Interaction of O-(undec-10-en)-yl-d-glucose derivatives with the Plasmodium falciparum hexose transporter (PfHT)
| Autor: | Sanjeev Krishna, Christophe Morin, Marina Ionita, Asha Parbhu Patel, Pierre-Marc Léo |
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| Rok vydání: | 2007 |
| Předmět: |
Monosaccharide Transport Proteins
Stereochemistry Chemistry Pharmaceutical Glucose uptake Plasmodium falciparum Clinical Biochemistry Protozoan Proteins Pharmaceutical Science Antigens Protozoan Biochemistry Antimalarials Inhibitory Concentration 50 Xenopus laevis chemistry.chemical_compound D-Glucose parasitic diseases Drug Discovery Animals Molecular Biology chemistry.chemical_classification biology Organic Chemistry Transporter biology.organism_classification In vitro Kinetics Glucose Models Chemical chemistry Aldose Drug Design Oocytes biology.protein Molecular Medicine GLUT1 Selectivity Protein Binding |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 17:4934-4937 |
| ISSN: | 0960-894X |
| DOI: | 10.1016/j.bmcl.2007.06.021 |
| Popis: | 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 μM) 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. |
| Databáze: | OpenAIRE |
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