ライフサイエンスコーパス: UGT

1 UGT enzyme activity toward estrone was unchanged 1 day p

2 UGT enzyme activity was determined toward two prototypic

3 UGTs accelerate the metabolic elimination of bile acids,

4 UGTs catalyze the covalent addition of glucuronic acid s

5 UGTs compete with P450 enzymes, which bioactivate HAAs b

6 UGTs convert metabolites, dietary constituents, and envi

7 UGTs eliminate by glucuronidation a broad variety of end

8 UGTs, distributed primarily in liver, kidney, and gastro

9 In a subset of tumors (33%), UGT protein levels and activity exceeded that of paired

10 nzymes are required for plant life in that a UGT from Pisum sativum (PsUGT1) controls plant developme

11 constitutive or hydrogen peroxide-activated-UGTs demonstrated that reactive oxygen species-related o

12 ng chloroanilines in Arabidopsis, additional UGTs could compensate for the conjugation of TCP in the

13 nd K404 are strictly conserved in 70 aligned UGTs, except for S321, equivalent to K314, in UGT2B15 an

14 roducts in stomach UGT1A mRNA expression and UGT catalytic activities were investigated in a panel of

15 osyltransferase (UGT) protein expression and UGT messenger RNA (mRNA) levels were measured by Western

16 Microsomal UGT protein expression and UGT mRNA levels were unaltered after hepatectomy.

17 f BPD glucuronide diastereomer formation and UGT expression.

18 rces that support research on the kidney and UGT.

19 oligonucleotide probes for rat GST, ST, and UGT.

20 of hUGT1A1 with itself, but not with another UGT isoform, human UGT1A6, which differs only in the N-t

21 Anti-UGT-1168 antibody trapped 2B15-His-containing co-immunop

22 st K(M) (300 micromol/L) against SAHA of any UGT in vitro.

23 suggestive of a possible interaction between UGT genotype and hormones.

24 ithin the gene encoding the enzyme bilirubin UGT.

25 ile concomitantly inducing hepatic bilirubin UGT mRNA and protein expression.

26 trongly with both liver microsomal bilirubin UGT activity and liver UGT1A1 mRNA level (r(2) =.82 and.

27 Bilirubin-UGT activity in liver homogenates was 8%-12% of normal,

28 indwelling portal vein catheter in bilirubin-UGT-deficient jaundiced Gunn rats, mean serum bilirubin

29 Both UGTs also were active in vitro on select flavonoids.

30 m(s) that enable endoplasmic reticulum-bound UGT isozymes to convert innumerable structurally diverse

31 d with purifying endoplasmic reticulum-bound UGTs for structural studies, we carried out homology-bas

32 um distachyon, we show that the Bradi5g03300 UGT converts DON into D3G in planta.

33 tic UGT activities were mainly determined by UGT gene transcription levels.

34 nd HONH-AalphaC underwent glucuronidation by UGTs to form, respectively, N(2)-(beta-D-glucosidurony1)

35 owing how candidate drugs are metabolized by UGTs.

36 arding differential phosphate utilization by UGTs to function efficiently.

37 eem to significantly modulate ABP-catalyzing UGT in liver.

38 ) regulating phosphorylation of constitutive UGTs in LS180 cells and 10 different human UGT cDNA-tran

39 ls; there is no direct inhibition of control UGT using curcumin as substrate in the in vitro assay.

40 Similar studies found that different UGT isoforms or CYP3A4 immunoprecipitated along with the

41 ereospecific activity exhibited by different UGTs against BPD is consistent with tissue-specific patt

42 e uridine diphosphoglucuronosyltransferases (UGTs) belong to a superfamily of enzymes that catalyse t

43 In addition, we describe five Drosophila UGTs belonging to two families.

44 t provides ontology of the cell types during UGT development and the molecular hallmarks of those cel

45 This review examines in detail each UGT isozyme known to be associated with cancer and carci

46 oreover, mutation of three PKC sites in each UGT isozyme demonstrated that T73A/G and T202A/G caused

47 se results indicate that early and efficient UGT-mediated conjugation of DON is necessary and suffici

48 Eight UGTs were identified with activity against isoflavones,

49 pt expression patterns for each of the eight UGTs in Medicago organs and cell suspension cultures, an

50 s only the second example of a human estrone UGT.

51 y of colon cancer biopsies studies expressed UGT protein at levels greater than in HT29 cells but wit

52 Six of the recombinantly expressed UGTs conjugated the TNT-transformation products 2- and 4

53 Several human hepatic and extrahepatic UGT isozymes have been characterized with respect to the

54 For variants of active extrahepatic UGTs, the UGT1A8(173Ala/277Tyr) variant exhibited no det

55 patic UGTs 2B17 and 1A9 and the extrahepatic UGTs 1A8 and 1A10 exhibited the highest overall activity

56 All five UGTs contain a putative transmembrane domain at their C

57 The fourth UGT family, called UGT8, contains only one member that,

58 DP-glucose:glycoprotein glucosyltransferase (UGT) is a soluble protein of the endoplasmic reticulum (

59 ization of a phenol UDP-glucosyltransferase (UGT) from the silkworm, Bombyx mori, which was named BmU

60 gene family of Group 1 glucosyltransferases (UGTs) of Arabidopsis thaliana revealed a gene, UGT84B1,

61 condary metabolism UDP-glucosyltransferases (UGTs).

62 Uridine diphosphate glucunosyltransferases (UGTs) metabolize 15% of FDA approved drugs.

63 The 9 UDP-glucuronosyltranferases (UGTs) encoded by the UGT1 locus in humans are key enzyme

64 uridine diphosphate glucuronosyltransferase (UGT) 1A1; we investigated its role in the association be

65 dine 5'-diphosphate glucuronosyltransferase (UGT) operates in opposition to glucuronidase (GUS) to co

66 iphosphoglucuronate glucuronosyltransferase (UGT) isoform bilirubin-UGT1 were implicated in the absen

67 tion in hepatic UDP glucuronosyltransferase (UGT) 1A1 activity that can lead to CNS toxicity, brain d

68 e diphosphate (UDP)-glucuronosyltransferase (UGT) protein expression and UGT messenger RNA (mRNA) lev

69 The human UDP-glucuronosyltransferase (UGT) 1A (UGT1A) locus is regulated in a tissue specific

70 ency of hepatic UDP-glucuronosyltransferase (UGT) 1A1 activity.

71 ariation at the UDP-glucuronosyltransferase (UGT) 1A1 locus in breast cancer susceptibility.

72 curonidation by UDP-glucuronosyltransferase (UGT) 1A1, it is now known that immaturity of UGT1A1, in

73 olizing enzyme--UDP-glucuronosyltransferase (UGT) 1A1--to prevent the onset of neonatal hyperbilirubi

74 asone-inducible UDP-glucuronosyltransferase (UGT) 2B13 RNA is related in sequence to a family of UGT

75 ate-distributed UDP-glucuronosyltransferase (UGT) 2B15 metabolizes 5alpha-dihydrotestosterone (DHT) a

76 ects of TKIs on UDP-glucuronosyltransferase (UGT) activities, and to quantitatively evaluate their po

77 nt of bilirubin UDP-glucuronosyltransferase (UGT) activity and would be most pronounced in individual

78 yzed by the two UDP-glucuronosyltransferase (UGT) enzymes UGT2B15 and UGT2B17, is the major androgen

79 g half of human UDP-glucuronosyltransferase (UGT) enzymes, undergo alternative splicing, resulting in

80 idation via the UDP-glucuronosyltransferase (UGT) family of enzymes.

81 idation via the UDP-glucuronosyltransferase (UGT) family of enzymes.

82 between several UDP-glucuronosyltransferase (UGT) isoforms and cytochrome P450 3A4.

83 The UDP-glucuronosyltransferase (UGT) isozyme system is critical for protecting the body

84 UDP-glucuronosyltransferase (UGT) isozymes catalyze detoxification of numerous chemic

85 UDP-glucuronosyltransferase (UGT) isozymes detoxify metabolites, drugs, toxins, and e

86 nsferase (GST), UDP-glucuronosyltransferase (UGT), and phenol sulfotransferase 1A1 (SULT1A1) were mea

87 nsferase (GST), UDP-glucuronosyltransferase (UGT), and sulfotransferase (ST) expression was evaluated

88 UDP-glucuronosyltransferase (UGT)-mediated glucuronidation of benzo(a)pyrene-trans-7,

89 upregulation of UDP-glucuronosyltransferase (UGT).

90 atic bilirubin UPD- glucuronosyltransferase (UGT) is associated with this syndrome.

91 ested that the UDP-glucuronosyltransferases (UGT) 2B10 and 2B17 play major roles in nicotine glucuron

92 Human UDP-glucuronosyltransferases (UGT) are the dominant phase II conjugative drug metaboli

93 UDP-glucuronosyltransferases (UGT) catalyze the conjugation of lipophilic exobiotic an

94 thetase (GCS), UDP-glucuronosyltransferases (UGT),epoxide hydrolase, as well as a number of new genes

95 enzyme and to UDP-glucuronosyltransferases (UGT).

96 ridine diphosphate glucuronosyltransferases (UGTs).

97 Family 1 UDP-glucuronosyltransferases (UGTs) (UGT1A) are encoded by a locus that predicts the e

98 n catalyzed by UDP-glucuronosyltransferases (UGTs) and now report on the role of glucuronidation in d

99 UDP-glucuronosyltransferases (UGTs) are critical to the detoxification of numerous dru

100 UDP-glucuronosyltransferases (UGTs) are highly expressed in liver, intestine and kidne

101 UDP-glucuronosyltransferases (UGTs) are important enzymes that detoxicate many procarc

102 UDP-glucuronosyltransferases (UGTs) are membrane-bound proteins localized to the endop

103 19 functional UDP-glucuronosyltransferases (UGTs) in humans, UGT2B7 is involved in the metabolism of

104 o-UDP-GlcUA to UDP-glucuronosyltransferases (UGTs) in intact, but not in detergent-disrupted, ER vesi

105 ation of human UDP-glucuronosyltransferases (UGTs) in LS180 cells following curcumin treatment led to

106 onides) by the UDP-glucuronosyltransferases (UGTs) is a significant metabolic pathway that facilitate

107 ha (PPARalpha)-UDP-glucuronosyltransferases (UGTs) signalling is an important determinant of bile aci

108 an recombinant UDP-glucuronosyltransferases (UGTs) was characterized and compared with the glucuronid

109 es a family of UDP-glucuronosyltransferases (UGTs), which facilitate cellular detoxification and remo

110 inding site of UDP-glucuronosyltransferases (UGTs).

111 II superfamily UDP-glucuronosyltransferases (UGTs).

112 gene family of UDP-glucuronosyltransferases (UGTs).

113 es such as the UDP-glucuronosyltransferases (UGTs).

114 human hepatic UDP-glucuronosyltransferases (UGTs).

115 uses the traditional UDP-glycosyltransferase UGT co-substrate UDP-glucuronic acid.

116 150 different family 1 glycosyltransferase (UGT) genes.

117 y 1 UDP-sugar dependent glycosyltransferase (UGT) to facilitate acetophenone accumulation in the plan

118 The human UDP glycosyltransferase (UGT) superfamily comprises four families of enzymes that

119 UDP-glycosyltransferase (UGT) plays a major role in the diversity and reactivity

120 ila melanogaster, a UDP-glycosyltransferase (UGT), as well as a short chain dehydrogenase/reductase a

121 entified four family 1 glycosyltransferases (UGTs) that catalyze 3-O-glucosylation of the sapogenins

122 ne URIDINE DIPHOSPHATE GLYCOSYLTRANSFERASES (UGTs) from Arabidopsis (Arabidopsis thaliana).

123 nt uridine diphosphate glycosyltransferases (UGTs).

124 dine diphosphate (UDP) glycosyltransferases (UGTs) from Arabidopsis thaliana (Arabidopsis).

125 Hepatic UGT activities were mainly determined by UGT gene transc

126 For active hepatic UGTs, the UGT2B7(268Tyr) variant exhibited significant (

127 into the genetic network regulating hepatic UGTs.

128 The hepatic UGTs 2B17 and 1A9 and the extrahepatic UGTs 1A8 and 1A10

129 e UGTs in LS180 cells and 10 different human UGT cDNA-transfected COS-1 systems.

130 osyltransferase UGT2B7 is an important human UGT isoform that catalyzes the conjugation of many endog

131 osyltransferase UGT2B7 is an important human UGT isoform that catalyzes the conjugation of many endog

132 UDP-glucuronic acid binding domain of human UGT isoform 2B7 (UGT2B7), which catalyzes the conjugativ

133 th human liver microsomes, recombinant human UGT isoforms, and human hepatocytes.

134 Using recombinant human UGT isoforms, we show that glucuronic acid conjugation o

135 this review focuses on the role of the human UGT genetic polymorphisms in carcinogenesis, chemopreven

136 Two human UGT homologues, HUGT1 and HUGT2, exist that share 55% id

137 avonoid glucosyltransferases indicates human UGTs share a common catalytic mechanism.

138 f having a complete set of recombinant human UGTs for comparative functional analyses.

139 brogated activity, strongly suggesting human UGTs also utilize a serine hydrolase-like catalytic mech

140 However, as yet not all of the human UGTs have been cloned and characterized.

141 2- to 4-fold interindividual differences in UGT activity and qualitative differences between individ

142 of immunodetectable [(33)P]orthophosphate in UGTs and protein kinase Cepsilon (PKCepsilon), following

143 metabolites and functional polymorphisms in UGTs 2B10 and 2B17 was analyzed in urine specimens from

144 ve form of human PXR show markedly increased UGT activity toward steroid, heme, and carcinogens, enha

145 o the expression of at least nine individual UGT genes.

146 The affinity of individual UGT enzymes as determined by K(m) analysis was UGT1A10 >

147 Indinavir was found to competitively inhibit UGT enzymatic activity (K(I) = 183 microM) while concomi

148 ereas saquinavir also competitively inhibits UGT activity, this drug has not been associated with hyp

149 Interestingly, UGT activity toward tertiary amines and some steroid hor

150 Hence, although higher liver UGT activity may protect the liver against ABP, it incre

151 and characterization of several rabbit liver UGT cDNAs.

152 expression for all other forms of rat liver UGT and ST isozymes that were tested was not significant

153 Major UGT isoforms were examined for their capacity to metabol

154 curonosyltransferase 1A7 (UGT1A7) is a major UGT contributing to the glucuronidation of xenobiotic ph

155 The UGT1A1 enzyme is a major UGT involved in estradiol glucuronidation.

156 ystal structure of any region of a mammalian UGT drug metabolism enzyme.

157 functional polymorphisms in TAM-metabolizing UGTs, including UGT2B7 and potentially UGT1A8, may be im

158 33+/-6.3, and 24+/-2.4 nL x min(-1) x microg UGT protein(-1), respectively), with UGT2B17 exhibiting

159 Microsomal UGT protein expression and UGT mRNA levels were unaltere

160 However, microsomal UGT activities in colon were up to 96-fold lower for man

161 The new UGT has been designated UGT2B16.

162 nal biologic role(s) for the truncated novel UGT proteins.

163 ectrometry for their profile and activity of UGT isozymes and screened for effective inhibitors of gl

164 Findings uncover new aspects of UGT functions diverging from their transferase activity.

165 13 RNA is related in sequence to a family of UGT genes.

166 Inhibition of UGT activity by PKCepsilon-specific antagonist peptide o

167 Furthermore, inhibition of UGT phosphorylation and activity by treatment with PKCep

168 tudy was to identify the specific isoform of UGT involved in SN-38 glucuronidation.

169 The lack of selection for higher levels of UGT capacity in the colon cells suggests that high level

170 as tested in vitro, in the Gunn rat model of UGT deficiency, and in HIV-infected patients with and wi

171 Inhibition kinetic profiles of a panel of UGT enzymes (UGT1A1, 1A3, 1A4, 1A6, 1A7, 1A8, 1A9, 1A10,

172 sm involving PKC-mediated phosphorylation of UGT such that phosphoserine/threonine regulates substrat

173 A range of UGT aglycones were capable of modulating glucuronidation

174 to be the most important trans-regulators of UGT transcription (median and range of correlation coeff

175 been carried out to characterize the role of UGT pharmacogenetics in several types of cancer, and the

176 In addition to predicting common sites of UGT conjugation, like hydroxyl groups, it can also accur

177 computational method for predicting sites of UGT-mediated metabolism on drug-like molecules.

178 yzed whether NGT and both splice variants of UGT (UGT1 and UGT2) are able to interact with four diffe

179 though much is known regarding the number of UGTs that make up the UGT1 and UGT2 gene families, as de

180 nctionally relevant genetic polymorphisms of UGTs are reviewed.

181 anges that confer sugar donor selectivity on UGTs, and demonstrates the usefulness of natural variati

182 tures that are different from those of other UGTs and related to the enzyme's functions and substrate

183 contains only one member that, unlike other UGTs, is considered biosynthetic.

184 enates from HEK293 cell lines overexpressing UGT wild-type or variant UGT were used.

185 nse elements (AREs), the mechanism of phenol UGT induction has remained unclear.

186 Thus, we propose that intestinal PPARalpha-UGTs and downstream FXR-FGF15 signalling play vital role

187 ation of the intestinal peroxisome PPARalpha-UGTs pathway.

188 ribe a simple heuristic model for predicting UGT-mediated sites of metabolism that performs nearly as

189 eted functional screening of the recombinant UGTs for their biological substrates was performed by ac

190 NA and activation of curcumin-down-regulated UGTs with typical PKC agonists verified a central PKC ro

191 ctionally characterize nine ripening-related UGTs (UDP-glucosyltransferases) in Fragaria that functio

192 ce of type 2 innate immunity for restricting UGT tissue damage in Chlamydia-infected mice, and in ini

193 rted intermediate inhibition against several UGTs (i.e., UGT1A7 by lapatinib; UGT1A1 by imatinib; UGT

194 The cancer-related substrates for several UGTs are summarized, and the functionally relevant genet

195 found to exhibit broad inhibition on several UGTs, particularly potent competitive inhibition against

196 These results suggest that several UGTs may play an important role in the overall glucuroni

197 Overall, these results suggest that several UGTs play an important role in the metabolism of SAHA an

198 Some UGTs showed a rather broad substrate tolerance and gluco

199 QO1, GST, and SULT1A1, but not with striatal UGT.

200 or the PKC inhibitor calphostin-C, suggested UGT phosphorylation is supported by active PKC(s).

201 PKC-dependent signaling evidently sustaining UGT phosphorylation and activity.

202 n, we examined UDP-glucurono-syltransferase (UGT) activity in parental and resistant cells by TLC.

203 Analysis of recombinant His-tag UGTs from the 1A family for their ability to glucuronida

204 ordihydroguaiaretic acid, reversibly targets UGTs causing inhibition without affecting protein levels

205 All tested UGTs preferred UDP-glucose as sugar donor.

206 We found that UGT expression and activity were highly variable among t

207 These data suggest that UGT isoforms may form complexes (dimers, tetramers, etc.

208 In summary, we demonstrate that UGTs are located in gastrointestinal mucosa, have vast o

209 curcumin treatment led to the discovery that UGTs require phosphorylation.

210 Our results show that UGTs play an integral role in the biochemical mechanism

211 These data suggest that UGTs 2B10 and 2B17 play important roles in the glucuroni

212 fense gene families, including the ABCC, the UGT, and the CYP families, have undergone expansion in t

213 In addition, the UGT isoforms tested here may have interacted with CYP3A4

214 isms have been identified for almost all the UGT family members.

215 Although AR and FOXA1 bound the UGT promoters in AR-positive/ERalpha-negative breast can

216 We have characterized the UGT-catalyzed metabolic products of AalphaC and the geno

217 Importantly, the UGT sequelae were significantly reduced in mice immunize

218 To examine whether polymorphisms in the UGT enzymes responsible for the glucuronidation of activ

219 mation and tissue repair are elicited in the UGT of Chlamydia-infected women.

220 An asparagine (Asn-391) in the UGT signature sequence of UGT3A1 is necessary for utiliz

221 evidence for the lumenal orientation of the UGT active site, and support the view that translocation

222 d support the view that translocation of the UGT cosubstrate is a rate-limiting step of the glucuroni

223 mino-acid identity with other members of the UGT family.

224 Identification of the UGT responsible for glucuronidation of SN-38 and the ant

225 cent biochemical evidence indicates that the UGT proteins may oligomerize in the membrane, but conclu

226 e involvement of the 2B17 isoform within the UGT protein family.

227 As the UGTs from both the resistant and susceptible types of B.

228 ns involved in drug disposition, such as the UGTs, significantly improves the ability to evaluate and

229 dinitrotoluenes, were also conjugated by the UGTs, but to a lesser extent.

230 To characterize the UGTs active against SAHA, homogenates from HEK293 cell l

231 d to identify the expression patterns of the UGTs in human tissues, paying particular attention to ex

232 Overexpression of two of these UGTs, 743B4 and 73C1, in Arabidopsis resulted in increas

233 iption factors (TFs) known to regulate these UGTs were quantified.

234 ical substrate but also disclosed that these UGTs may add to the production of further glycoconjugate

235 To date other substrates for this UGT have not been identified and there has been no sugge

236 Thus, UGTs, usually important enzymes in the detoxication of m

237 he residues that confer sugar specificity to UGT family members and suggests a primate-specific innov

238 equires regulated phosphorylation similar to UGTs already analyzed.

239 do not cause permanent upper genital tract (UGT) damage.

240 arance and reduction of upper genital tract (UGT) pathological sequelae.

241 from the lineages causing urogenital tract (UGT) and lymphogranuloma venerum diseases.

242 f the developing mammalian urogenital tract (UGT).

243 idine-disphosphate glucuronosyl transferase (UGT) enzymes catalyze the formation of glucuronide conju

244 UDP-galactose transporter (UGT; SLC35A2) and UDP-N-acetylglucosamine transporter (N

245 ruce bud burst and shoot growth revealed two UGTs, PgUGT5 and PgUGT5b, that glycosylate pungenol.

246 ines overexpressing UGT wild-type or variant UGT were used.

247 ll lines overexpressing wild-type or variant UGTs were examined for their activities against TAM meta

248 ne of the Drosophila families and vertebrate UGTs.

249 eir C terminus as is the case for vertebrate UGTs where it is required for enzymatic activity.

250 further biotransformed into glucuronides via UGT-mediated pathways.

251 eme oxygenase expression was higher, whereas UGT expression was lower, in neonatal compared with adul

252 homa isolates appear to be recombinants with UGT C. trachomatis genome backbones, in which loci that

253 cent and co-immunoprecipitation studies with UGT-transfected cells showed co-localization of UGT1A7Hi

254 different clades, and several clustered with UGTs annotated as glycosylating non-flavonoid substrates

255 rachoma lineage, instead being placed within UGT clades of the C. trachomatis phylogenetic tree.