MetAP2 Role in Obesity

MetAP2 is an enzyme that regulates cell growth and differentiation and plays a key role in insulin signaling and lipid metabolism in adipocytes, and its inhibitors reduce adipocyte accumulation by blocking adipogenesis. Obesity-related studies have shown that MetAP2 inhibitors significantly reduce body weight and adipose tissue weight, and improve obesity-related metabolic disorders, such as insulin resistance and lipid abnormalities. Therefore, MetAP2 is a promising drug target and provides an important direction for the development of new anti-obesity treatments. Protheragen has set up a team dedicated to obesity-related research. We comprehensively analyze obesity from several aspects such as Targets, Therapy Development, and Preclinical Research.

Targeting MetAP2 for Sustainable Anti-Obesity Therapy Development

Research has identified the importance of MetAP2 in lipid metabolism and it is one of the promising targets for combating obesity. By focusing on MetAP2, we provide development services such as small molecule inhibitors for a range of potential interventions that could revolutionize the treatment of obesity.

Anti-Obesity Therapy Development

Small Molecule Inhibitor: Small molecule MetAP2 inhibitors specifically bind to and inhibit the function of MetAP2, thereby regulating obesity-related metabolism such as reducing food intake, enhancing lipid catabolism, and promoting energy expenditure. For example, the MetAP2 inhibitor Beloranib has shown good results in clinical trials. Patients treated with Beloranib experienced significant weight loss and improved metabolic markers. However, due to safety issues, the development of Beloranib has stopped, indicating that further research is needed to find more effective and safer MetAP2 inhibitors. Protheragen helps clients develop small molecule inhibitors against the MetAP2 target, and we use high-throughput screening (HTS) to identify potential candidate molecules that exhibit inhibitory activity against MetAP2. Once promising candidate molecules are identified, our experts will optimize from candidate molecules to lead compounds, improving their chemical structures to improve potency, selectivity, and pharmacokinetic properties.

Gene Therapy: After identifying and characterizing the MetAP2 gene and its role in obesity, gene editing technologies are used to edit specific genes associated with MetAP2 to regulate its expression and function. By directly changing the genetic factors that lead to excessive fat accumulation, it brings sustained therapeutic effects and long-term management of obesity to obese people.

Combination Therapy: Combination therapy is a multifaceted approach, such as exploring the effects of combining small molecule MetAP2 inhibitors with other treatment modalities such as dietary intervention, exercise, or other agents. This multi-pronged strategy addresses obesity through various biological pathways and mechanisms, potentially improving the overall treatment effect and providing a holistic treatment plan for obese patients.

Preclinical Research of Anti-Obesity Therapies

We provide comprehensive preclinical research services for anti-obesity therapies with our advanced platforms and rich practical experience. The developed therapies are tested in vitro and in vivo in Obesity Models to evaluate their efficacy in reducing obesity parameters such as body weight and fat accumulation. In addition, we also conduct Pharmacodynamic and Toxicology Studies to ensure the safety and effectiveness of the therapy.

Workflow

Applications

• Drug development: MetAP2 inhibitors reduce fat accumulation and enhance fat metabolism. We help clients develop effective drugs for treating obesity by targeting MetAP2.
• Metabolic research: Studying MetAP2 targets provides insights into nutritional and lifestyle interventions that regulate MetAP2 enzyme activity and how to manipulate MetAP2 to combat obesity.
• Biomarker discovery: MetAP2 levels and activity are used as biomarkers to assess obesity susceptibility and monitor treatment effects.
• Diagnostic tool development: Understanding the MetAP2 pathway helps develop diagnostic tools for the early detection of obesity-related diseases and the development of personalized treatment plans.

Advantages

• Protheragen develops breakthrough anti-obesity therapies based on specific target information and uses technical advantages in proteomics, enzyme activity assays, etc., to identify and validate effective MetAP2 inhibitors.
• Protheragen uses a high-throughput screening platform to rapidly screen large compound libraries and quickly identify potential molecules with high specificity and potency against MetAP2.
• Our services also include comprehensive MetAP2 bioassays. These assays are critical for the preclinical evaluation of drug candidates and ensure accurate measurement of efficacy and safety under various experimental conditions.
• Our flexibility in experimental design and drug development strategy ensures that we meet the unique requirements of each project and provide personalized and optimized treatment development solutions.

Our Services

Publication

Frequently Asked Questions

What is the role of MetAP2 in fat metabolism?

MetAP2 is an enzyme that catalyzes the removal of methionine residues from nascent proteins and plays a key role in fat metabolism by affecting pathways essential for lipogenesis and lipid storage. In the context of obesity, MetAP2 helps control the balance between lipid accumulation and breakdown by regulating the activity of key enzymes involved in lipid metabolism. Inhibition of MetAP2 disrupts this balance, leading to reduced lipid storage and decreased adipose tissue mass. This makes MetAP2 a promising therapeutic target for the development of treatments aimed at reducing excessive fat accumulation and combating obesity.

How do you validate the efficacy of MetAP2 inhibitors in preclinical trials?

Protheragen uses the following steps to validate the effectiveness of MetAP2 inhibitors in preclinical trials: 1) In vitro enzyme activity tests evaluate the binding affinity and inhibitory potency of the inhibitors to MetAP2; 2) Cell tests evaluate how the inhibitors affect adipogenesis and lipid accumulation in adipocyte culture; 3) Determine parameters such as body weight, fat weight, glucose tolerance, and insulin sensitivity of rodents during treatment to evaluate the efficacy and safety of the inhibitors. Meanwhile, histological analysis of the adipose tissue and liver of the treated animals is performed to observe any cellular changes caused by treatment.

Protheragen targets MetAP2 to develop effective and targeted innovative treatments to reduce the burden of obesity-related health problems. Please feel free to contact us to learn about the progress and application development of MetAP2 in obesity research and work with you to advance your important research.

All of our services and products are intended for preclinical research use only and cannot be used to diagnose, treat or manage patients.

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