Abstract
All-O-undec-en-10-yl derivatives of d-glucose have been prepared and their affinities for the Plasmodium falciparum hexose transporter (PfHT) determined; the O-2 derivative displays a good apparent affinity for PfHT (K(I)=2 microM) with no significant interaction with the mammalian transporter GLUT1. This selectivity points to position -2 of glucose as an appropriate substitution site for the development of inhibitors of P. falciparum glucose uptake.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Antigens, Protozoan / chemistry
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Antimalarials / chemistry*
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Antimalarials / pharmacology
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Chemistry, Pharmaceutical / methods*
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Drug Design
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Glucose / chemistry*
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Glucose / pharmacokinetics
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Inhibitory Concentration 50
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Kinetics
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Models, Chemical
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Monosaccharide Transport Proteins / chemistry*
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Monosaccharide Transport Proteins / metabolism
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Oocytes / metabolism
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Plasmodium falciparum
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Protein Binding
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Protozoan Proteins / chemistry*
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Protozoan Proteins / metabolism
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Xenopus laevis
Substances
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Antigens, Protozoan
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Antimalarials
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Monosaccharide Transport Proteins
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Protozoan Proteins
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hexose transporter 1 protein, Plasmodium falciparum
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Glucose