UDP glucuronosyltransferase family 1 member A1 | UDP glucuronosyltransferases (UGT) | IUPHAR/BPS Guide to PHARMACOLOGY

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UDP glucuronosyltransferase family 1 member A1

Target id: 2990

Nomenclature: UDP glucuronosyltransferase family 1 member A1

Family: UDP glucuronosyltransferases (UGT)

Annotation status:  image of a grey circle Awaiting annotation/under development. Please contact us if you can help with annotation.  » Email us

   GtoImmuPdb view: OFF :     Currently no data for UDP glucuronosyltransferase family 1 member A1 in GtoImmuPdb

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 1 533 2q37.1 UGT1A1 UDP glucuronosyltransferase family 1 member A1
Mouse 1 533 Chromosome 1, 44.55 cM Ugt1a1 UDP glucuronosyltransferase 1 family, polypeptide A1
Rat 1 533 95,295,701 - 95,302,822 Ugt1a1 UDP glucuronosyltransferase family 1 member A1
Gene and Protein Information Comments
The UGT1A1 gene is part of a complex locus that encodes several UDP-glucuronosyltransferases. The locus includes thirteen unique alternate first exons followed by four common exons. Four of the alternate first exons are considered pseudogenes. Each of the remaining nine 5' exons may be spliced to the four common exons, resulting in nine proteins with different N-termini and identical C-termini. Each first exon encodes the substrate binding site, and is regulated by its own promoter. Over 100 genetic variants within the UGT1A1 gene have been described, some of which confer increased, reduced or inactive enzymatic activity. The UGT nomenclature committee has compiled a list of these variants, naming each with a * symbol followed by a number. Many exogenous substances, mutagenic xenobiotics and therapeutic drugs are UGT1A1 substrates.
Database Links
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Gene
OMIM
RefSeq Protein
UniProtKB
Wikipedia

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Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
ritonavir Hs Inhibition 5.8 pIC50 1
pIC50 5.8 (IC50 1.7x10-6 M) Both inhibitor and substrate [1]

References

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1. Zhou J, Tracy TS, Remmel RP. (2011) Correlation between bilirubin glucuronidation and estradiol-3-gluronidation in the presence of model UDP-glucuronosyltransferase 1A1 substrates/inhibitors. Drug Metab. Dispos., 39 (2): 322-9. [PMID:21030469]

How to cite this page

UDP glucuronosyltransferases (UGT): UDP glucuronosyltransferase family 1 member A1. Last modified on 05/03/2018. Accessed on 13/12/2018. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2990.