Targeting Glucagon Receptor (GCGR) for Developing Anti-Obesity Therapeutics
InquiryOverview
GCGR is expressed primarily in the liver, followed by the kidneys, heart, adipose tissue, pancreatic islets, and central nervous system. It is the largest family of membrane proteins in the human body and promotes glycogenolysis and gluconeogenesis via glucagon, thereby maintaining blood glucose levels. Based on its role in the regulation of energy balance, maintenance of glucose homeostasis, and metabolic function, GCGR is a key therapeutic target for diabetes and obesity. It also regulates key physiological functions through the peptide hormones Glucagon-like Peptide-1 (GLP-1), and Gastric Inhibitory Polypeptide (GIP). Therefore, targeting these receptors, therapies such as GCGR agonists, dual agonists, and triple agonists have been developed, which have good potential for application in the treatment of obesity diabetes, and other complications. Protheragen combines a variety of cutting-edge technologies and tools to provide a high-quality GCGR-targeting anti-obesity therapeutic development service. Our research team has extensive experience in GCGR, bioengineered pharmaceuticals, etc., and provides innovative solutions to advance anti-obesity therapeutic research targeting this receptor.
Exploring GCGR-Targeting Anti-Obesity Therapies Together at Protheragen
Anti-obesity therapy development service targeting GCGR includes computer-aided drug design, synthesis of anti-obesity drugs, and preclinical studies. We have rigorous quality control processes in place to ensure the highest quality of anti-obesity therapy development project results. Specific services include the following:
Anti-Obesity Drug Development
We have a variety of techniques to synthesize anti-obesity drugs targeting GCGR with potential therapeutic properties, such as genetic engineering, fully synthetic techniques, semi-synthetic techniques, etc. We support anti-obesity therapeutic research through the development of potent GCGR agonists.
- GCGR agonists: GCGR activation helps to increase metabolic rate and increase thermogenic activity to complement the therapeutic effects of other anti-obesity drugs that reduce body weight through appetite suppression. Drawing on our deep research into obesity and biopharmaceuticals, we develop a variety of GCGR agonists and evaluate their efficacy and safety in the treatment of obesity.
- Dual agonists: GLP-1 receptor (GLP-1R)/GCGR co-agonists have been found to have good potential in the treatment of obesity. On the one hand, it activates GCGR to promote lipid metabolism and reduce body weight. On the other hand, it activates GLP-1R to promote insulin secretion and lower blood glucose. We synthesize GLP-1R/GCGR co-agonists and investigate their receptor targeting, in vitro functional agonism, and in vivo anti-obesity effects.
- Triple agonists: Single molecule drugs that target multiple targets have been developed for the treatment of obesity and its related complications. Single-molecule triple agonists targeting insulin, GLP-1, and GCGR have been synthesized by click chemistry, which is useful in glycemic control and weight loss. We use various techniques to synthesize triple agonists targeting GCGR and other receptors. Then we use obesity models to evaluate their pharmacokinetic (PK) profiles and potential for the treatment of obesity.
Preclinical Studies of Anti-Obesity Therapies
We construct a variety of Obesity Models to support preclinical studies of anti-obesity therapies, including various In Vivo (Rat, Mouse, Pig, etc.) and In Vitro Models. Based on a variety of state-of-the-art instruments, we conduct a comprehensive evaluation of the therapeutic and toxicological effects of anti-obesity therapies targeting GCGR after defining the needs of the assays. Not only its functional efficacy in vitro is evaluated, but also its PK and pharmacodynamics through different dosing regimens, and the safety of this therapy is assessed. Through the testing of glucose tolerance, gene expression profiles, etc., in animal models, we deeply analyze the mechanism of action of this anti-obesity therapy.
Obesity models | Evaluation of obesity therapies |
---|---|
|
Workflow
We are committed to innovation and utilize a wealth of cutting-edge research methodologies to pursue a variety of potential anti-obesity drugs targeting GCGR.
Applications
- The development of anti-obesity therapies targeting GCGR provides theoretical support for research into methods of treating other metabolic diseases.
- GCGR has a crucial role in controlling blood glucose levels. Defects in this gene are a cause of the pathogenesis of non-insulin-dependent diabetes. Research on anti-obesity drugs targeting GCGR provides valuable information for the development of potential drugs for the treatment of diabetes.
- The development of anti-obesity therapies targeting GCGR provides theoretical support for research into more effective combination approaches to treating obesity.
Advantages
- Our team consists of highly skilled scientists and experts in the field of GCGR research and drug development. Their extensive knowledge and experience provide high-quality results.
- We provide customized solutions based on our client's specific needs and research objectives, from early computer simulations to final preclinical studies.
- Based on state-of-the-art technology and extensive hands-on experience, our research work on targeted GCGR anti-obesity therapies is highly efficient.
What are Our Specialty Services?
Our team specializes in obesity research and anti-obesity therapeutic innovation and provides cutting-edge solutions and comprehensive support. We analyze obesity risk by combining genetic, environmental factors, etc., and multiple technologies for diagnostic testing and obesity prediction. Obesity biomarkers and microbiomes are analyzed to provide reliable insights into the molecular mechanisms of obesity. We also utilize proficient gene editing technology to help model and develop anti-obesity therapies. Personalized weight loss and weight management are also our areas of expertise.
Publication
Technology: Microwave-assisted solid-phase peptide synthesis (SPPS)
Journal: Molecular Metabolism
IF: 8.1
Published: 2022
Results: BI 456906 is a novel GCGR/GLP-1R dual agonist. In this study, the researchers analyzed the functional agonism of BI 456906 in vitro and conducted in vivo pharmacological studies with different dosing regimens. Its in vivo binding to both receptors was demonstrated by glucose tolerance, food intake, gastric emptying tests, and gene expression profiling. It was also found that BI 456906 exerted anti-obesity effects by reducing food intake and increasing energy expenditure after administration.
Fig.1 Improvement of glucose tolerance, delayed gastric emptying, and reduced food intake after a single administration of BI 456906. (Zimmermann, et al., 2022)
Frequently Asked Questions
What are the advantages of multi-targeted drugs in the treatment of obesity research?
Multi-target drugs act on multiple targets that are intrinsically linked to obesity. The synergistic effect of target modulation makes the total effect of such drugs in treating obesity greater than the sum of the individual effects, resulting in better efficacy and fewer adverse effects.
What are the strategies to synthesize potential anti-obesity drugs targeting GCGR?
- Genetic engineering technology: This technique introduces different gene fragments into host cells, which are expressed and purified to obtain the target product.
- Total synthesis technology: This technique involves chemical synthesis (solid phase synthesis, etc.) and modification to obtain the target product.
- Semi-synthetic technology: This technology combines gene editing with modification to obtain the target product.
Protheragen remains at the forefront of obesity research and provides a one-stop service for the development of anti-obesity therapies targeting GCGR. Our goal is to provide high-quality services that advance our clients' research at all stages. Welcome to contact us if you are interested in this area or have specific research needs.
Reference
- Zimmermann, T.; et al. BI 456906: discovery and preclinical pharmacology of a novel GCGR/GLP-1R dual agonist with robust anti-obesity efficacy. Molecular metabolism. 2022, 66: 101633.
All of our services and products are intended for preclinical research use only and cannot be used to diagnose, treat or manage patients.