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PsychedeliaDokholyan Laboratory
TargetEnzymes

UDP-glucuronosyltransferase 1A8

Named enzymes, including the metabolising cytochromes and the monoamine oxidases.

Measurements
2
Compounds
2
Binding constants
0
Median pX
—

I · Identity

What this target is

Its function as UniProt states it, where in a cell the protein is found, and which cell types and tissues transcribe its gene.

Protein

UD18_HUMANUGT1A8Homo sapiens

UDP-glucuronosyltransferase 1A8

UDP-glucuronosyltransferase (UGT) that catalyzes phase II biotransformation reactions in which lipophilic substrates are conjugated with glucuronic acid to increase the metabolite's water solubility, thereby facilitating excretion into either the urine or bile15472229,16595710,18004212,18052087,18674515,18719240,19545173,23288867,21422672. Essential for the elimination and detoxification of drugs, xenobiotics and endogenous compounds15472229,16595710,23288867. Catalyzes the glucuronidation of endogenous steroid hormones such as androgens and estrogens15472229,16595710,18719240,23288867. Produces dihydrotestosterone (DHT) diglucuronide from the DHT after two subsequent glucoronidation steps16595710. Involved in the glucuronidation of the phytochemical ferulic acid at the phenolic or the carboxylic acid group21422672. Also catalyzes the glucuronidation of the isoflavones genistein, daidzein, glycitein, formononetin, biochanin A and prunetin, which are phytoestrogens with anticancer and cardiovascular properties18052087,19545173. Involved in the glucuronidation of the AGTR1 angiotensin receptor antagonist caderastan, a drug which can inhibit the effect of angiotensin II18674515. Also metabolizes mycophenolate, an immunosuppressive agent15470161,18004212
Lacks UGT glucuronidation activity but acts as a negative regulator of isoform 1

Quoted from UniProt’s FUNCTION annotation for Q9HAW9 (reviewed). The superscript numbers are UniProt’s own PubMed citations, kept in the sentence and in order, each linking to the paper it names.

What it acts with

STRING’s highest-confidence human functional partners. The combined score mixes several kinds of evidence, so each channel is shown separately — a partner supported by experiment is a different claim from one supported only by text mining, and for a receptor this is where its coupling appears as evidence rather than as assertion.

PartnerCombinedExperimentDatabaseText mining
UGT1A60.9970.9940.0000.063
UGT1A30.9970.9940.0000.065
UGT1A90.9970.9940.0000.054
UGT1A10.9960.9940.0000.061
UGT1A100.9950.9940.0000.051
UGT1A70.9940.9940.0000.052
UGT1A40.9940.9940.0000.051
CYP3A40.9920.0450.9060.914
SLC35A20.9890.0000.0000.989
CYP1A10.9850.0000.9090.838

Where it sits in the cell

UniProt, curated Endoplasmic reticulum membrane

Expression by cell type

Single cell type RNA, the 3 highest of those the Human Protein Atlas reports for this gene. Transcript, not protein, and a cell type rather than a tissue.

  • Urothelial cells19.1 nCPM
  • Prostatic hillock cells13 nCPM
  • Papillary tip epithelial cells5.7 nCPM

Expression by tissue

The tissues this gene is enriched in, by consensus RNA. A tissue absent from this list is one the Atlas does not call specific for this gene, which is not the same as absent from it.

  • urinary bladder28 nTPM
  • intestine14.9 nTPM
  • gallbladder6.1 nTPM

IV · Evidence

Every measurement at this target

Each row links to the ChEMBL assay it came from.

Other measurements 2

Everything else ChEMBL recorded for this compound — percentage inhibition, efficacy, half-life, cytotoxicity. Reported in the assay's own units, which is why no value is converted here.

TargetClassTypeValue (nM)pXOrganismAssay
UDP-glucuronosyltransferase 1A8EnzymesActivity— no normalized value— value does not convert to pXHomo sapiensCHEMBL1908085
UDP-glucuronosyltransferase 1A8EnzymesDrug metabolism— no normalized value— value does not convert to pXHomo sapiensCHEMBL3530642
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