P-glycoprotein 1 (PGY1, multidrug resistance protein 1, MDR1, gp170, ATP-binding cassette subfamily B member 1, ABCB1)
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Function
- energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells
- P-glycoprotein 1 helps eliminate drugs by pumping them OUT of cells, back into the gut, bile, & urine for excretion
- substrates
Structure
- belongs to the ABC transporter family, multidrug resistance exporter (TC 3.A.1.201) subfamily
- contains 2 ABC transmembrane type-1 domains
- contains 2 ABC transporter domains
Compartment
membrane
Expression
- expressed in liver, kidney, small intestine & brain
- inducers: St John's wort
- inhibitors:
Pathology
- tumor cells may up-relate P-glycoprotein 1 as a mechanism for development of resistance to antineoplastic agents
Polymorphism
- genetic variation in ABCB1 may play a role in patients who do not respond to drug treatment
- polymorphisms in ABCB1 may predispose to neuropsychiatric adverse effects of mefloquine[3]
More general terms
- P-glycoprotein (gp170) or multidrug-resistance glycoprotein
- ATP-binding cassette sub-family B (ABC transporter-B, ABCB)
References
- ↑ UniProt http://www.uniprot.org/uniprot/P08183.html
- ↑ Entrez Gene http://www.ncbi.nlm.nih.gov/sites/entrez?db=gene&cmd=Retrieve&dopt=Graphics&list_uids=5243
- ↑ 3.0 3.1 Aarnoudse ALHJ et al, MDR1 gene polymorphisms are associated with neuropsychiatric adverse effects of mefloquine. Clin Pharmacol Ther 2006, 80:367 PMID: https://www.ncbi.nlm.nih.gov/pubmed/17015054
- ↑ Atlas of genetics & cytogenetics in oncology & haematology http://atlasgeneticsoncology.org/genes/PGY1ID105.html
- ↑ NIEHS-SNPs http://egp.gs.washington.edu/data/abcb1/
- ↑ SHMPD; The Singapore human mutation and polymorphism database http://shmpd.bii.a-star.edu.sg/gene.php?genestart=A&genename=ABCB1
- ↑ Wikipedia; Note: P-glycoprotein entry http://en.wikipedia.org/wiki/P-glycoprotein