ArticleInternational journal of medical sciences2007
Thioglycosides as inhibitors of hSGLT1 and hSGLT2: potential therapeutic agents for the control of hyperglycemia in diabetes.
Article in International journal of medical sciences, 2007. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 papers.
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Who cites it
16 citing papers in PubMed, 75 citations in OpenAlex.
- Plant glycosides and glycosidases: classification, sources, and therapeutic insights in current medicine.Glycoconjugate journal · 2025Review
- Visible-Light-Mediated Synthesis of AnomericMolecules (Basel, Switzerland) · 2025Article
- Novel triple mutant of an extremophilic glycosyl hydrolase enables the rapid synthesis of thioglycosides.Chemical communications (Cambridge, England) · 2022Article
- Visible-Light-Mediated Stadler-Ziegler Arylation of Thiosugars with Anilines.ACS organic & inorganic Au · 2022Article
- Transition-metal-free synthesis of aryl 1-thioglycosides with arynes at room temperature.RSC advances · 2021Article
- Thioglycoligase derived from fungal GH3 β-xylosidase is a multi-glycoligase with broad acceptor tolerance.Nature communications · 2020Article
- 8-Hydroxyquinoline Glycoconjugates Containing Sulfur at the Sugar Anomeric Position-Synthesis and Preliminary Evaluation of Their Cytotoxicity.Molecules (Basel, Switzerland) · 2020Article
- SGLT1 Inhibition Attenuates Apoptosis in Diabetic Cardiomyopathy via the JNK and p38 Pathway.Frontiers in pharmacology · 2020Article
- Glycosylation in health and disease.Nature reviews. Nephrology · 2019Review
- What does sodium-glucose co-transporter 1 inhibition add: Prospects for dual inhibition.Diabetes, obesity & metabolism · 2019 · on this mapReview
- Convergent Synthesis of N,S-bis Glycosylquinolin-2-ones via a Pd-G3-XantPhos Precatalyst Catalysis.Molecules (Basel, Switzerland) · 2018Article
- Spotlight on ertugliflozin and its potential in the treatment of type 2 diabetes: evidence to date.Drug design, development and therapy · 2017Review
- Sodium glucose cotransporter SGLT1 as a therapeutic target in diabetes mellitus.Expert opinion on therapeutic targets · 2016Review
- Forces and dynamics of glucose and inhibitor binding to sodium glucose co-transporter SGLT1 studied by single molecule force spectroscopy.The Journal of biological chemistry · 2014Article
- Emerging treatment options for type 2 diabetes.British journal of clinical pharmacology · 2010Review
- Turning glucosuria into a therapy: Efficacy and safety with SGLT2 inhibitors.Current diabetes reports · 2010Review
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Authors and funding
4 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The treatment of diabetes has been mainly focused on maintaining normal blood glucose concentrations. Insulin and hypoglycemic agents have been used as standard therapeutic strategies. However, these are characterized by limited efficacy and adverse side effects, making the development of new therapeutic alternatives mandatory. Inhibition of glucose reabsorption in the kidney, mediated by SGLT1 or SGLT2, represents a promising therapeutic approach. Therefore, the aim of the present study was to evaluate the effect of thioglycosides on human SGLT1 and SGLT2. For this purpose, stably transfected Chinese hamster ovary (CHO) cells expressing human SGLT1 and SGLT2 were used. The inhibitory effect of thioglycosides was assessed in transport studies and membrane potential measurements, using alpha-methyl-glucoside uptake and fluorescence resonance energy transfer, respectively. We found that some thioglycosides inhibited hSGLT more strongly than phlorizin. Specifically, thioglycoside I (phenyl-1'-thio-beta-D-glucopyranoside) inhibited hSGLT2 stronger than hSGLT1 and to a larger extent than phlorizin. Thioglycoside VII (2-hydroxymethyl-phenyl-1'-thio-beta-D-galacto-pyranoside) had a pronounced inhibitory effect on hSGLT1 but not on hSGLT2. Kinetic studies confirmed the inhibitory effect of these thioglycosides on hSGLT1 or hSGLT2, demonstrating competitive inhibition as the mechanism of action. Therefore, these thioglycosides represent promising therapeutic agents for the control of hyperglycemia in patients with diabetes.
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