Targeting Exendin for Developing Anti-Obesity Therapeutics
InquiryOverview
Glucagon-like peptide-1 (GLP-1) binds to its receptor to exert a variety of actions, including inhibiting glucagon production, stimulating insulin production, reducing food consumption, and delaying gastric emptying. It has been used to develop anti-obesity therapies. Exendin-4, a peptide hormone with 53% homology to naturally occurring GLP-1, has been used in a variety of therapeutic studies for the treatment of obesity and type 2 diabetes. However, the short half-life of exendin-4 limits its use in the treatment of obesity. It needs to be optimized to improve its efficacy and safety.
Protheragen remains at the forefront of anti-obesity therapeutic research and offers an innovative anti-obesity therapeutic development service targeting exendin-4. Our services combine a deep understanding of obesity-related biology, cutting-edge pharmacology, and proprietary technologies to create targeted and highly effective treatments.
Your Best Partner for Developing Anti-Obesity Therapy
Our team of experienced scientists, researchers, and pharmaceutical professionals ensures the development of safe and effective treatments. Specific services include the following:
Anti-Obesity Therapy Development
Modification of exendin-4 has emerged as an effective means to improve the efficacy of obesity treatment, extend half-life, and reduce adverse effects. Based on our deep understanding of the molecular mechanisms of exendin-4 and obesity, we primarily use the following strategies to develop novel anti-obesity drugs:
Modification of exendin-4
Modification of Exendin-4 is an effective way to enhance its anti-obesity therapeutic efficacy and application potential. Exendin-4 analogs have been developed to study the potential of treating obesity symptoms. We use a variety of means to modify the molecular structure of exendin-4, such as non-covalent binding and gene fusion. The modifications are used to extend the half-life, improve degradation resistance, reduce immunogenicity, and decrease adverse effects. We have the experience to ensure that a wide range of exendin-4 modification needs are met.
Development of dual agonists
Integrating exendin-4 with other compounds that have synergistic effects into single-molecule drugs is a potential strategy for the treatment of obesity. It has been demonstrated that the fusion of exendin-4 and fibroblast growth factor 21 (FGF21) has great potential for the treatment of obesity. Based on our well-established protein production system, we also develop dual agonists against multiple targets and analyze the in vivo and in vitro anti-obesity activity and pharmacokinetic (PK) of the fusion proteins.
Preclinical Validation
Based on multiple types of obesity models, we evaluate the pharmacological and PK properties of the developed anti-obesity drugs in vivo and in vitro. In addition to this, we also perform other bioassays and safety assessments. The therapeutic potential of anti-obesity drugs is rapidly evaluated under the guidance of an experienced preclinical research team.
- Obesity Model: We have a wide range of obesity models, including various In Vivo (Rat, Mouse, Rabbit, Dog, etc.) and In Vitro Models (adipocytes, etc.). In addition, we also provide customized modeling services to ensure maximum satisfaction in preclinical studies of anti-obesity therapies.
- Pharmacodynamic Study: Relying on professional obesity models and advanced detection technologies, the mechanism of action of anti-obesity therapies is revealed through the analysis of fat distribution, biomarkers, energy expenditure, signal transduction pathways, etc.
- PK Study: We adopt reliable obesity models to analyze the PK of anti-obesity drugs, including absorption, bioavailability, distribution, metabolism, and excretion. Based on our comprehensive drug analysis platform, we provide a one-stop PK study service to accelerate anti-obesity therapeutic research.
- Bioanalysis: We use highly sensitive methods to analyze anti-obesity small and large molecule drugs and their related metabolites. The results are comprehensive and provide data to support the evaluation of drug therapeutic effects.
- Safety Assessment: We assess the safety of anti-obesity drugs by studying their effects on the central nervous system, immune system, etc., and provide reliable support for pre-clinical studies of anti-obesity drugs.
Workflow
Our team brings together researchers from diverse backgrounds, pooling their knowledge, skills, and expertise to develop new and innovative anti-obesity therapeutic solutions.
Applications
- Combination therapies: The study of anti-obesity therapies targeting exendin supports the development of combination therapy strategies using multiple drugs.
- Diabetes research: The study of anti-obesity therapies targeting exendin supports the development of promising anti-diabetic therapies.
- Metabolic diseases: The development of anti-obesity therapies targeting exendin may also be a reliable approach for the treatment of obesity-related metabolic diseases.
Advantages
- We are committed to providing unparalleled research services to assist you from project initiation to detailed analysis of the final anti-obesity therapy.
- We utilize proprietary methodologies and advanced technologies to complete experiments, accelerating the research process and ensuring an in-depth understanding of the efficacy of the anti-obesity therapies developed.
- We offer strong after-sales support and are ready to answer and resolve any questions you may have about your obesity research.
What Other Services Do We Offer?
As a leader in the field of anti-obesity research, we are committed to translating scientific analysis into the cornerstone of anti-obesity research. To this end, we also offer a comprehensive range of services including obesity analysis, diagnostic testing, risk assessment, microbiology studies, and more. By analyzing the pathogenesis of obesity, the profile of gut bacteria, and more, we provide support for obesity intervention, treatment, monitoring, and management.
Publication
Technology: Gene editing, Enzyme-linked immunosorbent assay
Journal: Iranian Journal of Pharmaceutical Research
IF: 1.8
Published: 2023
Results: In this study, a novel long-acting dual agonist, exendin-4/ FGF21 (Ex-DARP-FGF21), was designed by targeting GLP-1 and FGF21 receptors. The fusion protein was successfully expressed and purified in an Escherichia coli system and was tested to have a high binding affinity for human serum albumin in vitro. Injections into mice subcutaneously for PK and bioactivity studies showed that the protein had an extended half-life of 27.6 hours in vivo and significantly reduced blood glucose levels. This dual agonist showed enhanced hypoglycaemic bioactivity and superior weight management compared to Ex-DARP alone and had great potential for the treatment of obesity and type 2 diabetes.
Fig.1 Schematic diagram of
Ex-DARP-FGF21. (Zhang, et al., 2023)
Frequently Asked Questions
What is the mechanism of action of exendin-4?
Exendin-4 is a GLP-1 receptor agonist with a mechanism of action similar to GLP-1. It exerts anti-obesity effects by suppressing appetite, delaying gastric emptying, and promoting insulin secretion to improve blood glucose levels.
What is the current progress in the development of anti-obesity therapeutics targeting exendin?
Currently, significant progress has been made in the development of anti-obesity therapeutics targeting exendin. Some exendin analogs have been developed and shown to have favorable weight loss and anti-obesity effects in detailed preclinical studies.
Protheragen offers a flexible exendin-targeted anti-obesity therapeutic development solution and supports our clients in their studies. As the best partner for anti-obesity research, we provide ongoing support for your experiments. Welcome to contact us to discuss more details about anti-obesity therapy research.
Reference
- Zhang, C.; et al. Design of a dual agonist of exendin-4 and FGF21 as a potential treatment for type 2 diabetes mellitus and obesity. Iranian Journal of Pharmaceutical Research: IJPR. 2023, 22(1).
All of our services and products are intended for preclinical research use only and cannot be used to diagnose, treat or manage patients.