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