Details of the Target

General Information of Target

Target ID LDTP12148
Target Name UDP-glucuronosyltransferase 1A10 (UGT1A10)
Gene Name UGT1A10
Gene ID 54575
Synonyms
GNT1; UGT1; UDP-glucuronosyltransferase 1A10; UGT1A10; EC 2.4.1.17; UDP-glucuronosyltransferase 1-10; UDPGT 1-10; UGT1*10; UGT1-10; UGT1.10; UDP-glucuronosyltransferase 1-J; UGT-1J; UGT1J
3D Structure
Download
2D Sequence (FASTA)
Download
3D Structure (PDB)
Download
Sequence
MARAGWTGLLPLYVCLLLTCGFAKAGKLLVVPMDGSHWFTMQSVVEKLILRGHEVVVVMP
EVSWQLGRSLNCTVKTYSTSYTLEDQDREFMVFADARWTAPLRSAFSLLTSSSNGIFDLF
FSNCRSLFNDRKLVEYLKESCFDAVFLDPFDACGLIVAKYFSLPSVVFARGIFCHYLEEG
AQCPAPLSYVPRLLLGFSDAMTFKERVWNHIMHLEEHLFCPYFFKNVLEIASEILQTPVT
AYDLYSHTSIWLLRTDFVLEYPKPVMPNMIFIGGINCHQGKPVPMEFEAYINASGEHGIV
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, estrone and estriol. 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 losartan, caderastan and zolarsatan, drugs which can inhibit the effect of angiotensin II.; [Isoform 2]: Lacks UGT glucuronidation activity but acts as a negative regulator of isoform 1.
Uniprot ID
Q9HAW8
Ensemble ID
ENST00000344644.10
HGNC ID
HGNC:12531
ChEMBL ID
CHEMBL1743320

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
CHL1 SNV: p.G171R .
DU145 Substitution: p.G5L .
Ishikawa (Heraklio) 02 ER SNV: p.Q103Ter .
LN229 SNV: p.G273R .
PATU8988T SNV: p.W251R .
RVH421 SNV: p.M91I .

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
DBIA
 Probe Info  		C153(1.51)  LDD3440  [1]
PAL-AfBPP Probe
Click To Hide/Show 1 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
DFG-out-3
 Probe Info  		4.00  LDD0074  [2]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0022  KB02 BxPC-3 C153(1.84)  LDD2280  [1]
 LDCM0023  KB03 BxPC-3 C153(2.77)  LDD2697  [1]
 LDCM0024  KB05 SNU-245 C153(1.51)  LDD3440  [1]
 LDCM0016  Ranjitkar_cp1 A431 4.00  LDD0074  [2]

The Interaction Atlas With This Target

The Drug(s) Related To This Target

Approved
Click To Hide/Show 22 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Apomorphine Small molecular drug DB00714
Bazedoxifene Small molecular drug DB06401
Dronabinol Small molecular drug DB00470
Estradiol Small molecular drug DB00783
Etodolac Small molecular drug DB00749
Fostemsavir Small molecular drug DB11796
Ibrexafungerp Small molecular drug DB12471
Lamotrigine Small molecular drug DB00555
Losartan Small molecular drug DB00678
Mycophenolate Mofetil Small molecular drug DB00688
Mycophenolic Acid Small molecular drug DB01024
Nandrolone Decanoate Small molecular drug DB08804
Naproxen Small molecular drug DB00788
Nintedanib Small molecular drug DB09079
Pindolol Small molecular drug DB00960
Primidone Small molecular drug DB00794
Raloxifene Small molecular drug DB00481
Ritonavir Small molecular drug DB00503
Tamoxifen Small molecular drug DB00675
Terbutaline Small molecular drug DB00871
Troglitazone Small molecular drug DB00197
Valproic Acid Small molecular drug DB00313
Investigative
Click To Hide/Show 3 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Curcumin Sulfate . DB14635
Medical Cannabis . DB14009
Propacetamol . DB09288

References

1 DrugMap: A quantitative pan-cancer analysis of cysteine ligandability. Cell. 2024 May 9;187(10):2536-2556.e30. doi: 10.1016/j.cell.2024.03.027. Epub 2024 Apr 22.
Mass spectrometry data entry: PXD047840
2 Affinity-based probes based on type II kinase inhibitors. J Am Chem Soc. 2012 Nov 21;134(46):19017-25. doi: 10.1021/ja306035v. Epub 2012 Nov 6.