Targeting Sodium-Glucose Cotransporter for Developing Anti-Obesity Therapeutics
InquiryOverview
Obesity is a disorder disease of metabolism that is regulated by multiple factors. With the in-depth study of various pathophysiological mechanisms of obesity, more and more targets are being screened to develop anti-obesity therapies, such as Melanocortin 4 Receptor, Serotonin Receptor, Cannabinoid Receptor, Sodium-glucose cotransporter Receptor (SGLT), etc. SGLT is involved in glucose transport, including intestinal glucose uptake through the apical membrane and glucose transport through the basolateral membrane to the blood. Inhibition of SGLT-1 reduces blood glucose concentration in animals and provides some antidiabetic and weight loss effects. Blockade of SGLT-2 protein in proximal tubules induces glucose-mediated osmotic diuresis and sodium excretion and improves a variety of metabolic indices. Based on these studies, SGLT is a potential target for the treatment of obesity.
At Protheragen, our research team brings together scientists from various fields, including biopharmaceuticals, pathology research, etc., who have been working for years to find innovative and efficient anti-obesity therapies. We provide a customized SGLT-targeting anti-obesity therapeutic development service to support our clients' studies.
Explore More Efficient SGLT-Targeting Anti-Obesity Therapies with Us
Our goal is to develop anti-obesity therapies targeting SGLT with higher efficacy. Our team has deep scientific knowledge and years of experience in obesity research, translating deeper expertise and experience into reliable service support. Specific services include the following:
Anti-Obesity Drug Development
We screen or synthesize various natural products and other types of compounds. Then their inhibitory activity against SGLT, in vivo hypoglycaemic, and anti-obesity effects are evaluated.
Computer-aided Drug Design: The rapid development of bioinformatics tools makes it possible to predict the binding affinity between SGLT and potential anti-obesity drugs. We combine advanced analytical tools for the rational design of anti-obesity drugs targeting SGLT, including Molecular Docking, molecular dynamics simulation, etc. Our team designs and optimizes anti-obesity drug molecules by predicting whether the target substance binds to SGLT and its binding strength. We also computationally assess the drug-likeness, absorption, distribution, metabolism, excretion, toxicity, and other properties of potential anti-obesity drugs, and eliminate unsuitable compounds to accelerate the process of anti-obesity drug research.
SGLT-2 inhibitors: It is found that SGLT-2 inhibitors not only lower glucose but also play a role in weight loss and lipid regulation. It reduces the ratio of insulin to glucagon, thereby increasing hepatic glycogenolysis and gluconeogenesis. SGLT-2 inhibitors are potential anti-obesity drugs. We synthesize SGLT-2 inhibitors and conduct relevant preclinical studies.
SGLT-1 inhibitors: Natural products have been shown to inhibit SGLT-1 activity, thereby exerting a blood glucose-lowering effect. We also screen natural products and other types of compounds that inhibit SGLT-1 and evaluate their potential in the treatment of obesity.
Combination therapies: Combination therapies are effective in treating obesity in obesity models. We develop combination therapies that target SGLT and other targets. Two or more drugs with different mechanisms of action are administered and their effects on the pathology and physiology of animal models are evaluated.
Preclinical Studies of Anti-Obesity Therapies
Preclinical studies of our anti-obesity therapies include in vitro and in vivo experiments. In vitro experiments include the effects of SGLT inhibitors on cellular glucose uptake. In vivo experiments include studying the anti-obesity effects of SGLT inhibitors using various animal models, including physiology, blood sample testing, expression assays of pathway targets, and other analyses. The pharmacokinetic and pharmacodynamic profiles of different anti-obesity drugs vary and are suitable for different types of drug administration routes. We use the appropriate route of administration (oral, intravenous, subcutaneous, etc.) to analyze the absorption, bioavailability, etc., of the anti-obesity drug. In addition to this, we also evaluate the safety of this anti-obesity therapy.
Workflow
Applications
- The development of anti-obesity therapies targeting SGLT helps advance research on obesity intervention strategies.
- SGLT-2 inhibitors have an important potential in the treatment of diabetes by lowering blood glucose concentration through increasing urinary glucose excretion.
- Increasing evidence suggests that SGLT-2 inhibitors have potential in the treatment of cardiovascular disease by controlling blood glucose and lowering body mass index. The development of anti-obesity therapies targeting SGLT helps advance research on therapeutic strategies for cardiovascular disease.
Advantages
- We provide a one-stop service for anti-obesity therapeutic development from project initiation, computer simulation, SGLT inhibitor synthesis, and preclinical studies to data analysis.
- With the help of cheminformatics software and advanced modeling, we perform comprehensive computer-aided drug design to accelerate the development of anti-obesity drugs targeting SGLT.
- In addition to detailed data analysis reports, we provide ongoing after-sales and research support.
Our Featured Services to Support Obesity Research
We are committed to turning rigorous scientific analysis into a solid foundation for obesity mechanism research and anti-obesity therapy development. To achieve this goal, we have crafted a one-stop full-service system, covering in-depth obesity analysis, precise diagnostic tests, personalized risk assessment, obesity prediction, microbiome analysis, pathology testing, gene editing, and so on. In addition, we also provide weight loss and weight management services based on our in-depth exploration of the pathogenesis of obesity and the structure of the gut microbiome.
Publication
Technology: Quantitative real-time polymerase chain reaction, Western blotting
Journal: International Journal Of Molecular Sciences
IF: 4.183
Published: 2018
Results: SGLT2 inhibitors are a class of drugs that exert anti-obesity and anti-diabetic effects by promoting glucose excretion and calorie loss. In this study, the researchers analyzed the effects of dapagliflozin, a highly selective renal SGLT2 inhibitor, on diet-induced obese mice. It was found that dapagliflozin attenuated the increase in body weight, body mass, plasma triglycerides, and blood glucose in Western diet-fed mice. The collagen IV, synaptophysin, fibronectin immunofluorescence microscopy, etc., revealed that dapagliflozin treatment prevented renal fibrosis, glomerular pathological changes, and podocyte damage. It also reduced renal lipid accumulation. The results of this study demonstrate the potential of SGLT2 inhibitors in the treatment of obesity, renal diseases, and liver-related diseases.
Fig.1 Effect of dapagliflozin administration on food intake and body weight. (Wang, et al., 2018)
Frequently Asked Questions
What complications can obesity cause?
Obesity is a multifactorial disease that adversely affects the functioning of several organ systems and leads to abnormal hormonal and molecular changes. It has been found to increase the risk of cardiovascular disease, sleep disorders, diabetes mellitus, hypertension, dyslipidemia, neurological disorders, and many types of cancer. Research on anti-obesity therapies helps to advance research on interventions and treatments for these complications.
What is the relationship between SGLT and obesity?
SGLT2 is an important transporter that controls glucose reabsorption in the kidneys. SGLT2 inhibitors not only increase urinary glucose excretion and thus control blood glucose, but also lower blood pressure and thus provide cardiovascular protection. SGLT1 is a major transporter for glucose absorption in the intestine. Its expression is regulated by gastrointestinal hormones such as glucagon-like peptide-1, and interacts with taste receptors to influence human feeding behavior and appetite, thus participating in the pathogenesis of obesity.
Protheragen offers a full range of anti-obesity therapeutic development services targeting SGLT based on our in-depth understanding of the underlying pathophysiology of obesity. Welcome to contact us to explore innovative anti-obesity therapeutic options with us. We are ready to answer your questions and provide service support at any time.
Reference
- Wang, D.; et al. The sodium-glucose cotransporter 2 inhibitor dapagliflozin prevents renal and liver disease in western diet induced obesity mice. International journal of molecular sciences. 2018, 19(1): 137.
All of our services and products are intended for preclinical research use only and cannot be used to diagnose, treat or manage patients.