Details of the Target

General Information of Target

Target ID LDTP03752
Target Name UDP-glucuronosyltransferase 1A5 (UGT1A5)
Gene Name UGT1A5
Gene ID 54579
Synonyms
GNT1; UGT1; UDP-glucuronosyltransferase 1A5; UGT1A5; EC 2.4.1.17; UDP-glucuronosyltransferase 1-5; UDPGT 1-5; UGT1*5; UGT1-05; UGT1.5; UDP-glucuronosyltransferase 1-E; UGT-1E; UGT1E
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MATGLQVPLPQLATGLLLLLSVQPWAESGKVLVVPTDGSHWLSMREALRDLHARGHQVVV
LTLEVNMYIKEENFFTLTTYAISWTQDEFDRLLLGHTQSFFETEHLLMKFSRRMAIMNNM
SLIIHRSCVELLHNEALIRHLHATSFDVVLTDPFHLCAAVLAKYLSIPAVFFLRNIPCDL
DFKGTQCPNPSSYIPRLLTTNSDHMTFLQRVKNMLYPLALSYLCHAVSAPYASLASELFQ
REVSVVDLVSHASVWLFRGDFVMDYPRPIMPNMVFIGGINCANGKPLSQEFEAYINASGE
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 the AGTR1 angiotensin receptor antagonist zolarsatan, a drug 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
P35504
Ensemble ID
ENST00000373414.4
HGNC ID
HGNC:12537
ChEMBL ID
CHEMBL4523985

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(1.34)  LDD3489  [1]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0022  KB02 ICC10 C187(1.32); C128(1.12)  LDD2379  [1]
 LDCM0023  KB03 ICC13-7 C187(2.91); C178(3.94); C128(1.77)  LDD2801  [1]
 LDCM0024  KB05 WM1552C C178(1.34)  LDD3489  [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