Role and molecular mechanisms of SGLT2 inhibitors in pathological cardiac remodeling (Review)

Bixian Chen1, Jing Guo1, Hongmei Ye1

  • 1Department of Pharmacy, Peking University People's Hospital, Beijing 100044, P.R. China.

PubMed

Insights

Sodium-glucose cotransporter type 2 inhibitors (SGLT2is) show cardiac benefits by preventing pathological cardiac remodeling. This review explores SGLT2is mechanisms in heart failure, guiding future drug target development.

Area of Science:

  • Cardiology
  • Pharmacology
  • Molecular Biology

Background:

  • Cardiovascular diseases stem from pathological cardiac remodeling, including fibrosis, inflammation, and cell dysfunction, leading to heart failure.
  • Sodium-glucose cotransporter type 2 inhibitors (SGLT2is), initially for type 2 diabetes, demonstrate significant cardiac benefits in clinical trials.
  • SGLT2is are now recognized in heart failure guidelines, highlighting their therapeutic importance beyond glycemic control.

Conclusions:

  • SGLT2is represent a crucial therapeutic strategy for preventing and managing heart failure by targeting pathological cardiac remodeling.
  • Further investigation into the detailed mechanisms of SGLT2is is warranted for optimizing their use and developing new therapies.
  • Understanding these mechanisms can lead to the identification of novel therapeutic targets for cardiovascular diseases.

Related Concept Videos

Heart Failure Drugs: Inhibitors of Renin-Angiotensin System01:26

Heart Failure Drugs: Inhibitors of Renin-Angiotensin System

The activation of the sympathetic nervous system and the renin-angiotensin-aldosterone system (RAAS) contributes to cardiac remodeling, and inhibiting the RAAS is a pharmacological target in heart failure management. As a result, neurohumoral modulation is a crucial treatment principle for managing heart failure. This approach involves using medications like ACE inhibitors (ACEIs), angiotensin receptor blockers (ARBs), β-blockers, mineralocorticoid receptor antagonists (MRAs), and neutral...
428
Glucose Transporters01:27

Glucose Transporters

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:
22.7K
Secondary Active Transport01:32

Secondary Active Transport

One example of how cells use the energy contained in electrochemical gradients is demonstrated by glucose transport into cells. The ion vital to this process is sodium (Na+), which is typically present in higher concentrations extracellularly than in the cytosol. Such a concentration difference is due, in part, to the action of an enzyme "pump" embedded in the cellular membrane that actively expels Na+ from a cell. Importantly, as this pump contributes to the high concentration of...
7.0K
Glucose Absorption Into the Small Intestine01:26

Glucose Absorption Into the Small Intestine

Complex carbohydrates consumed cannot be absorbed into the small intestine in their original form. First, they must be hydrolyzed to a monosaccharide form such as glucose or galactose. These monosaccharides are then transported across the intestinal membrane and into the blood via transcellular transport. The intestinal epithelial cells allow the movement of these monosaccharides with a defined 'entry' through membrane transporter proteins present on their apical membrane and...
31.6K
Oral Hypoglycemic Agents: Biguanides and Glitazones01:26

Oral Hypoglycemic Agents: Biguanides and Glitazones

Biguanides, particularly metformin (Glucophage), are insulin sensitizers that enhance glucose uptake, thereby reducing insulin resistance. Unlike sulfonylureas, metformin doesn't prompt insulin secretion, which helps to curb hypoglycemia risk. Metformin is beneficial in treating conditions like polycystic ovary syndrome due to its insulin-resistance reduction capability. The drug's primary action involves curtailing hepatic gluconeogenesis, a significant contributor to high blood...
199
Transducer Mechanism: Enzyme-Linked Receptors01:27

Transducer Mechanism: Enzyme-Linked Receptors

Enzyme-linked receptors are cell-surface receptors acting as an enzyme or associating with an enzyme intracellularly. They make excellent drug targets. Drugs can bind to the extracellular ligand-binding domain or directly affect their enzymatic domain and alter their activity.
Major types that are helpful drug targets include:
2.5K