Details of the Target

General Information of Target

Target ID LDTP13672
Target Name Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2)
Gene Name ABCG2
Gene ID 9429
Synonyms
ABCP; BCRP; BCRP1; MXR; Broad substrate specificity ATP-binding cassette transporter ABCG2; EC 7.6.2.2; ATP-binding cassette sub-family G member 2; Breast cancer resistance protein; CDw338; Mitoxantrone resistance-associated protein; Placenta-specific ATP-binding cassette transporter; Urate exporter; CD antigen CD338
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MATTKRVLYVGGLAEEVDDKVLHAAFIPFGDITDIQIPLDYETEKHRGFAFVEFELAEDA
AAAIDNMNESELFGRTIRVNLAKPMRIKEGSSRPVWSDDDWLKKFSGKTLEENKEEEGSE
PPKAETQEGEPIAKKARSNPQVYMDIKIGNKPAGRIQMLLRSDVVPMTAENFRCLCTHEK
GFGFKGSSFHRIIPQFMCQGGDFTNHNGTGGKSIYGKKFDDENFILKHTGPGLLSMANSG
PNTNGSQFFLTCDKTDWLDGKHVVFGEVTEGLDVLRQIEAQGSKDGKPKQKVIIADCGEY
V
Target Type
Successful
Target Bioclass
Enzyme
Family
ABC transporter superfamily, ABCG family, Eye pigment precursor importer (TC 3.A.1.204) subfamily
Subcellular location
Cell membrane
Function
Broad substrate specificity ATP-dependent transporter of the ATP-binding cassette (ABC) family that actively extrudes a wide variety of physiological compounds, dietary toxins and xenobiotics from cells. Involved in porphyrin homeostasis, mediating the export of protoporphyrin IX (PPIX) from both mitochondria to cytosol and cytosol to extracellular space, it also functions in the cellular export of heme. Also mediates the efflux of sphingosine-1-P from cells. Acts as a urate exporter functioning in both renal and extrarenal urate excretion. In kidney, it also functions as a physiological exporter of the uremic toxin indoxyl sulfate. Also involved in the excretion of steroids like estrone 3-sulfate/E1S, 3beta-sulfooxy-androst-5-en-17-one/DHEAS, and other sulfate conjugates. Mediates the secretion of the riboflavin and biotin vitamins into milk. Extrudes pheophorbide a, a phototoxic porphyrin catabolite of chlorophyll, reducing its bioavailability. Plays an important role in the exclusion of xenobiotics from the brain (Probable). It confers to cells a resistance to multiple drugs and other xenobiotics including mitoxantrone, pheophorbide, camptothecin, methotrexate, azidothymidine, and the anthracyclines daunorubicin and doxorubicin, through the control of their efflux. In placenta, it limits the penetration of drugs from the maternal plasma into the fetus. May play a role in early stem cell self-renewal by blocking differentiation.
TTD ID
T56556
Uniprot ID
Q9UNQ0
DrugMap ID
TTIMJ02
Ensemble ID
ENST00000237612.8
HGNC ID
HGNC:74
ChEMBL ID
CHEMBL5393

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
CAL148 SNV: p.S2F .
HUH1 Deletion: p.F506SfsTer4 .
MEWO SNV: p.G197E .
SBC5 SNV: p.R163K .
TGBC52TKB SNV: p.V178I .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 6 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
STPyne
 Probe Info  		K157(5.00)  LDD0277  [1]
DBIA
 Probe Info  		C119(2.24)  LDD2370  [2]
BTD
 Probe Info  		C55(0.54)  LDD2127  [3]
WYneO
 Probe Info  		N.A.  LDD0022  [4]
IPM
 Probe Info  		C119(0.00); C43(0.00); C55(0.00)  LDD0147  [5]
TFBX
 Probe Info  		C374(0.00); C55(0.00)  LDD0148  [5]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0022  KB02 HT-1376 C119(2.24)  LDD2370  [2]
 LDCM0023  KB03 HT-1376 C119(1.22)  LDD2787  [2]
 LDCM0024  KB05 HT-1376 C119(1.29)  LDD3204  [2]
 LDCM0534  Nucleophilic fragment 30a MDA-MB-231 C55(0.54)  LDD2127  [3]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2) ABCG family Q9UNQ0
Other
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Polyubiquitin-C (UBC) Ubiquitin family P0CG48

The Drug(s) Related To This Target

Approved
Click To Hide/Show 210 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Cyclosporine Protein/peptide DB00091
Abemaciclib Small molecular drug DB12001
Afatinib Small molecular drug DB08916
Alectinib Small molecular drug DB11363
Allopurinol Small molecular drug DB00437
Alpelisib Small molecular drug DB12015
Amisulpride Small molecular drug DB06288
Apalutamide Small molecular drug DB11901
Apixaban Small molecular drug DB06605
Artesunate Small molecular drug DB09274
Asciminib Small molecular drug DB12597
Avanafil Small molecular drug DB06237
Avatrombopag Small molecular drug DB11995
Baloxavir Marboxil Small molecular drug DB13997
Baricitinib Small molecular drug DB11817
Beclomethasone Dipropionate Small molecular drug DB00394
Berotralstat Small molecular drug DB15982
Brigatinib Small molecular drug DB12267
Brincidofovir Small molecular drug DB12151
Buprenorphine Small molecular drug DB00921
Cabazitaxel Small molecular drug DB06772
Cabotegravir Small molecular drug DB11751
Caffeine Small molecular drug DB00201
Canagliflozin Small molecular drug DB08907
Cannabidiol Small molecular drug DB09061
Capmatinib Small molecular drug DB11791
Celecoxib Small molecular drug DB00482
Cerivastatin Small molecular drug DB00439
Cholesterol Small molecular drug DB04540
Cisplatin Small molecular drug DB00515
Cladribine Small molecular drug DB00242
Clofarabine Small molecular drug DB00631
Clofazimine Small molecular drug DB00845
Cobicistat Small molecular drug DB09065
Cobimetinib Small molecular drug DB05239
Conjugated Estrogens Small molecular drug DB00286
Dabrafenib Small molecular drug DB08912
Daclatasvir Small molecular drug DB09102
Dacomitinib Small molecular drug DB11963
Dactinomycin Small molecular drug DB00970
Dasabuvir Small molecular drug DB09183
Dasatinib Small molecular drug DB01254
Daunorubicin Small molecular drug DB00694
Delafloxacin Small molecular drug DB11943
Dexamethasone Small molecular drug DB01234
Diethylstilbestrol Small molecular drug DB00255
Docetaxel Small molecular drug DB01248
Dolutegravir Small molecular drug DB08930
Donepezil Small molecular drug DB00843
Doxorubicin Small molecular drug DB00997
Dronabinol Small molecular drug DB00470
Duvelisib Small molecular drug DB11952
Eltrombopag Small molecular drug DB06210
Empagliflozin Small molecular drug DB09038
Erlotinib Small molecular drug DB00530
Ertugliflozin Small molecular drug DB11827
Estradiol Small molecular drug DB00783
Estradiol Acetate Small molecular drug DB13952
Estradiol Cypionate Small molecular drug DB13954
Estradiol Valerate Small molecular drug DB13956
Estrone Small molecular drug DB00655
Etoposide Small molecular drug DB00773
Ezetimibe Small molecular drug DB00973
Febuxostat Small molecular drug DB04854
Fedratinib Small molecular drug DB12500
Fluorouracil Small molecular drug DB00544
Folic Acid Small molecular drug DB00158
Fostamatinib Small molecular drug DB12010
Fostemsavir Small molecular drug DB11796
Fusidic Acid Small molecular drug DB02703
Gefitinib Small molecular drug DB00317
Gilteritinib Small molecular drug DB12141
Glasdegib Small molecular drug DB11978
Glecaprevir Small molecular drug DB13879
Glyburide Small molecular drug DB01016
Idelalisib Small molecular drug DB09054
Imatinib Small molecular drug DB00619
Infigratinib Small molecular drug DB11886
Irinotecan Small molecular drug DB00762
Isavuconazole Small molecular drug DB11633
Istradefylline Small molecular drug DB11757
Lamivudine Small molecular drug DB00709
Lansoprazole Small molecular drug DB00448
Lasmiditan Small molecular drug DB11732
Ledipasvir Small molecular drug DB09027
Leflunomide Small molecular drug DB01097
Lenvatinib Small molecular drug DB09078
Lonafarnib Small molecular drug DB06448
Maribavir Small molecular drug DB06234
Methotrexate Small molecular drug DB00563
Mitoxantrone Small molecular drug DB01204
Mobocertinib Small molecular drug DB16390
Mycophenolate Mofetil Small molecular drug DB00688
Nelfinavir Small molecular drug DB00220
Nifurtimox Small molecular drug DB11820
Nilotinib Small molecular drug DB04868
Nintedanib Small molecular drug DB09079
Niraparib Small molecular drug DB11793
Nitrofurantoin Small molecular drug DB00698
Novobiocin Small molecular drug DB01051
Olaparib Small molecular drug DB09074
Ombitasvir Small molecular drug DB09296
Omeprazole Small molecular drug DB00338
Osimertinib Small molecular drug DB09330
Oteseconazole Small molecular drug DB13055
Pacritinib Small molecular drug DB11697
Palbociclib Small molecular drug DB09073
Pantoprazole Small molecular drug DB00213
Paritaprevir Small molecular drug DB09297
Pazopanib Small molecular drug DB06589
Pemetrexed Small molecular drug DB00642
Pibrentasvir Small molecular drug DB13878
Pitavastatin Small molecular drug DB08860
Ponatinib Small molecular drug DB08901
Pralatrexate Small molecular drug DB06813
Prasterone Small molecular drug DB01708
Pravastatin Small molecular drug DB00175
Prazosin Small molecular drug DB00457
Progesterone Small molecular drug DB00396
Rabeprazole Small molecular drug DB01129
Raloxifene Small molecular drug DB00481
Regorafenib Small molecular drug DB08896
Relugolix Small molecular drug DB11853
Rilpivirine Small molecular drug DB08864
Riluzole Small molecular drug DB00740
Rimegepant Small molecular drug DB12457
Riociguat Small molecular drug DB08931
Ritonavir Small molecular drug DB00503
Rivaroxaban Small molecular drug DB06228
Rolapitant Small molecular drug DB09291
Rosuvastatin Small molecular drug DB01098
Roxadustat Small molecular drug DB04847
Rucaparib Small molecular drug DB12332
Safinamide Small molecular drug DB06654
Saquinavir Small molecular drug DB01232
Selumetinib Small molecular drug DB11689
Simeprevir Small molecular drug DB06290
Sofosbuvir Small molecular drug DB08934
Sorafenib Small molecular drug DB00398
Sotagliflozin Small molecular drug DB12713
Sotorasib Small molecular drug DB15569
Stiripentol Small molecular drug DB09118
Sulfasalazine Small molecular drug D02ZTJ
Sulpiride Small molecular drug DB00391
Sumatriptan Small molecular drug DB00669
Sunitinib Small molecular drug DB01268
Talazoparib Small molecular drug DB11760
Tamoxifen Small molecular drug DB00675
Taurocholic Acid Small molecular drug DB04348
Tazemetostat Small molecular drug DB12887
Tegaserod Small molecular drug DB01079
Telmisartan Small molecular drug DB00966
Telotristat Ethyl Small molecular drug DB12095
Teniposide Small molecular drug DB00444
Tenofovir Alafenamide Small molecular drug DB09299
Tepotinib Small molecular drug DB15133
Teriflunomide Small molecular drug DB08880
Testosterone Small molecular drug DB00624
Testosterone Undecanoate Small molecular drug DB13946
Tezacaftor Small molecular drug DB11712
Tivozanib Small molecular drug DB11800
Topotecan Small molecular drug DB01030
Ubrogepant Small molecular drug DB15328
Vandetanib Small molecular drug DB05294
Velpatasvir Small molecular drug DB11613
Vemurafenib Small molecular drug DB08881
Venetoclax Small molecular drug DB11581
Venlafaxine Small molecular drug DB00285
Vericiguat Small molecular drug DB15456
Vincristine Small molecular drug DB00541
Vismodegib Small molecular drug DB08828
Voxilaprevir Small molecular drug DB12026
Zafirlukast Small molecular drug DB00549
Zidovudine Small molecular drug DB00495
Atogepant . DB16098
Avapritinib . DB15233
Belumosudil . DB16703
Copanlisib . DB12483
Darolutamide . DB12941
Deucravacitinib . DB16650
Dexamethasone Acetate . DB14649
Enasidenib . DB13874
Estradiol Benzoate . DB13953
Estradiol Dienanthate . DB13955
Futibatinib . DB15149
Hydrocortisone Acetate . DB14539
Hydrocortisone Butyrate . DB14540
Hydrocortisone Cypionate . DB14541
Hydrocortisone Phosphate . DB14542
Hydrocortisone Probutate . DB14543
Hydrocortisone Valerate . DB14544
Larotrectinib . DB14723
Letermovir . DB12070
Linzagolix . DB17083
Lusutrombopag . DB13125
Olutasidenib . DB16267
Opicapone . DB11632
Ozanimod . DB12612
Pemigatinib . DB15102
Pralsetinib . DB15822
Ripretinib . DB14840
Selpercatinib . DB15685
Tafamidis . DB11644
Tecovirimat . DB12020
Testosterone Cypionate . DB13943
Testosterone Enanthate . DB13944
Trastuzumab Deruxtecan . DB14962
Trilaciclib . DB15442
Tucatinib . DB11652
Upadacitinib . DB15091
Investigative
Click To Hide/Show 16 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Alvocidib Small molecular drug DB03496
Biricodar Small molecular drug DB04851
Camptothecin Small molecular drug DB04690
Daidzin Small molecular drug DB02115
Elacridar Small molecular drug DB04881
Genistein Small molecular drug DB01645
Hesperetin Small molecular drug DB01094
Nabiximols Small molecular drug DB14011
Naringenin Small molecular drug DB03467
Quercetin Small molecular drug DB04216
Topiroxostat Small molecular drug DB01685
Azvudine . DB16407
Dovitinib . DB05928
Fimasartan . DB09279
Hydrocortisone Aceponate . DB14538
Medical Cannabis . DB14009

References

1 A Paal-Knorr agent for chemoproteomic profiling of targets of isoketals in cells. Chem Sci. 2021 Oct 15;12(43):14557-14563. doi: 10.1039/d1sc02230j. eCollection 2021 Nov 10.
Mass spectrometry data entry: PXD028270
2 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
3 Nucleophilic covalent ligand discovery for the cysteine redoxome. Nat Chem Biol. 2023 Nov;19(11):1309-1319. doi: 10.1038/s41589-023-01330-5. Epub 2023 May 29.
Mass spectrometry data entry: PXD039908 , PXD029761
4 A modification-centric assessment tool for the performance of chemoproteomic probes. Nat Chem Biol. 2022 Aug;18(8):904-912. doi: 10.1038/s41589-022-01074-8. Epub 2022 Jul 21.
Mass spectrometry data entry: PXD027758 , PXD027755 , PXD027760 , PXD027762 , PXD027756 , PXD027591 , PXD007149 , PXD030064 , PXD032392 , PXD027789 , PXD027767 , PXD027764
5 Chemoproteomic Profiling by Cysteine Fluoroalkylation Reveals Myrocin G as an Inhibitor of the Nonhomologous End Joining DNA Repair Pathway. J Am Chem Soc. 2021 Dec 8;143(48):20332-20342. doi: 10.1021/jacs.1c09724. Epub 2021 Nov 24.
Mass spectrometry data entry: PXD029255