ATP-dependent translocase ABCB1

Function

Translocates drugs and phospholipids across the membrane. Catalyzes the flop of phospholipids from the cytoplasmic to the exoplasmic leaflet of the apical membrane. Participates mainly to the flop of phosphatidylcholine, phosphatidylethanolamine, beta-D-glucosylceramides and sphingomyelins. Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.

Classification

Family (Pfam)

PF00664 ABC_membrane, PF00005 ABC_tran

InterPro

AAA+_ATPase, ABC1_TM_dom, ABC1_TM_sf, ABC_transporter-like_ATP-bd, ABC_transporter-like_CS, P-loop_NTPase, Type_1_exporter

Functional cluster

Adenylate Kinases & Peroxiredoxins

Experimental structures · PDB · 24

• 6C0V EM 3.40A
• 6FN1 EM 3.58A
• 6FN4 EM 4.14A
• 6QEX EM 3.60A
• 7A65 EM 3.90A
• 7A69 EM 3.20A
• 7A6C EM 3.60A
• 7A6E EM 3.60A
• 7A6F EM 3.50A
• 7O9W EM 3.50A
• 8GMG EM 4.30A
• 8GMJ EM 4.40A
• … and 12 more

A predicted model is available from AlphaFold.

Gene Ontology · 36

• GO:0016324 apical plasma membrane
• GO:0009986 cell surface
• GO:0005737 cytoplasm
• GO:0098591 external side of apical plasma membrane
• GO:0070062 extracellular exosome
• GO:0016020 membrane
• GO:0005886 plasma membrane
• GO:0008559 ABC-type xenobiotic transporter activity
• GO:0005524 ATP binding
• GO:0016887 ATP hydrolysis activity
• GO:0042626 ATPase-coupled transmembrane transporter activity
• GO:0046943 carboxylic acid transmembrane transporter activity
• GO:0099038 ceramide floppase activity
• GO:0015562 efflux transmembrane transporter activity
• GO:0140328 floppase activity
• GO:0090554 phosphatidylcholine floppase activity
• GO:0090555 phosphatidylethanolamine flippase activity
• GO:0140341 phosphatidylethanolamine floppase activity
• GO:0022857 transmembrane transporter activity
• GO:0031625 ubiquitin protein ligase binding
• GO:0042910 xenobiotic transmembrane transporter activity
• GO:1905039 carboxylic acid transmembrane transport
• GO:0099040 ceramide translocation
• GO:0140115 export across plasma membrane
• GO:0000086 G2/M transition of mitotic cell cycle
• GO:0045332 phospholipid translocation
• GO:2001225 regulation of chloride transport
• GO:0009410 response to xenobiotic stimulus
• GO:0072089 stem cell proliferation
• GO:0046865 terpenoid transport
• GO:0070633 transepithelial transport
• GO:0055085 transmembrane transport
• GO:0150104 transport across blood-brain barrier
• GO:1990961 xenobiotic detoxification by transmembrane export across the plasma membrane
• GO:0006805 xenobiotic metabolic process
• GO:1990962 xenobiotic transport across blood-brain barrier

Disease associations

• inflammatory bowel disease 13 MONDO:0012831
• encephalopathy, acute transient MONDO:0975801

Drugs targeting this protein · 5

• VALSPODAR inhibitor
• TARIQUIDAR inhibitor
• BIRICODAR inhibitor
• ZOSUQUIDAR inhibitor
• ENCEQUIDAR inhibitor

Related proteins · sequence + function similarity

• ATP-dependent translocase ABCB1 0.99
• ATP-dependent translocase ABCB1 0.99
• ATP-dependent translocase ABCB1 0.98
• ATP-dependent translocase ABCB1 0.98
• Phosphatidylcholine translocator ABCB4 0.98
• Multidrug resistance protein 2 0.98
• Phosphatidylcholine translocator ABCB4 0.97
• Phosphatidylcholine translocator ABCB4 0.97
• Phosphatidylcholine translocator ABCB4 0.97
• Bile salt export pump 0.94
• ABC transporter B family member 4 0.94
• Multidrug resistance protein pgp-1 0.93

Co-cited proteins · studied together in the literature

• Required for drug-induced death protein 1 1 shared papers
• Tissue factor pathway inhibitor 2 1 shared papers
• ATP-dependent translocase ABCB1 1 shared papers
• Serine/threonine-protein phosphatase 2A regulatory subunit B'' subunit gamma 1 shared papers
• Multidrug resistance protein 1 1 shared papers
• Phosphatidylcholine translocator ABCB4 1 shared papers
• ATP-binding cassette sub-family C member 3 1 shared papers
• Solute carrier family 15 member 1 1 shared papers
• Chloroquine resistance transporter 1 shared papers
• Mitochondrial potassium channel ATP-binding subunit 1 shared papers
• Chloroquine resistance transporter 1 shared papers
• ATP-binding cassette sub-family B member 10, mitochondrial 1 shared papers

Literature · 28 cited papers

• Chemical genomics with pyrvinium identifies C1orf115 as a regulator of drug efflux. Nat. Chem. Biol. · 2022
• Mechanistic basis for multidrug resistance and collateral drug sensitivity conferred to the malaria parasite by polymorphisms in PfMDR1 and PfCRT. PLoS Biol. · 2022
• Serious Ivermectin toxicity and human ABCB1 nonsense mutations. N. Engl. J. Med. · 2020
• Biallelic mutations in ABCB1 display recurrent reversible encephalopathy. Ann. Clin. Transl. Neurol. · 2020
• The Organic Anion-Transporting Peptide 2B1 Is Localized in the Basolateral Membrane of the Human Jejunum and Caco-2 Monolayers. J. Pharm. Sci. · 2017
• Protein phosphatase complex PP5/PPP2R3C dephosphorylates P-glycoprotein/ABCB1 and down-regulates the expression and function. Cancer Lett. · 2014
• Initial characterization of the human central proteome. BMC Syst. Biol. · 2011
• A quantitative atlas of mitotic phosphorylation. Proc. Natl. Acad. Sci. U.S.A. · 2008
• The consensus coding sequences of human breast and colorectal cancers. Science · 2006
• Twelve novel single nucleotide polymorphisms in ABCB1/MDR1 among Japanese patients with ventricular tachycardia who were administered amiodarone. Drug Metab. Pharmacokinet. · 2002
• Polymorphism of MDR1 gene in healthy Japanese subjects: a novel SNP with an amino acid substitution (Glu108Lys). Drug Metab. Pharmacokinet. · 2002
• Cytoplasmic domains of the transporter associated with antigen processing and P-glycoprotein interact with subunits of the proteasome. Mol. Immunol. · 2005
• … and 16 more in the literature graph