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
-
Structural Characterization of Recombinant Therapeutic Proteins by Circular Dichroism
Current Pharmaceutical Biotechnology Patient, System and Clinician Level Interventions to Address Disparities in Diabetes Care
Current Diabetes Reviews Pharmacological Management of Type 2 Diabetes Mellitus: An Update
Current Diabetes Reviews Effects of Synthetic Peptides on the Inflammatory Response and their Therapeutic Potential
Mini-Reviews in Medicinal Chemistry Epidemiology of Hypertension and Diabetes Mellitus in Latin America
Current Hypertension Reviews Suppression of TLR Signaling by Targeting TIR domain-Containing Proteins
Current Protein & Peptide Science Antisynthetase Syndrome: A Review of Etiopathogenesis, Diagnosis and Management
Current Medicinal Chemistry Accuracy of Ultrasound Imaging Technique for Assessing Lipoatrophy in HIV-Infected Subjects
Current HIV Research Myocardial Infarction with and without ST-segment Elevation: a Contemporary Reappraisal of Similarities and Differences
Current Cardiology Reviews Antioxidant Effects of Natural Bioactive Compounds
Current Pharmaceutical Design Pattern and Correlates of Hypomagnesemia Among Subset of Diabetes Mellitus
Current Diabetes Reviews What Metabolic Syndrome Contributes to Brain Outcomes in African American & Caucasian Cohorts
Current Alzheimer Research Development and Characterization of Spray Dried Microparticles for Pulmonary Delivery of Antifungal Drug
Current Drug Delivery Intrauterine Effects of Impaired Lipid Homeostasis in Pregnancy Diseases
Current Medicinal Chemistry The Role of the ATP-Binding Cassette Transporter P-Glycoprotein in the Transport of β-Amyloid Across the Blood-Brain Barrier
Current Pharmaceutical Design Reliability of Blood Pressure Patterns Defined by a Single 24-Hour Ambulatory Blood Pressure Monitoring: The Case of the Dipping/Non Dipping and Isolated Clinic Hypertension
Current Hypertension Reviews The Diagnostic and Prognostic Value of Brain Natriuretic Peptide and Aminoterminal (nt)-pro Brain Natriuretic Peptide
Current Pharmaceutical Design Liver X Receptor: Crosstalk Node for the Signaling of Lipid Metabolism,Carbohydrate Metabolism, and Innate Immunity
Current Signal Transduction Therapy Human Urotensin II Promotes Hypertension and Atherosclerotic Cardiovascular Diseases
Current Medicinal Chemistry Role of Angiotensin-1-Receptor Blockers In Cardiorenal Disease
Current Drug Therapy