Abstract
The kidney plays an important role in the regulation of plasma glucose. It is estimated that greater than 99% of the renal glucose filtered by kidney glomerulus is resorbed by sodium-dependent glucose co-transporters (SGLTs), and that SGLT2 located in the proximal renal tubule achieves the most of this assignment. Studies of SGLT2 inhibitors indicate that raising renal glucose excretion by inhibiting SGLT2 helps effectively normalize the plasma glucose levels in individuals with type 2 diabetes mellitus (T2DM). This review discusses the discovery of SGLT2 inhibitors and the related structure-activity relationship (SAR) studies. The clinical trial data of dapagliflozin is also involved.
Keywords: Dapagliflozin, phlorizin, sodium-dependent glucose co-transporter, structure-activity relationships, type 2 diabetes mellitus, regulation of plasma glucose, SGLT2 inhibitors, relatedstructure-activity relationship, insulin deficiency
Current Topics in Medicinal Chemistry
Title: Development of Sodium-Dependent Glucose Co-Transporter 2 Inhibitors as Potential Anti-Diabetic Therapeutics
Volume: 11 Issue: 12
Author(s): Low-Tone Ho, Suvarn S. Kulkarni and Jinq-Chyi Lee
Affiliation:
Keywords: Dapagliflozin, phlorizin, sodium-dependent glucose co-transporter, structure-activity relationships, type 2 diabetes mellitus, regulation of plasma glucose, SGLT2 inhibitors, relatedstructure-activity relationship, insulin deficiency
Abstract: The kidney plays an important role in the regulation of plasma glucose. It is estimated that greater than 99% of the renal glucose filtered by kidney glomerulus is resorbed by sodium-dependent glucose co-transporters (SGLTs), and that SGLT2 located in the proximal renal tubule achieves the most of this assignment. Studies of SGLT2 inhibitors indicate that raising renal glucose excretion by inhibiting SGLT2 helps effectively normalize the plasma glucose levels in individuals with type 2 diabetes mellitus (T2DM). This review discusses the discovery of SGLT2 inhibitors and the related structure-activity relationship (SAR) studies. The clinical trial data of dapagliflozin is also involved.
Export Options
About this article
Cite this article as:
Ho Low-Tone, S. Kulkarni Suvarn and Lee Jinq-Chyi, Development of Sodium-Dependent Glucose Co-Transporter 2 Inhibitors as Potential Anti-Diabetic Therapeutics, Current Topics in Medicinal Chemistry 2011; 11 (12) . https://dx.doi.org/10.2174/156802611795860915
DOI https://dx.doi.org/10.2174/156802611795860915 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
- Author Guidelines
- 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
-
1-Deoxynojirimycin and its Derivatives: A Mini Review of the Literature
Current Medicinal Chemistry Role of NUCB2/nesfatin-1 in Glucose Control: Diverse Functions in Islets, Adipocytes and Brain
Current Pharmaceutical Design The Impact of Substance P on the Pathogenesis of Insulin Resistance Leading to Gestational Diabetes
Current Pharmaceutical Biotechnology Polymorphisms at the LDLR Locus may be Associated with Ischemic Cerebrovascular Disease Independent of Lipid Profile
Current Neurovascular Research Editorial: Natural Compounds and Their Derivatives as a Source of Promising Drugs for Diabetes and Insulin Resistance
Current Drug Targets Type 1 Diabetes Treatments Based on Stem Cells
Current Diabetes Reviews Molecular Dissection of Renal Ischemia-Reperfusion: Oxidative Stress and Cellular Events
Current Medicinal Chemistry Safety of Dipeptidyl Peptidase 4 Inhibitors for Treatment of Type 2 Diabetes
Current Drug Safety The Clinical Genetics of Psoriasis
Current Genomics Different Concepts of Drug Delivery in Disease Entities
Mini-Reviews in Medicinal Chemistry Editorial: Statins and Tissue Plasminogen Activator for Stroke: A Beneficial Combination?
Current Vascular Pharmacology Factors Affecting Residual Platelet Aggregation in Prasugrel Treated Patients
Current Pharmaceutical Design Prediction and Diagnosis of Post Transplant Diabetes
Current Diabetes Reviews Nanomedicine against Alzheimer’s and Parkinson’s Disease
Current Pharmaceutical Design Vascular Effects of Estrogenic Menopausal Hormone Therapy
Reviews on Recent Clinical Trials Effects of Long-Term Intraperitoneal Injection of Thyrotropin-Releasing Hormone (TRH) on Aging- and Obesity-Related Changes in Body Weight, Lipid Metabolism, and Thyroid Functions
Current Aging Science Endocannabinoid Receptor Antagonists and Other Emerging Pharmacological Strategies for Weight Reduction
Current Drug Targets - Cardiovascular & Hematological Disorders Thienocinnolinone Alkanoic Acid Derivatives as Aldose Reductase Inhibitors
Medicinal Chemistry Insulin Resistance and Postprandial Hyperglycemia the Bad Companions in Natural History of Diabetes: Effects on Health of Vascular Tree
Current Diabetes Reviews Protein-Tyrosine Phosphatase 1B (PTP1B): A Novel Therapeutic Target for Type 2 Diabetes Mellitus, Obesity and Related States of Insulin Resistance
Current Drug Targets - Immune, Endocrine & Metabolic Disorders