Recent progress in understanding the mechanism of P-glycoprotein-mediated drug efflux

P-glycoprotein (P-gp) is an ATP-dependent drug pump that can transport a broad range of hydrophobic compounds out of the cell. The protein is clinically important because of its contribution to the phenomenon of multidrug resistance during AIDS/HIV and cancer chemotherapy. P-gp is a member of the AT...

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Bibliographic Details
Published in:The Journal of membrane biology 2005-08, Vol.206 (3), p.173-185
Main Authors: Loo, T W, Clarke, D M
Format: Article
Language:English
Subjects:
Adenosine Triphosphate - chemistry
Adenosine Triphosphate - metabolism
Amino Acid Sequence
Animals
ATP-Binding Cassette Transporters - chemistry
ATP-Binding Cassette Transporters - metabolism
ATP-Binding Cassette, Sub-Family B, Member 1 - chemistry
ATP-Binding Cassette, Sub-Family B, Member 1 - metabolism
Binding Sites
Biological Transport, Active - physiology
Humans
Molecular Sequence Data
Pharmaceutical Preparations - metabolism
Protein Binding
Structure-Activity Relationship
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Summary:P-glycoprotein (P-gp) is an ATP-dependent drug pump that can transport a broad range of hydrophobic compounds out of the cell. The protein is clinically important because of its contribution to the phenomenon of multidrug resistance during AIDS/HIV and cancer chemotherapy. P-gp is a member of the ATP-binding cassette (ABC) family of proteins. It is a single polypeptide that contains two repeats joined by a linker region. Each repeat has a transmembrane domain consisting of six transmembrane segments followed by a hydrophilic domain containing the nucleotide-binding domain. In this mini-review, we discuss recent progress in determining the structure and mechanism of human P-glycoprotein.
ISSN:0022-2631
1432-1424
DOI:10.1007/s00232-005-0792-1