Interaction of O-(undec-10-en)-yl-D-glucose derivatives with the Plasmodium falciparum hexose transporter (PfHT).
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.
Ionita
Marina
M
Département de Chimie Moléculaire (Serco, UMR-5250, ICMG FR-2607, CNRS), Université Joseph Fourier, BP-53, 38041, Grenoble Cedex, France.
Krishna
Sanjeev
S
Léo
Pierre-Marc
PM
Morin
Christophe
C
Patel
Asha Parbhu
AP
D000818:Animals; D000953:Antigens, Protozoan / Q000737:chemistry; D000962:Antimalarials / Q000737:chemistry* / Q000494:pharmacology; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D015195:Drug Design; D005947:Glucose / Q000737:chemistry* / Q000493:pharmacokinetics; D020128:Inhibitory Concentration 50; D007700:Kinetics; D008956:Models, Chemical; D009004:Monosaccharide Transport Proteins / Q000737:chemistry* / Q000378:metabolism; D009865:Oocytes / Q000378:metabolism; D010963:Plasmodium falciparum; D011485:Protein Binding; D015800:Protozoan Proteins / Q000737:chemistry* / Q000378:metabolism; D014982:Xenopus laevis
D000953:Antigens, Protozoan; D000962:Antimalarials; D009004:Monosaccharide Transport Proteins; D015800:Protozoan Proteins; C118145:hexose transporter 1 protein, Plasmodium falciparum; D005947:Glucose