Abstract
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.
Publication types
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Research Support, Non-U.S. Gov't
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Review
MeSH terms
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ATP Binding Cassette Transporter, Subfamily B, Member 1 / chemistry*
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ATP Binding Cassette Transporter, Subfamily B, Member 1 / metabolism*
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ATP-Binding Cassette Transporters / chemistry*
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ATP-Binding Cassette Transporters / metabolism*
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Adenosine Triphosphate / chemistry*
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Adenosine Triphosphate / metabolism*
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Amino Acid Sequence
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Animals
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Binding Sites
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Biological Transport, Active / physiology
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Humans
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Molecular Sequence Data
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Pharmaceutical Preparations / metabolism*
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Protein Binding
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Structure-Activity Relationship
Substances
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ATP Binding Cassette Transporter, Subfamily B, Member 1
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ATP-Binding Cassette Transporters
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Pharmaceutical Preparations
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Adenosine Triphosphate