Probing structure/affinity relationships for the Plasmodium falciparum hexose transporter with glucose derivatives

Fayolle, Martine; Ionita, Marina; Krishna, Sanjeev; Morin, Christophe; Patel, Asha Parbhu

doi:10.1016/j.bmcl.2005.11.068

Cited by 13 publications

(17 citation statements)

References 31 publications

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“…A 3- O -substituted chain length of between 8-13 carbons is necessary to maintain inhibitory activity against PfHT [33]. Also, repositioning of the O -[undecyl-10-en]-1-yl substituent at C2 in the glucose molecule produced a significantly higher affinity inhibitor (K i of 2 μM against PfHT, see Figure 2B) compared with the C3 derivative, compound 3361 [34].…”

Section: Background - Malaria Burden and Drug Resistancementioning

confidence: 99%

Plasmodial sugar transporters as anti-malarial drug targets and comparisons with other protozoa

Slavic

Krishna

Derbyshire

et al. 2011

Malar J

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Glucose is the primary source of energy and a key substrate for most cells. Inhibition of cellular glucose uptake (the first step in its utilization) has, therefore, received attention as a potential therapeutic strategy to treat various unrelated diseases including malaria and cancers. For malaria, blood forms of parasites rely almost entirely on glycolysis for energy production and, without energy stores, they are dependent on the constant uptake of glucose. Plasmodium falciparum is the most dangerous human malarial parasite and its hexose transporter has been identified as being the major glucose transporter. In this review, recent progress regarding the validation and development of the P. falciparum hexose transporter as a drug target is described, highlighting the importance of robust target validation through both chemical and genetic methods. Therapeutic targeting potential of hexose transporters of other protozoan pathogens is also reviewed and discussed.

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Section: Background - Malaria Burden and Drug Resistancementioning

confidence: 99%

Plasmodial sugar transporters as anti-malarial drug targets and comparisons with other protozoa

Slavic

Krishna

Derbyshire

et al. 2011

Malar J

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“…Another attempt to inhibit P. falciparum hexose transporter (PfHT) expressed in a heterologous system (xenope oocyte) with 3-O-ferrocenyl-dglucose derivatives was performed, but the products failed to show an inhibitory effect upon the transporter. [34] Ferrocenyl chalcones were synthesized and, among them, some compounds had an antimalarial activity in the micromolar range. [35] Interestingly, the incorporation of the ferrocene moiety in the chalcone template was found to enhance its role in processes that involved free radicals.…”

Section: Atovaquonementioning

confidence: 99%

Ferrocene Conjugates of Chloroquine and other Antimalarials: the Development of Ferroquine, a New Antimalarial

Dive¹,

Biot²

2008

ChemMedChem

228

162

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A convenient approach to antimalarial drug discovery is the use of the organic scaffold of a known antimalarial drug and an organometallic moiety to alter its unwanted properties and/or to optimize its initial effects. This minireview focuses mainly on the discovery of ferroquine, which has emerged from a collaborative French discovery project, and efforts to understand its mechanism of action and resistance.

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“…Phloretin, bovine serum albumin (BSA), Giemsa stain, dimethyl sulfoxide (DMSO), and Bradford reagent were obtained from Sigma-Aldrich (Dorset, United Kingdom). 3-O-(Undec-10-en)-yl-D-glucose (compound 3361) was prepared as described previously (7). [ 14 C]2-Deoxy-D-glucose (2-DOG) was obtained from Amersham (Bucks, United Kingdom).…”

Section: Methodsmentioning

confidence: 99%

Use of a Selective Inhibitor To Define the Chemotherapeutic Potential of the Plasmodial Hexose Transporter in Different Stages of the Parasite's Life Cycle

Slavic

Delves

Prudêncio

et al. 2011

Antimicrob Agents Chemother

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Probing structure/affinity relationships for the Plasmodium falciparum hexose transporter with glucose derivatives

Cited by 13 publications

References 31 publications

Plasmodial sugar transporters as anti-malarial drug targets and comparisons with other protozoa

Plasmodial sugar transporters as anti-malarial drug targets and comparisons with other protozoa

Ferrocene Conjugates of Chloroquine and other Antimalarials: the Development of Ferroquine, a New Antimalarial

Use of a Selective Inhibitor To Define the Chemotherapeutic Potential of the Plasmodial Hexose Transporter in Different Stages of the Parasite's Life Cycle

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