Details of the Target

General Information of Target

Target ID LDTP12147
Target Name UDP-glucuronosyltransferase 1A7 (UGT1A7)
Gene Name UGT1A7
Gene ID 54577
Synonyms
GNT1; UGT1; UDP-glucuronosyltransferase 1A7; UGT1A7; EC 2.4.1.17; UDP-glucuronosyltransferase 1-7; UDPGT 1-7; UGT1*7; UGT1-07; UGT1.7; UDP-glucuronosyltransferase 1-G; UGT-1G; UGT1G
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MTGEVGSEVHLEINDPNVISQEEADSPSDSGQGSYETIGPLSEGDSDEEIFVSKKLKNRK
VLQDSDSETEDTNASPEKTTYDSAEEENKENLYAGKNTKIKRIYKTVADSDESYMEKSLY
QENLEAQVKPCLELSLQSGNSTDFTTDRKSSKKHIHDKEGTAGKAKVKSKRRLEKEERKM
EKIRQLKKKETKNQEDDVEQPFNDSGCLLVDKDLFETGLEDENNSPLEDEESLESIRAAV
KNKVKKHKKKEPSLESGVHSFEEGSELSKGTTRKERKAARLSKEALKQLHSETQRLIRES
ALNLPYHMPENKTIHDFFKRKPRPTCHGNAMALLKSSKYQSSHHKEIIDTANTTEMNSDH
HSKGSEQTTGAENEVETNALPVVSKETQIITGSDESCRKDLVKNEELEIQEKQKQSDIRP
SPGDSSVLQQESNFLGNNHSEECQVGGLVAFEPHALEGEGPQNPEETDEKVEEPEQQNKS
SAVGPPEKVRRFTLDRLKQLGVDVSIKPRLGADEDSFVILEPETNRELEALKQRFWKHAN
PAAKPRAGQTVNVNVIVKDMGTDGKEELKADVVPVTLAPKKLDGASHTKPGEKLQVLKAK
LQEAMKLRRFEERQKRQALFKLDNEDGFEEEEEEEEEMTDESEEDGEEKVEKEEKEEELE
EEEEKEEEEEEEGNQETAEFLLSSEEIETKDEKEMDKENNDGSSEIGKAVGFLSVPKSLS
SDSTLLLFKDSSSKMGYFPTEEKSETDENSGKQPSKLDEDDSCSLLTKESSHNSSFELIG
STIPSYQPCNRQTGRGTSFFPTAGGFRSPSPGLFRASLVSSASKSSGKLSEPSLPIEDSQ
DLYNASPEPKTLFLGAGDFQFCLEDDTQSQLLDADGFLNVRNHRNQYQALKPRLPLASMD
ENAMDANMDELLDLCTGKFTSQAEKHLPRKSDKKENMEELLNLCSGKFTSQDASTPASSE
LNKQEKESSMGDPMEEALALCSGSFPTDKEEEDEEEEFGDFRLVSNDNEFDSDEDEHSDS
GNDLALEDHEDDDEEELLKRSEKLKRQMRLRKYLEDEAEVSGSDVGSEDEYDGEEIDEYE
EDVIDEVLPSDEELQSQIKKIHMKTMLDDDKRQLRLYQERYLADGDLHSDGPGRMRKFRW
KNIDDASQMDLFHRDSDDDQTEEQLDESEARWRKERIEREQWLRDMAQQGKITAEEEEEI
GEDSQFMILAKKVTAKALQKNASRPMVIQESKSLLRNPFEAIRPGSAQQVKTGSLLNQPK
AVLQKLAALSDHNPSAPRNSRNFVFHTLSPVKAEAAKESSKSQVKKRGPSFMTSPSPKHL
KTDDSTSGLTRSIFKYLES
Target Bioclass
Enzyme
Family
UDP-glycosyltransferase family
Subcellular location
Endoplasmic reticulum membrane
Function
[Isoform 1]: 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 bile. Essential for the elimination and detoxification of drugs, xenobiotics and endogenous compounds. Catalyzes the glucuronidation of endogenous estrogen hormone epiestradiol. Also catalyzes the glucuronidation of the isoflavones genistein, daidzein, glycitein, formononetin, biochanin A and prunetin, which are phytoestrogens with anticancer and cardiovascular properties. Involved in the glucuronidation of the AGTR1 angiotensin receptor antagonist caderastan, a drug which can inhibit the effect of angiotensin II. Involved in the biotransformation of 7-ethyl-10-hydroxycamptothecin (SN-38), the pharmacologically active metabolite of the anticancer drug irinotecan. Also metabolizes mycophenolate, an immunosuppressive agent.; [Isoform 2]: Lacks UGT glucuronidation activity but acts as a negative regulator of isoform 1.
Uniprot ID
Q9HAW7
Ensemble ID
ENST00000373426.4
HGNC ID
HGNC:12539
ChEMBL ID
CHEMBL1743317

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
CAL27 Substitution: p.N129R .
HEC1B SNV: p.V57I .
IGR37 Substitution: p.N129R .
IGR39 Substitution: p.N129R .
MCC13 SNV: p.R68S .
NALM6 SNV: p.V57I .
NCIH2286 SNV: p.V14L .
RH30 SNV: p.Y222C .
SHP77 Substitution: p.N129R .

Probe(s) Labeling This Target

PAL-AfBPP Probe
Click To Hide/Show 1 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
A-DA
 Probe Info  		2.11  LDD0142  [1]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0082  FK866 A-549 2.11  LDD0142  [1]
 LDCM0084  Ro 48-8071 A-549 3.99  LDD0145  [1]

The Interaction Atlas With This Target

The Drug(s) Related To This Target

Approved
Click To Hide/Show 17 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Apomorphine Small molecular drug DB00714
Cannabidiol Small molecular drug DB09061
Carbamazepine Small molecular drug DB00564
Estradiol Small molecular drug DB00783
Fostemsavir Small molecular drug DB11796
Ibrexafungerp Small molecular drug DB12471
Ketoconazole Small molecular drug DB01026
Lamotrigine Small molecular drug DB00555
Mycophenolate Mofetil Small molecular drug DB00688
Mycophenolic Acid Small molecular drug DB01024
Naproxen Small molecular drug DB00788
Nintedanib Small molecular drug DB09079
Pindolol Small molecular drug DB00960
Primidone Small molecular drug DB00794
Ritonavir Small molecular drug DB00503
Terbutaline Small molecular drug DB00871
Troglitazone Small molecular drug DB00197
Investigative
Click To Hide/Show 2 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Curcumin Sulfate . DB14635
Medical Cannabis . DB14009

References

1 A Global Map of Lipid-Binding Proteins and Their Ligandability in Cells. Cell. 2015 Jun 18;161(7):1668-80. doi: 10.1016/j.cell.2015.05.045.