ライフサイエンスコーパス: glucuronidation

1 n of unconjugated bilirubin from the body by glucuronidation.

2 line capillary electrophoresis monitoring of glucuronidation.

3 egulatory and functional properties of human glucuronidation.

4 al bioavailability and rapid clearance via O-glucuronidation.

5 mes and screened for effective inhibitors of glucuronidation.

6 metabolites) undergoes clearance by Phase II glucuronidation.

7 enzyme is a major UGT involved in estradiol glucuronidation.

8 nsformation of oxidized products of atRA via glucuronidation.

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

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

11 contribute to the diversity of extrahepatic glucuronidation.

12 I metabolites, particularly those undergoing glucuronidation.

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

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

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

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

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

18 sing those involved in androgen-inactivating glucuronidation.

19 ate exhibited rapid clearance due to hepatic glucuronidation.

20 d bioisosterically by an indazole to inhibit glucuronidation.

21 , SN22, resisting ABCG2-mediated export, and glucuronidation.

22 GluN2B affinity and activity but inhibiting glucuronidation.

23 t further sulfation and, to a lesser extent, glucuronidation.

24 yunsaturated fatty acids increased substrate glucuronidation.

25 y in a mouse model of VL but was hampered by glucuronidation.

26 ely, these inducible modifications go beyond glucuronidation.

27 ucuronosyltransferase 1A1 (UGT1A1)-catalyzed glucuronidation.

28 target PXR as a positive regulator of human glucuronidation.

29 which inactivate and solubilize androgens by glucuronidation.

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

31 PKC agonists verified a central PKC role in glucuronidation.

32 e pharmacokinetic properties by reduction of glucuronidation.

33 infolding by hydrogen bonding seems to favor glucuronidation.

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

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

36 Glucuronidation, a common phase II biotransformation rea

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

38 Glucuronidation activities of 14 substrates were measure

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

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

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

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

43 3Ala/277Tyr) variant exhibited no detectable glucuronidation activity against the trans isomers of ei

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

45 Conserved glucuronidation activity attributed to the Ugt1 locus ca

46 Differences of glucuronidation activity between human liver and colon s

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

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

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

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

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

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

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

54 , respectively, and significant decreases in glucuronidation activity were observed for both substrat

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

56 phine, 4-methylumbelliferone, and zidovudine glucuronidation activity, but morphine glucosidation was

57 8p.Cys277Tyr variant exhibited no detectable glucuronidation activity; a similar lack of detectable g

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

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

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

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

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

63 any oral phenolics is mediated by intestinal glucuronidation and hepatic recycling.

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

65 Glucuronidation and oxidation studies of selected fluori

66 ps could sterically shield the OH group from glucuronidation and permeability challenges.

67 te identification by determining the site of glucuronidation and phase I oxidation in selected drug m

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

69 s successfully applied to obtain the dietary glucuronidation and sulfation profile of 116 compounds.

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

71 Glucuronidation and transporter-mediated efflux into bil

72 Other compounds underwent glucuronidation and were not hypercholeretic.

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

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

75 showed enrichment for biological oxidation, glucuronidation, and fatty acid metabolism pathways.

76 associated with inflammation, angiogenesis, glucuronidation, and homeodomain pathways.

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

78 major phase II modifications, sulfation and glucuronidation, and the corresponding unconjugated agly

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

80 ansferase 2B10 as the catalyst of nicotine N-glucuronidation, are discussed.

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

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

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

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

85 metabolites involved in glycogen synthesis, glucuronidation, bile acid conjugation, and antioxidant

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

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

88 , as is the molecular basis for preferential glucuronidation by UGT1 and UGT2 family enzymes.

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

90 hydroxy, amino, and carboxylic acid groups, glucuronidation can occur at any of those.

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

92 Glucuronidation capacity in humans is not a factor excep

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

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

95 biosynthetic enzymes of the glutathione and glucuronidation conjugation pathways.

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

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

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

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

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

101 sorbed and underwent an extensive first-pass glucuronidation either in the gut (44%) or in the liver

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

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

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

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

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

107 lly accessible approaches to inhibiting drug glucuronidation: (i) blocking an initial HDAC1-mediated

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

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

110 ts a metabolic "soft spot" for oxidation and glucuronidation in primary and secondary alcohols.

111 but these compounds suffered from extensive glucuronidation in primates.

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

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

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

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

116 es cause drug toxicity by reversing Phase II glucuronidation in the gastrointestinal tract.

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

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

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

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

121 Since glucuronidation is a common pathway of drug metabolism,

122 Glucuronidation is a detoxification process to eliminate

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

124 Glucuronidation is an enzymatic process that terminally

125 beta-Glucuronidation is an important metabolic pathway for a

126 Glucuronidation is an important pathway in the metabolis

127 Glucuronidation is in general considered as a terminal m

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

129 alyzed morphine glycosidation indicated that glucuronidation is the principal route of metabolism bec

130 However, rapid and efficient glucuronidation is thought to limit its utility for syst

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

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

133 tive allosteric modulators is prone to rapid glucuronidation, its bioisosteric replacement by an inda

134 Glucuronidation may represent a mechanism of intrinsic d

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

136 oach to measure free and total SN-38 and its glucuronidation metabolite (SN-38G) using stable isotope

137 enation and hydroxylation) and II reactions (glucuronidation, methylation and sulfation).

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

139 idinyldiphosphate activated glucuronic acid, glucuronidation of 10 and 11 was not observed.

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

141 syltransferase inhibitor, nilotinib, reduced glucuronidation of 2-OHCHR by 52.4 +/- 2.55% and of 6-OH

142 1 and 2B164342B13531 proteins, catalyzed the glucuronidation of 4-hydroxyestrone, indicating that the

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

144 Although glucuronidation of ABP and its metabolites is a detoxifi

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

146 (salen)chromium complexes catalyze the beta-glucuronidation of alcohols, phenols, and anilines via s

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

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

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

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

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

152 itonavir and fosamprenavir-ritonavir induced glucuronidation of buprenorphine.

153 ol is mild and pH-neutral, enabling the beta-glucuronidation of complex pharmaceuticals and natural p

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

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

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

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

158 Glucuronidation of p-nitrophenol in intact microsomes wa

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

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

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

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

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

164 reased UDPGT and increased the intracellular glucuronidation of testosterone.

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

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

167 Glucuronidation of these retinoids by human liver micros

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

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

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

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

172 in turn directed elevated glucose uptake and glucuronidation; our data also implicate the pentose pho

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

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

175 istance to trametinib; conversely, elevating glucuronidation pathway activity was sufficient to direc

176 etic inhibition of different steps along the glucuronidation pathway strongly reversed RAP resistance

177 dels to identify multiple metabolites in the glucuronidation pathway-a toxin clearance pathway that i

178 otransformation genes, especially within the glucuronidation pathway.

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

180 17 gene deletion variant (UGT2B17*2) on SAHA glucuronidation phenotype, human liver microsomes (HLM)

181 evealed associations with lipid homeostasis, glucuronidation, phospholipid metabolism, and gastrointe

182 This suggests that glucuronidation plays a significant role in detoxifying

183 ork demonstrates the important roles that AG glucuronidation plays in Arabidopsis sexual reproduction

184 e and the lack of species variability in the glucuronidation potential resulted in a greater confiden

185 icities were evaluated with regard to tissue glucuronidation potential.

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

187 I hydrolysis and hydroxylation and Phase II glucuronidation products, were identified in C57BL/6J ma

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

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

190 ed the interdependence of SER access and the glucuronidation rate of ezetimibe.

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

192 7 gene deletion significantly reduce overall glucuronidation rates of nicotine and its major metaboli

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

194 hydroxyurea which correlated to low in vitro glucuronidation rates.

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

196 Concurrent glucuronidation reaction mixtures containing equal amoun

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

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

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

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

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

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

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

204 atography-high-resolution mass spectrometry: glucuronidation, sulfation, dealkylation, and oxidation.

205 on the various components of the microsomal glucuronidation system.

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

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

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

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

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

211 ch in metabolism of our lead structures from glucuronidation to oxidation.

212 The contribution of glucuronidation toward human drug metabolism is carried

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

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

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

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

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

218 Therefore, a chemical triterpene 3-O-glucuronidation was conducted in this study to alleviate

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

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

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

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

223 The extent of acyl glucuronidation was reduced through structural optimizat

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

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

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

227 2A3.1 and UGT2A3.2 for hyodeoxycholic acid 6-glucuronidation were 69 +/- 7 and 44 +/- 12 microM, resp

228 al recessive inherited disorder of bilirubin glucuronidation which has not been investigated in Egypt

229 ) 2B10 and 2B17 play major roles in nicotine glucuronidation with polymorphisms in both enzymes shown

230 the hypothesis that attenuating the rate of glucuronidation would improve exposure and reduce variab

231 tically measured to study their influence on glucuronidation yield.

232 tween reactive donors/acceptors and improved glucuronidation yields.