Details of the Target

General Information of Target

Target ID LDTP01017
Target Name UDP-glucuronosyltransferase 1A9 (UGT1A9)
Gene Name UGT1A9
Gene ID 54600
Synonyms
GNT1; UGT1; UDP-glucuronosyltransferase 1A9; UGT1A9; EC 2.4.1.17; UDP-glucuronosyltransferase 1-9; UDPGT 1-9; UGT1*9; UGT1-09; UGT1.9; UDP-glucuronosyltransferase 1-I; UGT-1I; UGT1I; lugP4
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MACTGWTSPLPLCVCLLLTCGFAEAGKLLVVPMDGSHWFTMRSVVEKLILRGHEVVVVMP
EVSWQLGRSLNCTVKTYSTSYTLEDLDREFKAFAHAQWKAQVRSIYSLLMGSYNDIFDLF
FSNCRSLFKDKKLVEYLKESSFDAVFLDPFDNCGLIVAKYFSLPSVVFARGILCHYLEEG
AQCPAPLSYVPRILLGFSDAMTFKERVRNHIMHLEEHLLCHRFFKNALEIASEILQTPVT
EYDLYSHTSIWLLRTDFVLDYPKPVMPNMIFIGGINCHQGKPLPMEFEAYINASGEHGIV
VFSLGSMVSEIPEKKAMAIADALGKIPQTVLWRYTGTRPSNLANNTILVKWLPQNDLLGH
PMTRAFITHAGSHGVYESICNGVPMVMMPLFGDQMDNAKRMETKGAGVTLNVLEMTSEDL
ENALKAVINDKSYKENIMRLSSLHKDRPVEPLDLAVFWVEFVMRHKGAPHLRPAAHDLTW
YQYHSLDVIGFLLAVVLTVAFITFKCCAYGYRKCLGKKGRVKKAHKSKTH
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 hormones such as estradiol and estrone. 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
O60656
Ensemble ID
ENST00000354728.5
HGNC ID
HGNC:12541
ChEMBL ID
CHEMBL1743319

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
COLO792 SNV: p.M41I .
JHH7 SNV: p.H210Q .
JURKAT Deletion: p.S122QfsTer12 .
MOLT4 Deletion: p.S122QfsTer12 .
OVK18 SNV: p.S8I .
U937 SNV: p.H217N .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 1 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
IA-alkyne
 Probe Info  		N.A.  LDD0162  [1]

The Interaction Atlas With This Target

The Drug(s) Related To This Target

Approved
Click To Hide/Show 71 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Acetaminophen Small molecular drug DB00316
Ambrisentan Small molecular drug DB06403
Apomorphine Small molecular drug DB00714
Artesunate Small molecular drug DB09274
Cabotegravir Small molecular drug DB11751
Canagliflozin Small molecular drug DB08907
Cannabidiol Small molecular drug DB09061
Dabigatran Etexilate Small molecular drug DB06695
Dapagliflozin Small molecular drug DB06292
Dexibuprofen Small molecular drug DB09213
Diclofenac Small molecular drug DB00586
Diflunisal Small molecular drug DB00861
Dolutegravir Small molecular drug DB08930
Dronabinol Small molecular drug DB00470
Eltrombopag Small molecular drug DB06210
Empagliflozin Small molecular drug DB09038
Entacapone Small molecular drug DB00494
Ertugliflozin Small molecular drug DB11827
Estradiol Small molecular drug DB00783
Ethinylestradiol Small molecular drug DB00977
Etodolac Small molecular drug DB00749
Ezogabine Small molecular drug DB04953
Febuxostat Small molecular drug DB04854
Fenofibrate Small molecular drug DB01039
Flurbiprofen Small molecular drug DB00712
Formoterol Small molecular drug DB00983
Fosphenytoin Small molecular drug DB01320
Fostamatinib Small molecular drug DB12010
Fostemsavir Small molecular drug DB11796
Gemfibrozil Small molecular drug DB01241
Glasdegib Small molecular drug DB11978
Haloperidol Small molecular drug DB00502
Ibrexafungerp Small molecular drug DB12471
Ibuprofen Small molecular drug DB01050
Indomethacin Small molecular drug DB00328
Irinotecan Small molecular drug DB00762
Isavuconazole Small molecular drug DB11633
Labetalol Small molecular drug DB00598
Lamotrigine Small molecular drug DB00555
Lumiracoxib Small molecular drug DB01283
Mefenamic Acid Small molecular drug DB00784
Mycophenolate Mofetil Small molecular drug DB00688
Mycophenolic Acid Small molecular drug DB01024
Naproxen Small molecular drug DB00788
Nateglinide Small molecular drug DB00731
Oxymetazoline Small molecular drug DB00935
Phenolphthalein Small molecular drug DB04824
Phenytoin Small molecular drug DB00252
Pindolol Small molecular drug DB00960
Primidone Small molecular drug DB00794
Propofol Small molecular drug DB00818
Regorafenib Small molecular drug DB08896
Rifampicin Small molecular drug DB01045
Ritonavir Small molecular drug DB00503
Roxadustat Small molecular drug DB04847
Sorafenib Small molecular drug DB00398
Sotagliflozin Small molecular drug DB12713
Tapentadol Small molecular drug DB06204
Terbutaline Small molecular drug DB00871
Troglitazone Small molecular drug DB00197
Valdecoxib Small molecular drug DB00580
Valproic Acid Small molecular drug DB00313
Vericiguat Small molecular drug DB15456
Zileuton Small molecular drug DB00744
Artenimol . DB11638
Belumosudil . DB16703
Darolutamide . DB12941
Deucravacitinib . DB16650
Enasidenib . DB13874
Methylene Blue . DB09241
Viloxazine . DB09185
Investigative
Click To Hide/Show 8 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Ketobemidone Small molecular drug DB06738
Morniflumate Small molecular drug DB09285
Niflumic Acid Small molecular drug DB04552
Seratrodast Small molecular drug DB06739
Topiroxostat Small molecular drug DB01685
Curcumin Sulfate . DB14635
Medical Cannabis . DB14009
Propacetamol . DB09288

References

1 SP3-FAIMS Chemoproteomics for High-Coverage Profiling of the Human Cysteinome*. Chembiochem. 2021 May 14;22(10):1841-1851. doi: 10.1002/cbic.202000870. Epub 2021 Feb 18.
Mass spectrometry data entry: PXD023056 , PXD023059 , PXD023058 , PXD023057 , PXD023060