significant factor in renal e

76 This has been attributed to its unique glucuronidation detoxification pathway.

77 ntroversy exists regarding the regulation of glucuronidation during the process of hepatic regenerati

78 Enantioselective glucuronidation favoring (-)-1a was also found in human

79 gnificantly reduces nicotine- and cotinine-N-glucuronidation formation and plays an important role in

80 nscription and transcriptional activation of glucuronidation genes responsible for conjugation and de

81 omethyl ether (AME)) while hydroxylation and glucuronidation had the opposite effect (as seen for 4-h

82 re enriched for enzymes of detoxification by glucuronidation, had a different pattern with multiple m

83 sses an additional clearance pathway through glucuronidation in addition to that via CYP3A4 oxidation

84 ferases (UGTs) and now report on the role of glucuronidation in de novo resistance to two topoisomera

85 but these compounds suffered from extensive glucuronidation in primates.

86 UGT2B15 and UGT2B17 expression and androgen glucuronidation in prostate cancer cell lines.

87 ockout mouse models and examined the role of glucuronidation in protecting against irinotecan-induced

88 of UGT aglycones were capable of modulating glucuronidation in the biopies with octylgallate being 1

89 e high background uptake in the liver due to glucuronidation in the case of (18)F-FLT may limit utili

90 n the interplay between direct excretion and glucuronidation in the liver, we studied a series of nov

91 inhibition activity but also were subject to glucuronidation in vitro providing the potential for mul

92 zofurin, and MAD analogues were resistant to glucuronidation in vitro.

93 We conclude that microsomal glucuronidation, in contrast to other well characterized

94 Since glucuronidation is a common pathway of drug metabolism,

95 n to form the N-hydroxylamine followed by N2-glucuronidation is a general pathway of MeIQx metabolism

96 Glucuronidation is an enzymatic process that terminally

97 Glucuronidation is an important pathway in the metabolis

98 Glucuronidation is in general considered as a terminal m

99 l therapies or to regulate phase 2-dependent glucuronidation is questionable given the lack of in viv

100 uptake, due predominantly to N-oxidation and glucuronidation, is dependent on the NADPH redox state.

101 form of multidrug resistance, inducible drug glucuronidation, is discussed.

102 Glucuronidation may represent a mechanism of intrinsic d

103 e molecule for simultaneous improvement of N-glucuronidation metabolic liability and off-target pharm

104 extent of conversion and relative extent of glucuronidation of 0.05 (range, 0.01 to 0.25) and 2.24 (

105 ly UGT1A10 in cells supported 10-fold higher glucuronidation of 17beta-estradiol than UGT1A1.

106 1 and 2B164342B13531 proteins, catalyzed the glucuronidation of 4-hydroxyestrone, indicating that the

107 elis-Menten parameters (Km and Vmax) for the glucuronidation of 4-methyl-7-hydroxy coumarin and 4-nit

108 Although glucuronidation of ABP and its metabolites is a detoxifi

109 hisms in the UGT enzymes responsible for the glucuronidation of active TAM metabolites play an import

110 GTs) was characterized and compared with the glucuronidation of atRA.

111 glucuronosyltransferase UGT1A7 catalyzes the glucuronidation of benzo(a)pyrene metabolites and other

112 UDP-glucuronosyltransferase (UGT)-mediated glucuronidation of benzo(a)pyrene-trans-7,8-dihydrodiol

113 iver after administration of Ad-hBUGT1, with glucuronidation of biliary bilirubin of above 95%.

114 Ts may play an important role in the overall glucuronidation of BPD in humans, with UGT1A1, UGT1A7, U

115 itonavir and fosamprenavir-ritonavir induced glucuronidation of buprenorphine.

116 mice for 3 weeks increased liver microsomal glucuronidation of estradiol, estrone, 4-aminophenol, an

117 gens found in tobacco and tobacco smoke, and glucuronidation of its major metabolite, 4-(methylnitros

118 Ts 2B10 and 2B17 play important roles in the glucuronidation of nicotine, cotinine, and 3HC and sugge

119 o a superfamily of enzymes that catalyse the glucuronidation of numerous endobiotics and xenobiotics.

120 Glucuronidation of p-nitrophenol in intact microsomes wa

121 alone is sufficient to drive UGT1A-dependent glucuronidation of ribavirin and Ara-C, and thus drug re

122 UGT2B10 is a major enzyme involved in the N-glucuronidation of several tobacco-specific nitrosamines

123 Identification of the UGT responsible for glucuronidation of SN-38 and the anthraquinone NU/ICRF 5

124 In vitro glucuronidation of SN-38 was screened in hepatic microso

125 at this method can be used to screen for the glucuronidation of test compounds and should reduce the

126 reased UDPGT and increased the intracellular glucuronidation of testosterone.

127 onosyltransferase 1A1 (UGT1A1) catalyzes the glucuronidation of the active metabolite SN-38.

128 ally UGT1A8 playing an important role in the glucuronidation of the procarcinogenic (-)-BPD enantiome

129 Glucuronidation of these retinoids by human liver micros

130 d 4-nitrophenol between on-line and off-line glucuronidation of these two compounds.

131 (UGT1A7) is a major UGT contributing to the glucuronidation of xenobiotic phenols in rats.

132 two hydrolytic, two N-dealkylation, three N-glucuronidation, one N-methylation, and several aromatic

133 pathways through cytochrome p450 pathways or glucuronidation, or related to co-morbidities.

134 also significantly related to lower cotinine glucuronidation (P's < 0.00156).

135 chromosome 4q was related to lower cotinine glucuronidation (P's < 2.7 x 10(-7), smallest P = 1.5 x

136 f the epithelial-mesenchymal transition, and glucuronidation pathways.

137 17 gene deletion variant (UGT2B17*2) on SAHA glucuronidation phenotype, human liver microsomes (HLM)

138 This suggests that glucuronidation plays a significant role in detoxifying

139 icities were evaluated with regard to tissue glucuronidation potential.

140 Analysis of the glucuronidation products showed that the hydroxyl-linked

141 ationship between para-nitrophenol and SN-38 glucuronidation (r = 0.08; P = 0.703).

142 ion was observed between SN-38 and bilirubin glucuronidation (r = 0.89; P = 0.001), whereas there was

143 UGT2B17 gene transcription and testosterone glucuronidation rate, in addition to that attributable t

144 7 gene deletion significantly reduce overall glucuronidation rates of nicotine and its major metaboli

145 /HT29-MTX co-culture model, overall relative glucuronidation rates were much higher than in HepG2 cel

146 hydroxyurea which correlated to low in vitro glucuronidation rates.

147 ecific inhibitor PP2 down-regulated 4-OHE(1) glucuronidation reaching 60% maximum while simultaneousl

148 Concurrent glucuronidation reaction mixtures containing equal amoun

149 nd evaluate their function in regulating the glucuronidation reaction, we examined the effect of hist

150 T cosubstrate is a rate-limiting step of the glucuronidation reaction.

151 Microsomal uptake of the cosubstrate for all glucuronidation reactions, UDP-glucuronic acid (UDP-GlcU

152 ned to account for the variable and specific glucuronidation requirements.

153 Inhibition of glucuronidation resulted in up to a 5-fold enhancement i

154 Of 81 structurally diverse glucuronidation substrates tested, UGT2A3 expressed by a

155 f targeted cancer drugs that undergo hepatic glucuronidation, such as sorafenib.

156 on the various components of the microsomal glucuronidation system.

157 and breast cancer cells have a capacity for glucuronidation that could contribute to intrinsic drug

158 that results in failure of proper bilirubin glucuronidation, the once futuristic idea of treatment b

159 investigated the effect of ADTh on androgen glucuronidation to evaluate its potential clinical utili

160 HONH-AalphaC also underwent glucuronidation to form a novel O-linked glucuronide con

161 h is excreted by the kidney after undergoing glucuronidation to MPAG.

162 The contribution of glucuronidation toward human drug metabolism is carried

163 observed in the expression of transcripts in glucuronidation, tRNA synthetase, and immune surveillanc

164 cophore appears metabolically resistant to O-glucuronidation unlike other structurally related DAAO i

165 olites of TAM, 4-OH-TAM and endoxifen, is by glucuronidation via the UDP-glucuronosyltransferase (UGT

166 A major mode of SAHA metabolism is by glucuronidation via the UDP-glucuronosyltransferase (UGT

167 The predicted decrease in cotinine glucuronidation was 8.6% (P = 4.5 x 10(-6)) per a 20% in

168 In the hamster, glucuronidation was greater, and the unconjugated fracti

169 expressing WT UGT2B10 in vitro, little or no glucuronidation was observed for microsomes from cells o

170 Intact SN-38 glucuronidation was observed only in HK293 cells transfe

171 On-line glucuronidation was observed within 15 min without any s

172 The extent of acyl glucuronidation was reduced through structural optimizat

173 Furthermore, the rate of in vitro glucuronidation was shown to be stereoselective for cert

174 The pattern of glucuronidation was similar for both bilirubin and 17 al

175 Because these compounds are susceptible to glucuronidation, we examined UDP-glucurono-syltransferas

176 2A3.1 and UGT2A3.2 for hyodeoxycholic acid 6-glucuronidation were 69 +/- 7 and 44 +/- 12 microM, resp

177 ) 2B10 and 2B17 play major roles in nicotine glucuronidation with polymorphisms in both enzymes shown