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UGT1A1 (UDP-glucuronosyltransferase 1A1) is an enzyme. The public catalogues list it as a drug target and a biomarker, and an approved or late-stage drug is recorded against it.
UDP-glucuronosyltransferase (UGT) that catalyses 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 bile. Essential for the elimination and detoxification of drugs, xenobiotics and endogenous compounds. Catalyses the glucuronidation of endogenous oestrogen hormones such as estradiol, estrone and estriol.
CIViC holds 2 clinical evidence items and 0 assertions across 2 variants, naming Belinostat. In OnCo, 1 product record names it (Irinotecan (and liposomal irinotecan)).
In plain words · UGT1A1 (UDP-glucuronosyltransferase 1A1) is an enzyme. The public catalogues list it as a drug target and a biomarker, and an approved or late-stage drug is recorded against it.
UGT1A1 (UDP-glucuronosyltransferase 1A1) is an enzyme. The public catalogues list it as a drug target and a biomarker, and an approved or late-stage drug is recorded against it.
UDP-glucuronosyltransferase (UGT) that catalyses 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 bile.
1 product aims at UGT1A1: other agents. Inhibitors are shaped to fit the enzyme's active site so the reaction the cancer relies on stops.
Tumour-associated overexpression: HPA finds the RNA cancer enriched in cancer (Liver Hepatocellular Carcinoma (TCGA)) and group enriched in normal intestine, liver, so the tumour and the normal tissue it comes from share the target and the medicine relies on the difference in level. HPA UGT1A1: RNA group enriched (intestine 189 nTPM, liver 345 nTPM); blood lineage lineage enriched (granulocytes 1 nTPM); no normal tissue stained high. Distribution: no corpus cancer carries a prevalence row, threshold or catalogue link for it; Open Targets associates it with 0 specific cancer types at or above 0.5. (Rule 7 of scripts/fetch-target-specificity.ts.)
Sources: Human Protein Atlas UGT1A1 tissue; Human Protein Atlas UGT1A1 pathology; Open Targets ENSG00000241635 associations
First described 1991. Earliest sequence paper UniProt cites for the protein: Ritter J.K. et al, J. Biol. Chem, 1991, "Cloning of two human liver bilirubin UDP-glucuronosyltransferase cDNAs with expression in COS-1 cells". Source.
Sources: HGNC HGNC:12530 (approved symbol, name, aliases, locus and cross-references (hgnc_complete_set.txt)); UniProt P22309 (protein name, function text, keywords and locations (REST API)); CIViC gene UGT1A1 (2 evidence items, 0 assertions, 2 variants; diseases: Cancer (GraphQL API, CC0))
UDP-glucuronosyltransferase (UGT) that catalyses 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 bile. Essential for the elimination and detoxification of drugs, xenobiotics and endogenous compounds. Catalyses the glucuronidation of endogenous oestrogen hormones such as estradiol, estrone and estriol. Involved in the glucuronidation of bilirubin, a degradation product occurring in the normal catabolic pathway that breaks down heme in vertebrates. Involved in the glucuronidation of arachidonic acid (AA) and AA-derived eicosanoids including 15-HETE, 20-HETE, PGB1 and F2-isoprostane (8-iso-PGF2alpha). Involved in the glucuronidation of the phytochemical ferulic acid at the phenolic or the carboxylic acid group. Location: Endoplasmic reticulum membrane; Cytoplasm, perinuclear region (UniProt). Locus 2q37.1 (HGNC).
RNA: group enriched (intestine 189 nTPM, liver 345 nTPM), detected in some normal tissues. Blood: lineage enriched (granulocytes 1 nTPM).
No normal tissue stained high.
RNA cancer enriched: Liver Hepatocellular Carcinoma 168 pTPM.
No cancer sample stained medium or high.
Human Protein Atlas version 25.1, antibody staining at reliability approved, enhanced or supported; used under CC BY-SA 3.0. Staining counts are patients per level in the atlas cohort, not population prevalence.
All three of the active bowel cancer chemotherapy drugs given together instead of two. It shrinks more tumours than a doublet and is chosen when shrinking the tumour is what matters, usually with bevacizumab.
Query for this target: (TITLE:"UGT1A1" OR ABSTRACT:"UGT1A1" OR TITLE:"UDP glucuronosyltransferase family 1 member A1" OR ABSTRACT:"UDP glucuronosyltransferase family 1 member A1" OR TITLE:"UDP-glucuronosyltransferase 1A1" OR ABSTRACT:"UDP-glucuronosyltransferase 1A1" OR TITLE:"UGT1A" OR ABSTRACT:"UGT1A" OR TITLE:"UGT1" OR ABSTRACT:"UGT1" OR TITLE:"GNT1" OR ABSTRACT:"GNT1") AND (cancer OR tumor OR tumour OR oncology OR carcinoma OR lymphoma OR leukemia OR leukaemia OR myeloma OR sarcoma OR melanoma OR glioma). Results are unfiltered search hits about UGT1A1, not a curated reading list.
Shares High-dose FOLFIRI in Advanced Colorectal Cancer Patients With Wild-type UGT1A1*6 and *28, Combination Chemotherapy and Bevacizumab in Treating Patients With Metastatic Colorectal Cancer, G-CSF in Preventing Neutropenia During First-Line Treatment With Chemotherapy and Bevacizumab in Patients With Metastatic Colorectal Cancer, Irinotecan (and liposomal irinotecan).
Shares FOLFOXIRI (5-FU, leucovorin, oxaliplatin, irinotecan), CIViC.
Shares FOLFOXIRI (5-FU, leucovorin, oxaliplatin, irinotecan), Irinotecan (and liposomal irinotecan).