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PubMed · 9441945

How does P-glycoprotein recognize its substrates?

K Ueda·Y Taguchi·M Morishima
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Abstract

We review how P-glycoprotein recognizes a wide variety of compounds and how it carries its substrates across membranes. Amino acid substitutions that affect the substrate specificity of P-glycoprotein have been found scattered throughout the molecule. In particular, some amino acid residues in the putative transmembrane domain (TM) 1 together with TM5-6 and TM11-12 may help to govern substrate specificity. The features that substrates for P-glycoprotein share are also discussed. The amphipathy of a substrate may decide whether the substrate can be intercalated into the lipid bilayer of the membrane. In addition, only certain molecular volumes and tertiary structures may make it possible for the substrate to fit into the substrate-binding site(s) of P-glycoprotein.

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ATP Binding Cassette Transporter, Subfamily B, Member 1AnimalsDNA Mutational AnalysisHumansRecombinant Fusion ProteinsStructure-Activity RelationshipSubstrate SpecificityJournal ArticleResearch Support, Non-U.S. Gov'tReview

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K Ueda, Y Taguchi, M Morishima. 1997. How does P-glycoprotein recognize its substrates?. https://doi.org/10.1006/scbi.1997.0066

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