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Literature summary for 2.4.1.17 extracted from

  • Bock, K.W.
    Roles of human UDP-glucuronosyltransferases in clearance and homeostasis of endogenous substrates, and functional implications (2015), Biochem. Pharmacol., 96, 77-82.
    View publication on PubMed

Application

Application Comment Organism
diagnostics androgen glucuronidation by UGT2B17 is particularly interesting in doping control Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
gene UGT2A2
-
Homo sapiens O60656 UGT1A9; gene UGT1A9
-
Homo sapiens O75310 UGT2B11; gene UGT2B11
-
Homo sapiens O75795 UGT2B17; gene UGT2B17
-
Homo sapiens P06133 UGT2B4; gene UGT2B4
-
Homo sapiens P16662 UGT2B7; gene UGT2B7
-
Homo sapiens P19224 UGT1A6; gene UGT1A6
-
Homo sapiens P22309 UGT1A1; gene UGT1A1
-
Homo sapiens P22310 UGT1A4; gene UGT1A4
-
Homo sapiens P35503 UGT1A3; gene UGT1A3
-
Homo sapiens P35504 UGT1A5; gene UGT1A5
-
Homo sapiens P36537 UGT2B10; gene UGT2B10
-
Homo sapiens P54855 UGT2B15; gene UGT2B15
-
Homo sapiens Q6UWM9 UGT2A3; gene UGT2A3
-
Homo sapiens Q9BY64 UGT2B28; gene UGT2B28
-
Homo sapiens Q9HAW7 UGT1A7; gene UGT1A7
-
Homo sapiens Q9HAW8 UGT1A10; gene UGT1A10
-
Homo sapiens Q9HAW9 UGT1A8; gene UGT1A8
-
Homo sapiens Q9Y4X1 UGT2A1; gene UGT2A1
-

Source Tissue

Source Tissue Comment Organism Textmining
brain for example in the nucleus bulbosus of the olfactory system Homo sapiens
-
breast
-
Homo sapiens
-
Caco-2 cell
-
Homo sapiens
-
colon high expression level of UGT1A6 Homo sapiens
-
gastrointestinal tract
-
Homo sapiens
-
intestine
-
Homo sapiens
-
keratinocyte
-
Homo sapiens
-
liver
-
Homo sapiens
-
liver strong expression of UGT2B4 in human fetal liver Homo sapiens
-
olfactory tissue
-
Homo sapiens
-
small intestine high expression level of UGT1A6 Homo sapiens
-
stellate cell
-
Homo sapiens
-
stomach high expression level of UGT1A6 Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
additional information the enzyme UGT2B4 is also active with bile acids Homo sapiens ?
-
?
UDP-alpha-D-glucuronate + chloramphenicol
-
Homo sapiens UDP + chloramphenicol beta-D-glucuronide
-
?
UDP-alpha-D-glucuronate + sorafenib
-
Homo sapiens UDP + ?
-
?
UDP-D-glucuronate + nicotine
-
Homo sapiens UDP + ?
-
?
UDP-glucuronate + (S)-oxazepam
-
Homo sapiens UDP + (S)-oxazepam beta-D-glucuronoside
-
?
UDP-glucuronate + 1,25-dihydroxyergocalciferol
-
Homo sapiens UDP + 1,25-dihydroxyergocalciferol beta-D-glucuronoside
-
?
UDP-glucuronate + 1-hydroxypyrene
-
Homo sapiens UDP + 1-hydroxypyrene beta-D-glucuronoside
-
?
UDP-glucuronate + 12-hydroxyeicosatetraenoic acid
-
Homo sapiens UDP + 12-hydroxyeicosatetraenoyl beta-D-glucuronoside
-
?
UDP-glucuronate + 12-hydroxyeicosatetraenoic acid
-
Homo sapiens UDP + 12-hydroxyeicosatetraenoyl-beta-D-glucuronoside
-
?
UDP-glucuronate + 15-hydroxyeicosatetraenoic acid
-
Homo sapiens UDP + 15-hydroxyeicosatetraenoyl beta-D-glucuronoside
-
?
UDP-glucuronate + 15-hydroxyeicosatetraenoic acid
-
Homo sapiens UDP + 15-hydroxyeicosatetraenoyl-beta-D-glucuronoside
-
?
UDP-glucuronate + 20-hydroxyeicosatetraenoic acid
-
Homo sapiens UDP + 20-hydroxyeicosatetraenoyl beta-D-glucuronoside
-
?
UDP-glucuronate + 25-hydroxyergocalciferol
-
Homo sapiens UDP + 25-hydroxyergocalciferol beta-D-glucuronoside
-
?
UDP-glucuronate + 4-hydroxyestradiol
-
Homo sapiens UDP + 4-hydroxyestradiol beta-D-glucuronoside
-
?
UDP-glucuronate + 4-hydroxyretinoic acid mainly conjugated by UGT2B7 Homo sapiens UDP + 4-hydroxyretinoic acid beta-D-glucuronoside
-
?
UDP-glucuronate + 5-hydroxytryptophol
-
Homo sapiens UDP + 5-hydroxy-tryptophol beta-D-glucuronoside
-
?
UDP-glucuronate + 5-hydroxytryptophol mucosal serotonin and its metabolite 5-hydroxytryptophol are solely conjugated by UGT1A6 Homo sapiens UDP + 5-hydroxytryptophol beta-D-glucuronoside
-
?
UDP-glucuronate + 7-ethyl-10-hydroxy-camptothecin i.e. SN-38, an active metabolite of irinotecan Homo sapiens UDP + 7-ethyl-10-hydroxy-camptothecin beta-D-glucuronoside
-
?
UDP-glucuronate + all-trans-retinoic acid mainly conjugated by UGT2B7 Homo sapiens UDP + all-trans-retinoic acid beta-D-glucuronoside
-
?
UDP-glucuronate + amitryptiline
-
Homo sapiens UDP + amitryptiline beta-D-glucuronoside
-
?
UDP-glucuronate + androstanediol
-
Homo sapiens UDP + androstanediol beta-D-glucuronoside
-
?
UDP-glucuronate + bilirubin
-
Homo sapiens UDP + bilirubin beta-D-glucuronoside
-
?
UDP-glucuronate + carvedilol
-
Homo sapiens UDP + carvedilol beta-D-glucuronoside
-
?
UDP-glucuronate + chenodeoxycholic acid
-
Homo sapiens UDP + chenodeoxycholic acid 24-beta-D-glucuronoside
-
?
UDP-glucuronate + citronellol
-
Homo sapiens UDP + citronellol beta-D-glucuronoside
-
?
UDP-glucuronate + deferiprone
-
Homo sapiens UDP + deferiprone beta-D-glucuronoside
-
?
UDP-glucuronate + diclofenac
-
Homo sapiens UDP + diclofenac beta-D-glucuronoside
-
?
UDP-glucuronate + dihydrotestosterone
-
Homo sapiens UDP + dihydrotestosterone beta-D-glucuronoside
-
?
UDP-glucuronate + diphenhydramine
-
Homo sapiens UDP + diphenhydramine beta-D-glucuronoside
-
?
UDP-glucuronate + dopamine
-
Homo sapiens UDP + dopamine beta-D-glucuronoside
-
?
UDP-glucuronate + epirubicin
-
Homo sapiens UDP + epirubicin beta-D-glucuronoside
-
?
UDP-glucuronate + estradiol
-
Homo sapiens UDP + estradiol beta-D-glucuronoside
-
?
UDP-glucuronate + estradiol the enzyme UGT1A9 is active with estrogens Homo sapiens UDP + estradiol beta-D-glucuronoside
-
?
UDP-glucuronate + estrone
-
Homo sapiens UDP + estrone beta-D-glucuronoside
-
?
UDP-glucuronate + ethinylestradiol
-
Homo sapiens UDP + ethinylestradiol beta-D-glucuronoside
-
?
UDP-glucuronate + etoposide
-
Homo sapiens UDP + etoposide beta-D-glucuronoside
-
?
UDP-glucuronate + flavopiridol
-
Homo sapiens UDP + flavopiridol beta-D-glucuronoside
-
?
UDP-glucuronate + hyodeoxycholic acid
-
Homo sapiens UDP + hyodeoxycholoyl beta-D-glucuronoside
-
?
UDP-glucuronate + imipramine
-
Homo sapiens UDP + imipramine beta-D-glucuronoside
-
?
UDP-glucuronate + ketotifen
-
Homo sapiens UDP + ketotifenbeta-D-glucuronoside
-
?
UDP-glucuronate + L-thyroxine
-
Homo sapiens UDP + L-thyroxyl beta-D-glucuronoside
-
?
UDP-glucuronate + L-thyroxine UGT1A1 and UGT1A3 are the major UGTs glucuronidating T4 at the hydroxyl and carboxyl groups, respectively Homo sapiens UDP + L-thyroxyl beta-D-glucuronoside
-
?
UDP-glucuronate + lamotrigine
-
Homo sapiens UDP + lamotrigine beta-D-glucuronoside
-
?
UDP-glucuronate + leukotriene B4
-
Homo sapiens UDP + leukotriene B4 beta-D-glucuronoside
-
?
UDP-glucuronate + lorazepam
-
Homo sapiens UDP + lorazepam beta-D-glucuronoside
-
?
UDP-glucuronate + mycophenolic acid
-
Homo sapiens UDP + mycophenolic acid beta-D-glucuronoside
-
?
UDP-glucuronate + mycophenolic acid
-
Homo sapiens UDP + mycophenoloyl beta-D-glucuronoside
-
?
UDP-glucuronate + naproxen
-
Homo sapiens UDP + naproxen beta-D-glucuronoside
-
?
UDP-glucuronate + olanzapine
-
Homo sapiens UDP + olanzapine beta-D-glucuronoside
-
?
UDP-glucuronate + paracetamol
-
Homo sapiens UDP + paracetamol beta-D-glucuronoside
-
?
UDP-glucuronate + pregnan-3,17-diol
-
Homo sapiens UDP + pregnan-3,17-diol beta-D-glucuronoside
-
?
UDP-glucuronate + propofol
-
Homo sapiens UDP + propofol beta-D-glucuronoside
-
?
UDP-glucuronate + quercetin
-
Homo sapiens UDP + quercetin beta-D-glucuronoside
-
?
UDP-glucuronate + serotonin mucosal serotonin and its metabolite 5-hydroxytryptophol are solely conjugated by UGT1A6 Homo sapiens UDP + serotonin beta-D-glucuronoside
-
?
UDP-glucuronate + tacrolimus
-
Homo sapiens UDP + tacrolimus beta-D-glucuronoside
-
?
UDP-glucuronate + tamoxifen
-
Homo sapiens UDP + tamoxifen beta-D-glucuronoside
-
?
UDP-glucuronate + Telmisartan
-
Homo sapiens UDP + Telmisartan beta-D-glucuronoside
-
?
UDP-glucuronate + testosterone
-
Homo sapiens UDP + testosterone beta-D-glucuronoside
-
?
UDP-glucuronate + thymol
-
Homo sapiens UDP + thymol beta-D-glucuronoside
-
?
UDP-glucuronate + trifluperazine
-
Homo sapiens UDP + trifluperazine
-
?
UDP-glucuronate + vorinostat
-
Homo sapiens UDP + vorinostat beta-D-glucuronoside
-
?
UDP-glucuronate + zidovudine
-
Homo sapiens UDP + zidovudine beta-D-glucuronoside
-
?

Synonyms

Synonyms Comment Organism
UGT
-
Homo sapiens
UGT1A1
-
Homo sapiens
UGT1A10
-
Homo sapiens
UGT1A3
-
Homo sapiens
UGT1A4
-
Homo sapiens
UGT1A5
-
Homo sapiens
UGT1A6
-
Homo sapiens
UGT1A7
-
Homo sapiens
UGT1A8
-
Homo sapiens
UGT1A9
-
Homo sapiens
UGT2A1
-
Homo sapiens
UGT2A2
-
Homo sapiens
UGT2A3
-
Homo sapiens
UGT2B10
-
Homo sapiens
UGT2B11
-
Homo sapiens
UGT2B15
-
Homo sapiens
UGT2B17
-
Homo sapiens
UGT2B28
-
Homo sapiens
UGT2B4
-
Homo sapiens
UGT2B7
-
Homo sapiens

Expression

Organism Comment Expression
Homo sapiens all-trans-retinoic acid appears to downregulate UGT2B7 expression down
Homo sapiens bilirubin and 20-hydroxyeicosatetraenoic acid act as activators of transcription factors that regulate UGT expression, and are involved in important feedback loops up
Homo sapiens bilirubin and 20-hydroxyeicosatetraenoic acid act as activators of transcription factors that regulate UGT expression, and are involved in important feedback loops. Induction of UGT1A1 in keratinocytes by UV radiation-generated 6-formylindolo[3,2-b]carbazole, which is a potent activator of AhR transcription factor. Induction of UGT1A1 in the neonatal period is controlled in part by a cluster of 6 transcription factor response elements, termed gtPBREM (phenobarbital-responsive enhancer module) binding CAR, PXR, AhR, NRF2, PPARa and glucocorticoid receptor up
Homo sapiens bilirubin and 20-hydroxyeicosatetraenoic acid act as activators of transcription factors that regulate UGT expression, and are involved in important feedback loops. Intestinal UGT1A6 expression and serotonin glucuronidation is induced by activation of the AhR and Nrf2, the genetically-linked master regulator of the antioxidant response up

General Information

General Information Comment Organism
evolution feedback loops between endobiotic UGT substrates and their transcription factors suggest an important role of their glucuronidation in evolution Homo sapiens
malfunction due to frequent haplotype blocks within the UGT1 gene locus, the Gilbert variant UGT1A1*28 is often associated with polymorphisms of UGT1A6. Rare hyperserotoninemia mimicking carcinoid syndrome may be due to the linked dual polymorphisms of UGT1A1 and UGT1A6 Homo sapiens
malfunction life saving function of bilirubin glucuronidation is obvious from death of children carrying the UGT1A1-deficient Crigler-Najjar syndrome, type 1 genotype. Excessive serum bilirubin levels leading to brain damage in neonates are prevented by induction of UGT1A1, the sole enzyme conjugating bilirubin. Reduced L-thyroxine (T4)glucuronidation in carriers of the Gilbert genotype UGT1A1*28 substantiates a role for UGT1A1 in T4 glucuronidation. Due to frequent haplotype blocks within the UGT1 gene locus, the Gilbert variant UGT1A1*28 is often associated with polymorphisms of UGT1A6. Rare hyperserotoninemia mimicking carcinoid syndrome may be due to the linked dual polymorphisms of UGT1A1 and UGT1A6 Homo sapiens
metabolism feedback loops between endobiotic UGT substrates and their transcription factors suggest an important role of their glucuronidation in evolution Homo sapiens
metabolism feedback loops between endobiotic UGT substrates and their transcription factors suggest an important role of their glucuronidation in evolution. AhR- and Nrf2-binding domains, termed XRE (xenobiotic responsive element) and ARE (antioxidant responsive element), respectively, are identified in the regulatory region of UGT1A1 and UGT1A6. The neurotransmitter serotonin is also solely glucuronidated by the human UGT1A6, which is highly expressed in the stomach and intestine. Serotonin exhibits a variety of functions in the gastrointestinal tract including gastrointestinal motility, mucosal growth/maintenance and intestinal inflammation Homo sapiens
physiological function human UDP-glucuronosyltransferases are major phase II enzymes in the drug metabolism system, they also have a role in clearance and homeostasis of endogenous substrates, UGTs are often involved in detoxification of endobiotic CYP metabolites. Species- and tissue/cell-dependent regulation of UGT expression by ligand-activated transcription factors is often involved in endobiotic homeostasis. All UGT1 family members appear to be controlled by the AhR transcription factor. Bilirubin and 20-hydroxyeicosatetraenoic acid act as activators of transcription factors that regulate UGT expression, and are involved in important feedback loops Homo sapiens
physiological function human UDP-glucuronosyltransferases are major phase II enzymes in the drug metabolism system, they also have a role in clearance and homeostasis of endogenous substrates, UGTs are often involved in detoxification of endobiotic CYP metabolites. Species- and tissue/cell-dependent regulation of UGT expression by ligand-activated transcription factors is often involved in endobiotic homeostasis. All UGT1 family members appear to be controlled by the AhR transcription factor. Bilirubin and 20-hydroxyeicosatetraenoic acid act as activators of transcription factors that regulate UGT expression, and are involved in important feedback loops, proposed feedback loop between bilirubin, AhR and AhR-controlled UGT1A1. UGT1A1 is the sole enzyme conjugating bilirubin. AhR- and Nrf2-binding domains, termed XRE (xenobiotic responsive element) and ARE (antioxidant responsive element), respectively, are identified in the regulatory region of UGT1A1 and UGT1A6 Homo sapiens
physiological function human UDP-glucuronosyltransferases are major phase II enzymes in the drug metabolism system, they also have a role in clearance and homeostasis of endogenous substrates, UGTs are often involved in detoxification of endobiotic CYP metabolites. Species- and tissue/cell-dependent regulation of UGT expression by ligand-activated transcription factors is often involved in endobiotic homeostasis. All UGT1 family members appear to be controlled by the AhR transcription factor. Bilirubin and 20-hydroxyeicosatetraenoic acid act as activators of transcription factors that regulate UGT expression, and are involved in important feedback loops. In the intestine, L-thyroxine is conjugated by UGT1A8 and UGT1A10 suggesting first-pass metabolism of oral L-thyronine, although UGT1A1 and UGT1A3 are the major UGTs glucuronidating T4 at the hydroxyl and carboxyl groups, respectively Homo sapiens
physiological function human UDP-glucuronosyltransferases are major phase II enzymes in the drug metabolism system, they also have a role in clearance and homeostasis of endogenous substrates, UGTs are often involved in detoxification of endobiotic CYP metabolites. Species- and tissue/cell-dependent regulation of UGT expression by ligand-activated transcription factors is often involved in endobiotic homeostasis. All UGT1 family members appear to be controlled by the AhR transcription factor. Bilirubin and 20-hydroxyeicosatetraenoic acid act as activators of transcription factors that regulate UGT expression, and are involved in important feedback loops. The family 2 member UGT2B7 is regulated by Nrf2, but not by the AhR. UGT1A9- and UGT2B7-mediated detoxification of 20-hydroxyeicosatetraenoic acid to prevent hypertension. UGT1A9 and UGT2B7 appear to be major UGT enzymes responsible for 20-hydroxyeicosatetraenoic acid and leukotriene B4 glucuronidation Homo sapiens
physiological function human UDP-glucuronosyltransferases are major phase II enzymes in the drug metabolism system, they also have a role in clearance and homeostasis of endogenous substrates, UGTs are often involved in detoxification of endobiotic CYP metabolites. Species- and tissue/cell-dependent regulation of UGT expression by ligand-activated transcription factors is often involved in endobiotic homeostasis. All UGT1 family members appear to be controlled by the AhR transcription factor. Bilirubin and 20-hydroxyeicosatetraenoic acid act as activators of transcription factors that regulate UGT expression, and are involved in important feedback loops. UGT1A9- and UGT2B7-mediated detoxification of 20-hydroxyeicosatetraenoic acid to prevent hypertension. UGT1A9 and UGT2B7 appear to be major UGT enzymes responsible for 20-hydroxyeicosatetraenoic acid and leukotriene B4 glucuronidation Homo sapiens
physiological function human UDP-glucuronosyltransferases are major phase II enzymes in the drug metabolism system, they also have a role in clearance and homeostasis of endogenous substrates, UGTs are often involved in detoxification of endobiotic CYP metabolites. Species- and tissue/cell-dependent regulation of UGT expression by ligand-activated transcription factors is often involved in endobiotic homeostasis. All UGT1 family members appear to be controlled by the AhR transcription factor. Bilirubin and 20-hydroxyeicosatetraenoic acid act as activators of transcription factors that regulate UGT expression, and are involved in important feedback loops. UGT2B28 is involved in estradiol and testosterone glucuronidation in a variety of tissues including breast cells Homo sapiens
physiological function human UDP-glucuronosyltransferases are major phase II enzymes in the drug metabolism system, they also have a role in clearance and homeostasis of endogenous substrates. Species- and tissue/cell-dependent regulation of UGT expression by ligand-activated transcription factors is often involved in endobiotic homeostasis. All UGT1 family members appear to be controlled by the AhR transcription factor. Bilirubin and 20-hydroxyeicosatetraenoic acid act as activators of transcription factors that regulate UGT expression, and are involved in important feedback loops Homo sapiens