General Information of Target

Target ID LDTP00638
Target Name ATP-binding cassette sub-family C member 3 (ABCC3)
Gene Name ABCC3
Gene ID 8714
Synonyms
CMOAT2; MLP2; MRP3; ATP-binding cassette sub-family C member 3; EC 7.6.2.-; EC 7.6.2.2; EC 7.6.2.3; Canalicular multispecific organic anion transporter 2; Multi-specific organic anion transporter D; MOAT-D; Multidrug resistance-associated protein 3
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MDALCGSGELGSKFWDSNLSVHTENPDLTPCFQNSLLAWVPCIYLWVALPCYLLYLRHHC
RGYIILSHLSKLKMVLGVLLWCVSWADLFYSFHGLVHGRAPAPVFFVTPLVVGVTMLLAT
LLIQYERLQGVQSSGVLIIFWFLCVVCAIVPFRSKILLAKAEGEISDPFRFTTFYIHFAL
VLSALILACFREKPPFFSAKNVDPNPYPETSAGFLSRLFFWWFTKMAIYGYRHPLEEKDL
WSLKEEDRSQMVVQQLLEAWRKQEKQTARHKASAAPGKNASGEDEVLLGARPRPRKPSFL
KALLATFGSSFLISACFKLIQDLLSFINPQLLSILIRFISNPMAPSWWGFLVAGLMFLCS
MMQSLILQHYYHYIFVTGVKFRTGIMGVIYRKALVITNSVKRASTVGEIVNLMSVDAQRF
MDLAPFLNLLWSAPLQIILAIYFLWQNLGPSVLAGVAFMVLLIPLNGAVAVKMRAFQVKQ
MKLKDSRIKLMSEILNGIKVLKLYAWEPSFLKQVEGIRQGELQLLRTAAYLHTTTTFTWM
CSPFLVTLITLWVYVYVDPNNVLDAEKAFVSVSLFNILRLPLNMLPQLISNLTQASVSLK
RIQQFLSQEELDPQSVERKTISPGYAITIHSGTFTWAQDLPPTLHSLDIQVPKGALVAVV
GPVGCGKSSLVSALLGEMEKLEGKVHMKGSVAYVPQQAWIQNCTLQENVLFGKALNPKRY
QQTLEACALLADLEMLPGGDQTEIGEKGINLSGGQRQRVSLARAVYSDADIFLLDDPLSA
VDSHVAKHIFDHVIGPEGVLAGKTRVLVTHGISFLPQTDFIIVLADGQVSEMGPYPALLQ
RNGSFANFLCNYAPDEDQGHLEDSWTALEGAEDKEALLIEDTLSNHTDLTDNDPVTYVVQ
KQFMRQLSALSSDGEGQGRPVPRRHLGPSEKVQVTEAKADGALTQEEKAAIGTVELSVFW
DYAKAVGLCTTLAICLLYVGQSAAAIGANVWLSAWTNDAMADSRQNNTSLRLGVYAALGI
LQGFLVMLAAMAMAAGGIQAARVLHQALLHNKIRSPQSFFDTTPSGRILNCFSKDIYVVD
EVLAPVILMLLNSFFNAISTLVVIMASTPLFTVVILPLAVLYTLVQRFYAATSRQLKRLE
SVSRSPIYSHFSETVTGASVIRAYNRSRDFEIISDTKVDANQRSCYPYIISNRWLSIGVE
FVGNCVVLFAALFAVIGRSSLNPGLVGLSVSYSLQVTFALNWMIRMMSDLESNIVAVERV
KEYSKTETEAPWVVEGSRPPEGWPPRGEVEFRNYSVRYRPGLDLVLRDLSLHVHGGEKVG
IVGRTGAGKSSMTLCLFRILEAAKGEIRIDGLNVADIGLHDLRSQLTIIPQDPILFSGTL
RMNLDPFGSYSEEDIWWALELSHLHTFVSSQPAGLDFQCSEGGENLSVGQRQLVCLARAL
LRKSRILVLDEATAAIDLETDNLIQATIRTQFDTCTVLTIAHRLNTIMDYTRVLVLDKGV
VAEFDSPANLIAARGIFYGMARDAGLA
Target Bioclass
Enzyme
Family
ABC transporter superfamily, ABCC family, Conjugate transporter (TC 3.A.1.208) subfamily
Subcellular location
Basolateral cell membrane
Function
ATP-dependent transporter of the ATP-binding cassette (ABC) family that binds and hydrolyzes ATP to enable active transport of various substrates including many drugs, toxicants and endogenous compound across cell membranes. Transports glucuronide conjugates such as bilirubin diglucuronide, estradiol-17-beta-o-glucuronide and GSH conjugates such as leukotriene C4 (LTC4). Transports also various bile salts (taurocholate, glycocholate, taurochenodeoxycholate-3-sulfate, taurolithocholate- 3-sulfate). Does not contribute substantially to bile salt physiology but provides an alternative route for the export of bile acids and glucuronides from cholestatic hepatocytes. May contribute to regulate the transport of organic compounds in testes across the blood-testis-barrier (Probable). Can confer resistance to various anticancer drugs, methotrexate, tenoposide and etoposide, by decreasing accumulation of these drugs in cells.
Uniprot ID
O15438
Ensemble ID
ENST00000285238.13
HGNC ID
HGNC:54
ChEMBL ID
CHEMBL5918

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
CAL27 SNV: p.S91F DBIA    Probe Info 
CMK SNV: p.Q614H DBIA    Probe Info 
HCT15 SNV: p.V806M DBIA    Probe Info 
HEC1 SNV: p.C82Y .
HEC1B SNV: p.C82Y .
JHH7 SNV: p.N716Y .
JURKAT Deletion: p.Q614RfsTer34 .
KYSE510 SNV: p.E126Q DBIA    Probe Info 
LOXIMVI SNV: p.D791N DBIA    Probe Info 
LS180 SNV: p.P1056S DBIA    Probe Info 
MEWO SNV: p.L1484P .
NCIH2286 SNV: p.Q477H DBIA    Probe Info 
NCIH716 SNV: p.G1378V .
ONS76 SNV: p.T628S DBIA    Probe Info 
RKO SNV: p.S7P DBIA    Probe Info 
TOV21G SNV: p.W995R DBIA    Probe Info 

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 4 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
IPM
 Probe Info 
C665(0.00); C1435(0.00); C1071(0.00)  LDD0241  [1]
DBIA
 Probe Info 
C716(1.90); C1486(2.82)  LDD3310  [2]
BTD
 Probe Info 
C1071(4.49)  LDD2097  [3]
WYneN
 Probe Info 
N.A.  LDD0021  [4]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0519  1-(6-methoxy-3,4-dihydroquinolin-1(2H)-yl)-2-nitroethan-1-one MDA-MB-231 C1071(1.06)  LDD2112  [3]
 LDCM0022  KB02 22RV1 C1486(1.89)  LDD2243  [2]
 LDCM0023  KB03 22RV1 C1486(1.33)  LDD2660  [2]
 LDCM0024  KB05 COLO792 C716(1.90); C1486(2.82)  LDD3310  [2]
 LDCM0504  Nucleophilic fragment 15a MDA-MB-231 C1071(4.49)  LDD2097  [3]
 LDCM0507  Nucleophilic fragment 16b MDA-MB-231 C1071(0.84)  LDD2100  [3]
 LDCM0513  Nucleophilic fragment 19b MDA-MB-231 C1071(0.79)  LDD2106  [3]
 LDCM0525  Nucleophilic fragment 25b MDA-MB-231 C1071(0.97)  LDD2118  [3]
 LDCM0541  Nucleophilic fragment 36 MDA-MB-231 C1071(0.92)  LDD2134  [3]
 LDCM0542  Nucleophilic fragment 37 MDA-MB-231 C1435(1.01)  LDD2135  [3]
 LDCM0547  Nucleophilic fragment 41 MDA-MB-231 C1071(0.75)  LDD2141  [3]
 LDCM0554  Nucleophilic fragment 7a MDA-MB-231 C1071(0.34)  LDD2148  [3]
 LDCM0555  Nucleophilic fragment 7b MDA-MB-231 C1071(0.67)  LDD2149  [3]

The Interaction Atlas With This Target

The Drug(s) Related To This Target

Approved
Click To Hide/Show 29 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Belantamab Mafodotin Antibody drug conjugate DB15719
Bempedoic Acid Small molecular drug DB11936
Cholic Acid Small molecular drug DB02659
Cisplatin Small molecular drug DB00515
Conjugated Estrogens Small molecular drug DB00286
Doxorubicin Small molecular drug DB00997
Etoposide Small molecular drug DB00773
Ezetimibe Small molecular drug DB00973
Fexofenadine Small molecular drug DB00950
Fluorouracil Small molecular drug DB00544
Folic Acid Small molecular drug DB00158
Glutathione Small molecular drug DB00143
Glyburide Small molecular drug DB01016
Indomethacin Small molecular drug DB00328
Lamivudine Small molecular drug DB00709
Methotrexate Small molecular drug DB00563
Metyrapone Small molecular drug DB01011
Nifedipine Small molecular drug DB01115
Omeprazole Small molecular drug DB00338
Phenobarbital Small molecular drug DB01174
Pralatrexate Small molecular drug DB06813
Probenecid Small molecular drug DB01032
Promethazine Small molecular drug DB01069
Raloxifene Small molecular drug DB00481
Rifampicin Small molecular drug DB01045
Sulfinpyrazone Small molecular drug DB01138
Taurocholic Acid Small molecular drug DB04348
Verapamil Small molecular drug DB00661
Vincristine Small molecular drug DB00541
Investigative
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Dovitinib . DB05928

References

1 Oxidant-Induced Bioconjugation for Protein Labeling in Live Cells. ACS Chem Biol. 2023 Jan 20;18(1):112-122. doi: 10.1021/acschembio.2c00740. Epub 2022 Dec 21.
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