UGT1A1
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.
Overview
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)).
- Target · the protein and the cell it sits on
- Drug · antibody, small molecule, cell or radioligand
- Effect · signal, damage or kill
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.
- 1 · What it is
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.
- 2 · What goes wrong in cancer
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.
- 3 · How drugs use it
No product in this corpus aims at UGT1A1 yet. Inhibitors are shaped to fit the enzyme's active site so the reaction the cancer relies on stops.
External identifiers
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))
Biology
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).
Notes
top- Written by scripts/fetch-cancer-genes.ts from CIViC, Open Targets, IntOGen, HGNC and UniProt; the function text is UniProt's, condensed and in UK spelling. Roles: CIViC lists 1 therapies; CIViC holds 2 clinical evidence items on its variants. Evidence tier "approved-drug" is the strongest of those signals.
- Prevalence not recorded: none of the sources gives a positivity rate.
Latest papers
topQuery 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.
Similar pages
not linked directly; found by shared links- TechnologyUGT1A1 genotyping before irinotecan
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).
- TreatmentLeucovorin (folinic acid)
Shares 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.