Details of the Target

General Information of Target

Target ID LDTP03164
Target Name UDP-glucuronosyltransferase 1A1 (UGT1A1)
Gene Name UGT1A1
Gene ID 54658
Synonyms
GNT1; UGT1; UDP-glucuronosyltransferase 1A1; UGT1A1; EC 2.4.1.17; Bilirubin-specific UDPGT isozyme 1; hUG-BR1; UDP-glucuronosyltransferase 1-1; UDPGT 1-1; UGT1*1; UGT1-01; UGT1.1; UDP-glucuronosyltransferase 1A isoform 1
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MAVESQGGRPLVLGLLLCVLGPVVSHAGKILLIPVDGSHWLSMLGAIQQLQQRGHEIVVL
APDASLYIRDGAFYTLKTYPVPFQREDVKESFVSLGHNVFENDSFLQRVIKTYKKIKKDS
AMLLSGCSHLLHNKELMASLAESSFDVMLTDPFLPCSPIVAQYLSLPTVFFLHALPCSLE
FEATQCPNPFSYVPRPLSSHSDHMTFLQRVKNMLIAFSQNFLCDVVYSPYATLASEFLQR
EVTVQDLLSSASVWLFRSDFVKDYPRPIMPNMVFVGGINCLHQNPLSQEFEAYINASGEH
GIVVFSLGSMVSEIPEKKAMAIADALGKIPQTVLWRYTGTRPSNLANNTILVKWLPQNDL
LGHPMTRAFITHAGSHGVYESICNGVPMVMMPLFGDQMDNAKRMETKGAGVTLNVLEMTS
EDLENALKAVINDKSYKENIMRLSSLHKDRPVEPLDLAVFWVEFVMRHKGAPHLRPAAHD
LTWYQYHSLDVIGFLLAVVLTVAFITFKCCAYGYRKCLGKKGRVKKAHKSKTH
Target Type
Clinical trial
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. Involved in the glucuronidation of bilirubin, a degradation product occurring in the normal catabolic pathway that breaks down heme in vertebrates. Also catalyzes the glucuronidation 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, 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.; [Isoform 2]: Lacks UGT glucuronidation activity but acts as a negative regulator of isoform 1.
TTD ID
T93480
Uniprot ID
P22309
DrugMap ID
TT34ZAF
Ensemble ID
ENST00000305208.10
HGNC ID
HGNC:12530
ChEMBL ID
CHEMBL1287617

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
CAL72 SNV: p.H55Y .
LS180 SNV: p.V226I .
MEWO SNV: p.L238F .
TE4 SNV: p.G28V .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 2 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
DBIA
 Probe Info  		C127(1.35)  LDD2379  [1]
Acrolein
 Probe Info  		N.A.  LDD0221  [2]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0107  IAA HeLa N.A.  LDD0221  [2]
 LDCM0022  KB02 ICC10 C127(1.35)  LDD2379  [1]
 LDCM0023  KB03 ICC10 C127(1.45)  LDD2796  [1]
 LDCM0024  KB05 ICC106 C127(1.59)  LDD3214  [1]
 LDCM0109  NEM HeLa N.A.  LDD0224  [2]

The Interaction Atlas With This Target

The Drug(s) Related To This Target

Approved
Click To Hide/Show 119 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Abacavir Small molecular drug DB01048
Acetaminophen Small molecular drug DB00316
Adenine Small molecular drug DB00173
Apomorphine Small molecular drug DB00714
Asciminib Small molecular drug DB12597
Atazanavir Small molecular drug DB01072
Atorvastatin Small molecular drug DB01076
Axitinib Small molecular drug DB06626
Binimetinib Small molecular drug DB11967
Cabotegravir Small molecular drug DB11751
Carbamazepine Small molecular drug DB00564
Carvedilol Small molecular drug DB01136
Cerivastatin Small molecular drug DB00439
Dabrafenib Small molecular drug DB08912
Dacomitinib Small molecular drug DB11963
Dasabuvir Small molecular drug DB09183
Delafloxacin Small molecular drug DB11943
Desogestrel Small molecular drug DB00304
Dexibuprofen Small molecular drug DB09213
Dolutegravir Small molecular drug DB08930
Dronabinol Small molecular drug DB00470
Efavirenz Small molecular drug DB00625
Eltrombopag Small molecular drug DB06210
Elvitegravir Small molecular drug DB09101
Erlotinib Small molecular drug DB00530
Ertugliflozin Small molecular drug DB11827
Eslicarbazepine Small molecular drug DB14575
Eslicarbazepine Acetate Small molecular drug DB09119
Estradiol Small molecular drug DB00783
Estradiol Acetate Small molecular drug DB13952
Estradiol Cypionate Small molecular drug DB13954
Estradiol Valerate Small molecular drug DB13956
Ethinylestradiol Small molecular drug DB00977
Etoposide Small molecular drug DB00773
Ezetimibe Small molecular drug DB00973
Ezogabine Small molecular drug DB04953
Febuxostat Small molecular drug DB04854
Flurbiprofen Small molecular drug DB00712
Fluvastatin Small molecular drug DB01095
Fostamatinib Small molecular drug DB12010
Fostemsavir Small molecular drug DB11796
Fulvestrant Small molecular drug DB00947
Furosemide Small molecular drug DB00695
Fusidic Acid Small molecular drug DB02703
Gemfibrozil Small molecular drug DB01241
Glecaprevir Small molecular drug DB13879
Glipizide Small molecular drug DB01067
Ibrexafungerp Small molecular drug DB12471
Indacaterol Small molecular drug DB05039
Indinavir Small molecular drug DB00224
Indomethacin Small molecular drug DB00328
Irinotecan Small molecular drug DB00762
Ketoconazole Small molecular drug DB01026
Ketoprofen Small molecular drug DB01009
Labetalol Small molecular drug DB00598
Lamotrigine Small molecular drug DB00555
Levothyroxine Small molecular drug DB00451
Liothyronine Small molecular drug DB00279
Loratadine Small molecular drug DB00455
Losartan Small molecular drug DB00678
Lovastatin Small molecular drug DB00227
Lumateperone Small molecular drug DB06077
Metronidazole Small molecular drug DB00916
Migalastat Small molecular drug DB05018
Minoxidil Small molecular drug DB00350
Morphine Small molecular drug DB00295
Mycophenolate Mofetil Small molecular drug DB00688
Mycophenolic Acid Small molecular drug DB01024
Naloxone Small molecular drug DB01183
Naltrexone Small molecular drug DB00704
Nandrolone Decanoate Small molecular drug DB08804
Nelfinavir Small molecular drug DB00220
Nilotinib Small molecular drug DB04868
Nintedanib Small molecular drug DB09079
Norgestimate Small molecular drug DB00957
Olaparib Small molecular drug DB09074
Ombitasvir Small molecular drug DB09296
Paritaprevir Small molecular drug DB09297
Pazopanib Small molecular drug DB06589
Phenobarbital Small molecular drug DB01174
Phenytoin Small molecular drug DB00252
Pibrentasvir Small molecular drug DB13878
Pindolol Small molecular drug DB00960
Ponesimod Small molecular drug DB12016
Primidone Small molecular drug DB00794
Probenecid Small molecular drug DB01032
Propofol Small molecular drug DB00818
Raloxifene Small molecular drug DB00481
Raltegravir Small molecular drug DB06817
Regorafenib Small molecular drug DB08896
Rifampicin Small molecular drug DB01045
Ritonavir Small molecular drug DB00503
Rucaparib Small molecular drug DB12332
Selumetinib Small molecular drug DB11689
Simvastatin Small molecular drug DB00641
Sorafenib Small molecular drug DB00398
Sotagliflozin Small molecular drug DB12713
Suprofen Small molecular drug DB00870
Terbutaline Small molecular drug DB00871
Testosterone Propionate Small molecular drug DB01420
Tiagabine Small molecular drug DB00906
Tipranavir Small molecular drug DB00932
Tramadol Small molecular drug DB00193
Troglitazone Small molecular drug DB00197
Ubrogepant Small molecular drug DB15328
Valproic Acid Small molecular drug DB00313
Vericiguat Small molecular drug DB15456
Zidovudine Small molecular drug DB00495
Zonisamide Small molecular drug DB00909
Belumosudil . DB16703
Bictegravir . DB11799
Enasidenib . DB13874
Estradiol Benzoate . DB13953
Estradiol Dienanthate . DB13955
Letermovir . DB12070
Mitapivat . DB16236
Pexidartinib . DB12978
Sacituzumab Govitecan . DB12893
Tecovirimat . DB12020
Phase 2
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
At-342 Gene therapy D84EGX
Investigative
Click To Hide/Show 5 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Alvocidib Small molecular drug DB03496
Muraglitazar Small molecular drug DB06510
Curcumin Sulfate . DB14635
Lenacapavir . DB15673
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 ACR-Based Probe for the Quantitative Profiling of Histidine Reactivity in the Human Proteome. J Am Chem Soc. 2023 Mar 8;145(9):5252-5260. doi: 10.1021/jacs.2c12653. Epub 2023 Feb 27.