Details of the Target

General Information of Target

Target ID LDTP03165
Target Name UDP-glucuronosyltransferase 1A4 (UGT1A4)
Gene Name UGT1A4
Gene ID 54657
Synonyms
GNT1; UGT1; UDP-glucuronosyltransferase 1A4; UGT1A4; EC 2.4.1.17; Bilirubin-specific UDPGT isozyme 2; hUG-BR2; UDP-glucuronosyltransferase 1-4; UDPGT 1-4; UGT1*4; UGT1-04; UGT1.4; UDP-glucuronosyltransferase 1-D; UGT-1D; UGT1D
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MARGLQVPLPRLATGLLLLLSVQPWAESGKVLVVPTDGSPWLSMREALRELHARGHQAVV
LTPEVNMHIKEEKFFTLTAYAVPWTQKEFDRVTLGYTQGFFETEHLLKRYSRSMAIMNNV
SLALHRCCVELLHNEALIRHLNATSFDVVLTDPVNLCGAVLAKYLSIPAVFFWRYIPCDL
DFKGTQCPNPSSYIPKLLTTNSDHMTFLQRVKNMLYPLALSYICHTFSAPYASLASELFQ
REVSVVDLVSYASVWLFRGDFVMDYPRPIMPNMVFIGGINCANGKPLSQEFEAYINASGE
HGIVVFSLGSMVSEIPEKKAMAIADALGKIPQTVLWRYTGTRPSNLANNTILVKWLPQND
LLGHPMTRAFITHAGSHGVYESICNGVPMVMMPLFGDQMDNAKRMETKGAGVTLNVLEMT
SEDLENALKAVINDKSYKENIMRLSSLHKDRPVEPLDLAVFWVEFVMRHKGAPHLRPAAH
DLTWYQYHSLDVIGFLLAVVLTVAFITFKCCAYGYRKCLGKKGRVKKAHKSKTH
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. Involved in the glucuronidation of calcidiol, which is the major circulating form of vitamin D3 essential for the regulation of calcium and phosphate homeostasis. Also glucuronidates the biologically active form of vitamin D3, calcitriol, probably leading to its biliary transport and intestinal reabsorption.; [Isoform 2]: Lacks UDP-glucuronosyltransferase (UGT) activity but acts as a negative regulator of isoform 1.
Uniprot ID
P22310
Ensemble ID
ENST00000373409.8
HGNC ID
HGNC:12536
ChEMBL ID
CHEMBL3619

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
22RV1 SNV: p.A115T .
FADU SNV: p.E64D .
HCC1187 SNV: p.S446I .
HEP3B217 SNV: p.I315V .
IGR1 SNV: p.I351L .
Ishikawa (Heraklio) 02 ER Deletion: p.R524EfsTer22 .
LUDLU1 Insertion: p.V503SfsTer7 .
MOLT4 Deletion: p.R524EfsTer22 .
NCIH1944 SNV: p.A498S .
RL952 Deletion: p.R524EfsTer22 .
SKMEL30 SNV: p.K429N .
U937 SNV: p.Q23K .

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  		C178(0.95)  LDD2379  [1]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0022  KB02 ICC10 C178(0.95)  LDD2379  [1]
 LDCM0023  KB03 ICC13-7 C178(4.60)  LDD2801  [1]
 LDCM0024  KB05 ICC106 C178(1.04)  LDD3214  [1]

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