The role of transporter ectodomains in drug recognition and binding: phlorizin and the sodium–glucose cotransporter

Raja, Mobeen; Puntheeranurak, Theeraporn; Gruber, Hermann J.; Hinterdorfer, Peter; Kinne, Rolf

doi:10.1039/c5md00572h

Cited by 2 publications

(1 citation statement)

References 60 publications

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“…The software program MOE Dock (Version 2022.02) was utilized to perform molecular docking between monosaccharides and MoHXT2 in order to predict sites playing critical roles in their binding affinity. Monosaccharides, as well as their inhibitor phlorizin dihydrate, were designated as ligands, while MoHXT2 served as the target molecule [26] (Table S3). The 2D structures of all four molecules were transformed into 3D structures via energy minimization.…”

Section: Modeling and Docking Of Mohxt2 And Hexosesmentioning

confidence: 99%

Influence of Two Hexose Transporters on Substrate Affinity and Pathogenicity in Magnaporthe oryzae

Huang,

Guo,

Luo

et al. 2024

Microorganisms

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Hexose transporters (HXT) play a crucial role in the pathogenicity of Magnaporthe oryzae, serving not only as key facilitators for acquiring and transporting sugar nutrients to support pathogen development, but also as sugar sensors which receive transduction signals. The objective of this study is to investigate the impact of MoHXT1-3 on rice pathogenicity and hexose affinity. MoHXT1-3 deletion mutants were generated using CRISPR/Cas9 technology, and their affinity for hexose was evaluated through yeast complementation assays and electrophysiological experiments in Xenopus oocytes. The results suggest that MoHXT1 does not contribute to melanin formation or hexose transportation processes. Conversely, MoHXT2, despite displaying lower affinity towards the hexoses tested in comparison to MoHXT3, is likely to have a more substantial impact on pathogenicity. The analysis of the transcription profiles demonstrated that the deletion of MoHXT2 caused a decrease in the expression of MoHXT3, whereas the knockout of MoHXT3 resulted in an upregulation of MoHXT2 transcription. It is noteworthy that the MoHXT2M145K variant displayed an incapacity to transport hexoses. This investigation into the functional differences in hexose transporters in Magnaporthe oryzae provides insights into potential advances in new strategies to target hexose transporters to combat rice blast by blocking carbon nutrient supply.

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Section: Modeling and Docking Of Mohxt2 And Hexosesmentioning

confidence: 99%

Influence of Two Hexose Transporters on Substrate Affinity and Pathogenicity in Magnaporthe oryzae

Huang,

Guo,

Luo

et al. 2024

Microorganisms

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Design, synthesis and biological evaluation of 6-deoxy O-spiroketal C-arylglucosides as novel renal sodium-dependent glucose cotransporter 2 (SGLT2) inhibitors for the treatment of type 2 diabetes

Wang

Lou

Wang

et al. 2019

European Journal of Medicinal Chemistry

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The role of transporter ectodomains in drug recognition and binding: phlorizin and the sodium–glucose cotransporter

Abstract: This article reviews the role of segments of SLCs located outside the plasma membrane bilayer (ectodomains) using the inhibition of SGLTs (SLC5 family) by the aromatic glucoside phlorizin as a model system.

Cited by 2 publications

References 60 publications

Influence of Two Hexose Transporters on Substrate Affinity and Pathogenicity in Magnaporthe oryzae

Influence of Two Hexose Transporters on Substrate Affinity and Pathogenicity in Magnaporthe oryzae

Design, synthesis and biological evaluation of 6-deoxy O-spiroketal C-arylglucosides as novel renal sodium-dependent glucose cotransporter 2 (SGLT2) inhibitors for the treatment of type 2 diabetes

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