Related Experiment Video
Updated: Jan 14, 2026
10:29
Quantitative Structure-Activity Relationship, Activity Prediction, and Molecular Dynamics of Non-nucleotide Reverse Transcriptase Inhibitors
Published on: May 9, 2025
2.2K
An Insight Into Commercially Available SGLT2 Inhibitors and Their Structure-Activity Relationship Studies.
Asiya Parveen1, Shazia Parveen2, Nisha Vats1
1Department of Pharmaceutical Chemistry, School of Pharmaceutical Education and Research, Jamia Hamdard, New Delhi, India.
Archiv Der Pharmazie
|October 24, 2025
Summary
Sodium-glucose co-transporter 2 (SGLT-2) inhibitors offer a novel approach to managing type 2 diabetes. These gliflozins reduce blood glucose by preventing kidney glucose reabsorption, addressing the need for safer antidiabetic treatments.
Area of Science:
- Pharmacology
- Endocrinology
- Nephrology
Background:
- Type 2 diabetes mellitus is a growing global health concern.
- Current anti-hyperglycemic medications have limitations, necessitating safer and more effective treatments.
- Insulin deficiency or resistance characterizes type 2 diabetes, a chronic condition requiring continuous management.
Purpose of the Study:
- To review sodium-glucose co-transporter 2 (SGLT-2) inhibitors as a novel therapeutic class for type 2 diabetes.
- To explore the characteristics, mechanism of action, and therapeutic applications of gliflozins.
- To provide an overview of SGLT-2 inhibitors approved by major regulatory bodies.
Main Methods:
- Literature review focusing on SGLT-2 inhibitors.
- Analysis of drug design, development, and structure-activity relationships.
- Examination of regulatory approvals (FDA, EMA, PMDA).
Main Results:
- SGLT-2 inhibitors represent a significant advancement in managing type 2 diabetes.
- These agents lower blood glucose by inhibiting glucose reabsorption in the kidneys.
- Approved gliflozins demonstrate efficacy and offer an alternative to existing therapies.
Conclusions:
- SGLT-2 inhibitors are a valuable addition to the antidiabetic treatment arsenal.
- Their unique mechanism offers potential benefits beyond glycemic control.
- Further research into their therapeutic applications and long-term effects is warranted.
Related Concept Videos
01:27Glucose Transporters
27.2K
Glucose transporters facilitate the transport of glucose across the cell membrane. In addition to glucose, some glucose transporters can also aid the movement of other hexoses such as fructose, mannose, and galactose.
Facilitated diffusion-glucose transporters (GLUTs) are encoded by the solute-linked carrier (SLC) family 2, subfamily A gene family, or SLC2A. The 14 GLUT protein members are distributed into three classes:
Facilitated diffusion-glucose transporters (GLUTs) are encoded by the solute-linked carrier (SLC) family 2, subfamily A gene family, or SLC2A. The 14 GLUT protein members are distributed into three classes:
27.2K
01:28Structure-Activity Relationships and Drug Design
1.7K
Drug design is a dynamic field that involves discovering and developing new medications based on specific biological targets. This process heavily relies on structure-activity relationships (SAR) and quantitative structure-activity relationships (QSAR) to guide the design and optimization of efficient drugs.
SAR studies the intricate relationship between a drug's chemical structure and biological activity. It focuses on understanding how modifications to a drug's structure can influence...
SAR studies the intricate relationship between a drug's chemical structure and biological activity. It focuses on understanding how modifications to a drug's structure can influence...
1.7K
01:24Glucagon-like Receptor Agonists
840
Incretins include glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP), which stimulate insulin secretion post-meals. In type 2 diabetes, GIP's efficacy is reduced, making GLP-1 a viable drug target. GIP originates from preproGIP.
GLP-1, when administered in high doses intravenously, triggers insulin secretion, inhibits glucagon release, slows gastric emptying, reduces food intake, and restores normal insulin secretion. However, its rapid inactivation by...
GLP-1, when administered in high doses intravenously, triggers insulin secretion, inhibits glucagon release, slows gastric emptying, reduces food intake, and restores normal insulin secretion. However, its rapid inactivation by...
840
01:23Dipeptidyl Peptidase 4 Inhibitors
581
Dipeptidyl peptidase 4 (DPP-4) is a serine protease widely distributed in the body. It's involved in the inactivation of GLP-1 and GIP hormones, which are crucial for insulin regulation. DPP-4 inhibitors, such as sitagliptin (Januvia), saxagliptin (Onglyza), linagliptin (Tradjenta), alogliptin (Nesina), and vildagliptin (Galvus), help increase the proportion of active GLP-1, enhancing insulin secretion. These inhibitors work by competitively binding to DPP-4. This binding causes a...
581
00:49Ligand Binding and Linkage
5.5K
Allosteric proteins have more than one ligand binding site; the binding of a ligand to any of these sites influences the binding of ligands to the other sites. When a protein is allosteric, its binding sites are called coupled or linked. In the case of enzymes, the site that binds to the substrate is known as the active site and the other site is known as the regulatory site. When a ligand binds to the regulatory site, this leads to conformational changes in the protein that can influence...
5.5K
01:06Oral Hypoglycemic Agents: Glinides
595
Repaglinide (Prandin) and Nateglinide (Starlix), known as glinides, are oral insulin secretagogues that stimulate insulin release from pancreatic β cells by closing the ATP-sensitive potassium channels (KATP channel). Repaglinide controls insulin release from pancreatic β cells by managing potassium efflux. It shares two binding sites with sulfonylureas and also has a unique site, indicating overlapping mechanisms of action. With a rapid onset and a 4-7 hour duration, it effectively...
595