UDP-glycosyltransferase (UGT) Phenotyping Assay Services
UDP-glycosyltransferase (UGT) Superfamily
The UDP-glycosyltransferase (UGT) superfamily is a group of enzymes that catalyze the covalent addition of sugars, primarily from nucleotide UDP-sugar donors, to functional groups on a wide range of lipophilic molecules. In mammals, the UGT superfamily comprises four main families: UGT1, UGT2, UGT3, and UGT8.
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Families
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Characteristics
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UGT1 and UGT2
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These families contain enzymes that play crucial roles in pharmacology and toxicology, particularly in drug metabolism and clearance. They are involved in the detoxification of various exogenous chemicals and the regulation of endogenous signaling molecules. UGT1 and UGT2 enzymes are highly expressed in detoxifying organs such as the liver, kidney, and intestine, and their expression is regulated by both endogenous and exogenous signals.
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UGT3 and UGT8
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These families have been characterized more recently. UGT3 enzymes utilize different UDP-sugar donors, such as UDP-glucose and UDP-xylose, while UGT8 specifically uses UDP-galactose. To date, the contributions of UGT3 and UGT8 to drug metabolism appear to be relatively minor, but they may play significant roles in modulating endogenous signaling pathways.
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UGT Phenotyping Assay at Creative Biolabs
The process of UGT reaction phenotyping focuses on identifying the specific UGT enzymes that play a key role in the glucuronidation of a given compound. This method is frequently employed in the drug development phase for compounds predominantly metabolized through glucuronidation, facilitating informed predictions regarding possible drug interactions and variations in pharmacogenomics.
Creative Biolabs evaluates whether the test compound is a substrate of a specific UGT enzyme by HPLC-MS/MS. The focus of the UGT enzymes we assessed is primarily on the UGT1 and UGT2 families. Creative Biolabs is devoted to offering robust support for your research projects. Should you find our services appealing, please do not hesitate to contact us. Additionally, you might find the following ADME services we offer to be of interest.
Additional Information
These UGT enzymes play crucial roles in drug metabolism, detoxification, and the regulation of endogenous signaling molecules. The UGT enzymes we assessed with a detailed list as follows:
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UTG
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Characteristics
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UGT1A1
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Primarily responsible for the elimination of its main endogenous substrate, bilirubin. Low-activity or low-expression alleles of UGT1A1 are associated with the development of unconjugated hyperbilirubinemia.
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UGT1A3
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Expressed in the liver and gastrointestinal tract, involved in the metabolism of various drugs and endogenous compounds.
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UGT1A4
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Known for its N-glucuronidation activity, it has numerous endogenous substrates, including progestins and carcinogens.
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UGT1A6
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Involved in the metabolism of numerous endogenous substances and drugs, although the exact substrates are not specified.
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UGT1A8
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Mainly expressed in the intestine, involved in the first-pass metabolism of dietary constituents and a wide range of orally administered therapeutic drugs.
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UGT1A9
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Highly expressed in the intestine and liver, responsible for the metabolism of various dietary compounds and carcinogens, particularly related to ethanol glucuronidation.
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UGT1A10
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Primarily expressed in the intestine, participates in the metabolism of various dietary constituents and drugs.
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UGT2B4
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Involved in the metabolism of numerous compounds.
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UGT2B7
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Highly expressed in the liver, responsible for the glucuronidation of various xenobiotics, including drugs and dietary compounds.
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UGT2B15
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Widely expressed in various tissues, involved in the metabolism of numerous endogenous compounds and drugs, particularly androgens and their metabolites.
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For Research Use Only | Not For Clinical Use
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