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A general pattern for substrate recognition by P-glycoprotein
JournalArticle (Originalarbeit in einer wissenschaftlichen Zeitschrift)
 
ID 155452
Author(s) Seelig, A
Author(s) at UniBasel Seelig-Löffler, Anna
Year 1998
Title A general pattern for substrate recognition by P-glycoprotein
Journal European journal of biochemistry
Volume 251
Number 1-2
Pages / Article-Number 252-61
Keywords P-glycoprotein, substrate recognition, recognition pattern, hydrogen bonding, multidrug resistance
Abstract P-glycoprotein actively transports a wide variety of chemically diverse compounds out of the cell. Based on a comparison of a hundred compounds previously tested as P-glycoprotein substrates, we suggest that a set of well-defined structural elements is required for an interaction with P-glycoprotein. The recognition elements are formed by two (type I unit) or three electron donor groups (type II unit) with a fixed spatial separation. Type I units consist of two electron donor groups with a spatial separation of 2.5 +/- 0.3 A. Type II units contain either two electron donor groups with a spatial separation of 4.6 +/- 0.6 A or three electron donor groups with a spatial separation of the outer two groups of 4.6 +/- 0.6 A. All molecules that contain at least one type I or one type II unit are predicted to be P-glycoprotein substrates. The binding to P-glycoprotein increases with the strength and the number of electron donor or hydrogen bonding acceptor groups forming the type I and type II units. Correspondingly, a high percentage of amino acids with hydrogen bonding donor side chains is found in the transmembrane sequences of P-glycoprotein relevant for substrate interaction. Molecules that minimally contain one type II unit are predicted to be inducers of P-glycoprotein over-expression.
Publisher Blackwell
ISSN/ISBN 0014-2956
edoc-URL http://edoc.unibas.ch/dok/A5258480
Full Text on edoc No
Digital Object Identifier DOI 10.1046/j.1432-1327.1998.2510252.x
PubMed ID http://www.ncbi.nlm.nih.gov/pubmed/9492291
ISI-Number WOS:000071706800029
Document type (ISI) Journal Article
 
   

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