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ABCC1

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Target id: 779

Nomenclature: ABCC1

Abbreviated Name: MRP1

Systematic Nomenclature: ABCC1

Family: ABCC subfamily

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 17 1531 16p13.11 ABCC1 ATP binding cassette subfamily C member 1 (ABCC1 blood group)
Mouse 17 1528 16 A1 Abcc1 ATP-binding cassette, sub-family C member 1
Rat 17 1532 10q11 Abcc1 ATP binding cassette subfamily C member 1
Previous and Unofficial Names Click here for help
leukotriene C4 transporter | GS-X | MRP | multidrug resistance associated protein 1 | Abcc1a | ATP-binding cassette sub-family C (CFTR/MRP) member 1 (multiple drug resistance-associated protein) | ATP-binding cassette, sub-family C (CFTR/MRP), member 1 | ATP-binding cassette, sub-family C (CFTR/MRP), member 1a | Avcc1a | LTC4 transporter | Multidrug resistance protein 1 | Abcc1b | Mdrap | ATP-binding cassette sub-family C (CFTR/MRP) member 1a | MRP1 | ATP-binding cassette, subfamily C (CFTR/MRP), member 1 | ATP-binding cassette | ATP binding cassette subfamily C member 1
Database Links Click here for help
Alphafold P33527 (Hs), O35379 (Mm), Q8CG09 (Rn)
ChEMBL Target CHEMBL3004 (Hs), CHEMBL2532 (Mm), CHEMBL5680 (Rn)
DrugBank Target P33527 (Hs)
Ensembl Gene ENSG00000103222 (Hs), ENSMUSG00000023088 (Mm), ENSRNOG00000022305 (Rn)
Entrez Gene 4363 (Hs), 17250 (Mm), 24565 (Rn)
Human Protein Atlas ENSG00000103222 (Hs)
KEGG Gene hsa:4363 (Hs), mmu:17250 (Mm), rno:24565 (Rn)
OMIM 158343 (Hs)
Pharos P33527 (Hs)
UniProtKB P33527 (Hs), O35379 (Mm), Q8CG09 (Rn)
Wikipedia ABCC1 (Hs)
Selected 3D Structures Click here for help
Image of receptor 3D structure from RCSB PDB
Description:  Structure of the human multidrug resistance protein 1 nucleotide binding domain 1
PDB Id:  2CBZ
Resolution:  1.5Å
Species:  Human
References:  3
Image of receptor 3D structure from RCSB PDB
Description:  Cryo-EM structure of human ABC transporter ABCC1
PDB Id:  8VT4
Resolution:  3.79Å
Species:  Human
References:  4
Image of receptor 3D structure from RCSB PDB
Description:  Cryo-EM structure of human ABC transporter (hABCC1) bound to cGAMP
PDB Id:  8VUX
Ligand:  2'3'-cGAMP
Resolution:  3.549207Å
Species:  Human
References: 

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Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
WP814 Small molecule or natural product Hs Inhibition 7.2 pKi 2
⤷ pKi 7.2 (Ki 7x10-8 M) [2]
compound 14 [PMID: 30925062] Small molecule or natural product Click here for species-specific activity table Hs Competitive 5.3 pIC50 5
⤷ pIC50 5.3 (IC50 5.04x10-6 M) [5]
Description: Measuring inhibition of calcein AM transport in H69AR cells overexpressing hABCC1.
biricodar Small molecule or natural product Click here for species-specific activity table Hs Inhibition 5.3 pIC50 6
⤷ pIC50 5.3 (IC50 5.18x10-6 M) [6]
Immunopharmacology Comments
ABCC1 actively exports the immunostimulatory cyclic dinucleotide cGAMP, and thereby participates in regulating the cGAS-STING-mediated innate immune response in mammalian cells [1,4].
Immuno Process Associations
Immuno Process:  Immune regulation
Immuno Process:  Inflammation

References

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1. Maltbaek JH, Cambier S, Snyder JM, Stetson DB. (2022) ABCC1 transporter exports the immunostimulatory cyclic dinucleotide cGAMP. Immunity, 55 (10): 1799-1812.e4. [PMID:36070769]

2. Priebe W, Krawczyk M, Kuo MT, Yamane Y, Savaraj N, Ishikawa T. (1998) Doxorubicin- and daunorubicin-glutathione conjugates, but not unconjugated drugs, competitively inhibit leukotriene C4 transport mediated by MRP/GS-X pump. Biochem Biophys Res Commun, 247 (3): 859-63. [PMID:9647783]

3. Ramaen O, Leulliot N, Sizun C, Ulryck N, Pamlard O, Lallemand JY, Tilbeurgh Hv, Jacquet E. (2006) Structure of the human multidrug resistance protein 1 nucleotide binding domain 1 bound to Mg2+/ATP reveals a non-productive catalytic site. J Mol Biol, 359 (4): 940-9. [PMID:16697012]

4. Shinde O, Boyer JA, Cambier S, VanPortfliet JJ, Sui X, Yadav GP, Viverette EG, Borgnia MJ, West AP, Zhang Q et al.. (2025) Structures of ATP-binding cassette transporter ABCC1 reveal the molecular basis of cyclic dinucleotide cGAMP export. Immunity, 58 (1): 59-73.e5. [PMID:39765229]

5. Silbermann K, Stefan SM, Elshawadfy R, Namasivayam V, Wiese M. (2019) Identification of Thienopyrimidine Scaffold as an Inhibitor of the ABC Transport Protein ABCC1 (MRP1) and Related Transporters Using a Combined Virtual Screening Approach. J Med Chem, 62 (9): 4383-4400. [PMID:30925062]

6. Wang S, Ryder H, Pretswell I, Depledge P, Milton J, Hancox TC, Dale I, Dangerfield W, Charlton P, Faint R et al.. (2002) Studies on quinazolinones as dual inhibitors of Pgp and MRP1 in multidrug resistance. Bioorg Med Chem Lett, 12 (4): 571-4. [PMID:11844674]

Contributors

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