Abstract
Plasma glucose is continuously filtered through the glomerulus and then is reabsorbed via the transcellular transport system of proximal tubules in the kidney. The glucose reabsorption system in the kidney is mediated by sodiumdependent glucose cotransporters (SGLTs). Most of filtered glucose is reabsorbed by the low affinity, high capacity SGLT2 located in the proximal renal tubule. SGLT2 inhibitors, such as T-1095, enhance urinary glucose excretion and consequently lower blood glucose levels independent of insulin action. The principle behind SGLT inhibition involves the amelioration of diabetic conditions without increasing body weight and the risk of hypoglycemia. A number of SGLT2 inhibitors are being developed for the treatment of diabetes. This review offers the summary of structure-activity relationships (SARs) and pharmacological profiles of T-1095 and diverse SGLT2 inhibitors.
Keywords: SGLT, anti-diabetic agent, urinary glucose excretion, diabetes mellitus, phlorizin, T-1095, remogliflozin etabonate, sergliflozin, dapagliflozin
Current Topics in Medicinal Chemistry
Title: Renal Sodium-Dependent Glucose Cotransporter 2 (SGLT2) Inhibitors for New Anti-Diabetic Agent
Volume: 10 Issue: 4
Author(s): Sumihiro Nomura
Affiliation:
Keywords: SGLT, anti-diabetic agent, urinary glucose excretion, diabetes mellitus, phlorizin, T-1095, remogliflozin etabonate, sergliflozin, dapagliflozin
Abstract: Plasma glucose is continuously filtered through the glomerulus and then is reabsorbed via the transcellular transport system of proximal tubules in the kidney. The glucose reabsorption system in the kidney is mediated by sodiumdependent glucose cotransporters (SGLTs). Most of filtered glucose is reabsorbed by the low affinity, high capacity SGLT2 located in the proximal renal tubule. SGLT2 inhibitors, such as T-1095, enhance urinary glucose excretion and consequently lower blood glucose levels independent of insulin action. The principle behind SGLT inhibition involves the amelioration of diabetic conditions without increasing body weight and the risk of hypoglycemia. A number of SGLT2 inhibitors are being developed for the treatment of diabetes. This review offers the summary of structure-activity relationships (SARs) and pharmacological profiles of T-1095 and diverse SGLT2 inhibitors.
Export Options
About this article
Cite this article as:
Nomura Sumihiro, Renal Sodium-Dependent Glucose Cotransporter 2 (SGLT2) Inhibitors for New Anti-Diabetic Agent, Current Topics in Medicinal Chemistry 2010; 10 (4) . https://dx.doi.org/10.2174/156802610790980567
DOI https://dx.doi.org/10.2174/156802610790980567 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |

- Author Guidelines
- Bentham Author Support Services (BASS)
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
- Announcements
Related Articles
-
Phenylbutyric Acid: Simple Structure - Multiple Effects
Current Pharmaceutical Design Vascular Effects of Insulin and Their Relation to Endothelial Dysfunction, Insulin Resistance and Hypertension
Current Hypertension Reviews Docking of Natural Products against Neurodegenerative Diseases: General Concepts
Combinatorial Chemistry & High Throughput Screening Oleic Acid in Olive Oil: From a Metabolic Framework Toward a Clinical Perspective
Current Pharmaceutical Design Efficacy of HGF Gene Transfer for Various Nervous Injuries and Disorders
Central Nervous System Agents in Medicinal Chemistry Patent Selections:
Recent Patents on Endocrine, Metabolic & Immune Drug Discovery (Discontinued) Editorial [Hot topic: Angiogenesis and Lymphangiogenesis in Common Diseases (Guest Editor: Y. Cao)]
Current Molecular Medicine Advances and Barriers in Mammalian Cell Encapsulation for Treatment of Diabetes
Immunology, Endocrine & Metabolic Agents in Medicinal Chemistry (Discontinued) Neurobiology of Sleep Disturbances in Neurodegenerative Disorders
Current Pharmaceutical Design Stem Cells as a Potential Therapeutic Option for Treating Neurodegenerative Diseases
Current Stem Cell Research & Therapy Reappraising the Relationship Between Mitochondrial DNA Variant m.16189T>C and Type 2 Diabetes Mellitus in East Asian Populations
Current Molecular Medicine Does Ceruloplasmin Defend Against Neurodegenerative Diseases?
Current Neuropharmacology Direct Targeting of the Ras GTPase Superfamily Through Structure- Based Design
Current Topics in Medicinal Chemistry Thrombomodulin – A New Target for Treating Stroke at the Crossroad of Coagulation and Inflammation
Current Medicinal Chemistry An Image-based Mouth Switch for People with Severe Disabilities
Recent Patents on Computer Science Antiglycation Activity of Triazole Schiff’s Bases Against Fructosemediated Glycation: In Vitro and In Silico Study
Medicinal Chemistry An Overview of Published Papers and Important Developments in the Past Three Years
Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry Hepatocyte Growth Factor (HGF): Neurotrophic Functions and Therapeutic Implications for Neuronal Injury/Diseases
Current Signal Transduction Therapy Inflammatory Mechanisms and Redox Status in Periodontal and Cardiometabolic Diseases: Effects of Adjunctive Nutritional Antioxidants and Statins
Infectious Disorders - Drug Targets Editorial [Hot Topic: Regulation of Glutamate Synthesis Via Inhibition of Glutamate Carboxypeptidase II (GCPII): An Effective Method to Treat Central and Peripheral Nervous System Disorders (Guest Editors: Guido Cavaletti and Barbara Slusher)]
Current Medicinal Chemistry