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

T W Loo; D M Clarke

doi:10.1007/s00232-005-0792-1

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

J Membr Biol. 2005 Aug;206(3):173-85. doi: 10.1007/s00232-005-0792-1.

Authors

T W Loo¹, D M Clarke

Affiliation

¹ Department of Medicine and Department of Biochemistry, University of Toronto, Toronto, Ontario, Canada.

PMID: 16456713
DOI: 10.1007/s00232-005-0792-1

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

Research Support, Non-U.S. Gov't
Review

MeSH terms

ATP Binding Cassette Transporter, Subfamily B, Member 1 / chemistry*
ATP Binding Cassette Transporter, Subfamily B, Member 1 / metabolism*
ATP-Binding Cassette Transporters / chemistry*
ATP-Binding Cassette Transporters / metabolism*
Adenosine Triphosphate / chemistry*
Adenosine Triphosphate / metabolism*
Amino Acid Sequence
Animals
Binding Sites
Biological Transport, Active / physiology
Humans
Molecular Sequence Data
Pharmaceutical Preparations / metabolism*
Protein Binding
Structure-Activity Relationship

Substances

ATP Binding Cassette Transporter, Subfamily B, Member 1
ATP-Binding Cassette Transporters
Pharmaceutical Preparations
Adenosine Triphosphate