Targeting Cannabinoid Receptors (CB1 and CB2) for Developing Anti-Obesity Therapeutics
InquiryOverview
CB is a key factor in the maintenance of energy homeostasis, regulating lipid signaling and several metabolic processes. Targeting two CB receptors (CB1 receptor and CB2 receptor) for the treatment of obesity and its complications is an attractive research direction. Many studies have focused on determining the pharmacophore requirements within the binding domains of CB1 and CB2 receptors, synthesizing novel ligands, and determining whether these ligands have beneficial pharmacotherapeutic activities. Protheragen draws on its extensive knowledge and research experience to provide a personalized anti-obesity therapeutic development service targeting CB1 and CB2 receptors in line with our client's research needs. Our comprehensive capabilities maximize specific experimental needs and help ease the critical junctions in the therapeutic development process.
Promoting the Development of CB Receptor-Targeting Anti-Obesity Therapies Through Personalised Service
We are dedicated to accelerating and innovating the development of gene therapy and anti-obesity drugs targeting CB receptors. Combining a variety of advanced technologies and techniques, our services include the following:
Anti-Obesity Therapy Development
Anti-obesity gene therapy: CB receptors play a role in lipid metabolism, diet, and more. It is found that CB1 knockout mice are less likely to gain weight, eat less, and do not develop insulin resistance, even when fed through a high-fat diet. We develop anti-obesity gene therapies targeting CB and evaluate their potential in the treatment of obesity.
Anti-obesity drug development: In order to develop more efficient and specific anti-obesity drugs without side effects, we concentrate on compounds with restricted action or activation of CB2 receptors present in the liver, skeletal muscle, adipose tissue, pancreas, and periphery. The combination of computer, in vitro, and in vivo techniques makes it possible to develop faster anti-obesity drugs that selectively and specifically target CB receptors.
- Computer-aided Drug Design: Computer simulation tools provide valuable insights into potential drug-target interactions. We use a variety of advanced computer simulation tools for molecular modeling and analyze the binding force between compounds and CB receptors through molecular docking and molecular dynamics simulations. Ultimately, through screening, design, and optimization, we obtain a variety of CB1 receptor antagonists or CB2 receptor activators.
- CB1: The CB1 receptor is widely distributed in the central and peripheral and it is present in organs such as the pancreas, adipose tissue, gastrointestinal tract, and liver. It is involved in a variety of functions such as stress, anxiety, gastrointestinal motility, etc, and regulates food intake through pro-appetite signaling. Excessive activation of CB1 increases body weight and appetite, which makes it an interesting focus for anti-obesity research. CB1 antagonists are found to promote weight loss in diet-induced obesity models compared to untreated animals. Inhibition of CB1 in the gastrointestinal tract acts to control food consumption by decreasing levels of growth hormone-releasing peptide and increasing levels of cholecystokinin. CB1 antagonists also provide therapeutic benefits in the treatment of obesity by desensitizing hypothalamic leptin signaling. We use the obesity model to explore the role of CB1 antagonists in reducing body weight and treating obesity.
- CB2: It is suggested that stimulation of CB2 may exert anti-obesity effects by reducing weight gain and food intake. We design and synthesize CB2 agonists through molecular modeling and assess their potential for treating obesity.
Preclinical Studies for Anti-Obesity Therapies
We provide a full range of preclinical testing services for anti-obesity therapies, including the construction of obesity models, safety assessment, and bioanalysis of treatment effects. Based on reliable animal model construction and analysis technology, we provide support for basic medicine, anti-obesity drugs, and other therapeutic research.
Obesity Models: Our obesity animal models include diet-induced models, Gene Editing Models, and so on. They are effective tools for obesity basic science research and preclinical evaluation of anti-obesity therapies. Based on the specialized animal experiment technical team and perfect facilities, we use Mice, Rats, Rabbits, etc., to construct obesity models and test their physiological and biochemical tests, etc.
Therapeutic efficacy evaluation: We conduct comprehensive evaluations of designed anti-obesity therapies, including pharmacodynamics, pharmacokinetics, bioanalysis, and safety assessment. Reliable technology and optimal testing processes enable us to provide reliable data in the research and critical phases of anti-obesity therapies.
- Pharmacodynamics Study: Relying on specialized obesity models and comprehensive assay technologies, we elucidate the mechanism of action of anti-obesity treatment strategies through in-depth analysis of key elements such as adipose tissue characteristics, biomarker changes, and differences in energy metabolism levels.
- Pharmacokinetics Study: We use validated obesity animal models to systematically investigate the pharmacokinetic properties of each anti-obesity drug, including absorption efficiency, bioavailability, metabolic transformation, excretion, etc. The whole process is efficient and effectively accelerates the research process of anti-obesity therapies.
- Bioanalysis: Highly sensitive assays are used to accurately quantify the levels of anti-obesity small molecules, large compounds, and their metabolites. We also offer other bioanalytical assays and provide reliable data for evaluating the efficacy of drug treatments.
- Safety Assessment: We assess the effects of anti-obesity drugs on the central nervous system, immune system, and other important physiological systems to ensure the safety of the drugs. We also evaluate their toxicity to provide a basis for therapy optimization.
Workflow
We provide a competitive anti-obesity therapeutic development service targeting CB receptors to our global clients to accelerate research on personalized obesity treatments.
Applications
- Mechanism of action studies: CB receptor modulator development helps to gain insight into the mechanism of action of CB1 and CB2 receptors and their role in obesity.
- Development of combination therapies: The development of anti-obesity drugs targeting the CB receptor is helping to drive research into combination therapies using drugs that work through different mechanisms.
- Cardiometabolic disease therapeutics: CB1 receptor antagonists are also a potential avenue for the treatment of obesity-related cardiometabolic diseases.
Advantages
- Relying on the integrated R&D service platform of innovative anti-obesity therapy, we provide a one-stop therapy development service targeting CB1 and CB2 receptors from anti-obesity therapy design, computer simulation, and obesity model development to preclinical studies.
- Our experienced research team provides rational experimental design, anti-obesity therapy development, and pre-clinical studies. We also provide extensive and professional advice on data interpretation to make your studies faster.
- We follow a rigorous quality system and scientific norms to ensure the high quality and compliance of each anti-obesity therapy development project.
Our Services Based on Cutting-edge Technology
In addition to anti-obesity therapy development, we offer a wide range of obesity analysis, prediction, and management services. We utilize a multidimensional analysis strategy to deeply explore the root causes of abnormal weight gain, including genetic characteristics, environment, and so on. We provide customized diagnostic testing services by employing comprehensive research tools to support the development of precise treatment strategies. In addition, we have always been at the forefront of obesity research, seeking to uncover the complex mechanisms of obesity from a comprehensive and in-depth perspective through the identification of biomarkers and in-depth exploration of the microbiome. At the same time, our team utilizes precision gene editing technology to provide continuous support for obesity research and therapy development. The continuous exploration of weight loss and weight management also enables us to provide scientific services.
Publication
Technology: Molecular modeling, Thin layer chromatography
Journal: Scientific Reports
IF: 4.011
Published: 2018
Results: CB1 receptor antagonists are a novel strategy for the treatment of obesity. In this study, a backbone of CB1 receptor antagonists was identified by virtual screening. This was followed by the design and optimization of a series of novel phenothiazines as CB1 receptor antagonists for the treatment of obesity. The researchers performed parallel artificial membrane permeability assays and pharmacological evaluations to assess the therapeutic potential of these compounds. The results showed that several of the synthesized compounds showed significant reduction in food intake and had great potential for application in the treatment of obesity.
Fig.1 The effect of compounds on appetite. (Sharma, et al., 2018)
Frequently Asked Questions
What are the implications of molecular modeling for CB1 receptor antagonist design?
Molecular modeling is a critical step in the design and development of anti-obesity drugs. It helps to better understand ligand-receptor interactions as well as to further develop or design selective CB receptor antagonists. Various molecular modeling studies have been carried out, including ligand- and structure-based drug design and design tools.
- Ligand-based drug design: Ligand-based drug design plays a key role in identifying lead compounds. Researchers use each pharmacophore, virtual screening, and others for design to obtain CB1 receptor antagonists.
- Structure-based design: Structure-based drug design is used to understand CB receptor-ligand interactions. Design tools include homology-type modeling and docking. Researchers have developed homology models to design CB1 receptor antagonists.
What other receptors do we offer for the development of anti-obesity therapies?
- Targeting Melanocortin 4 Receptor (MC4R) for Developing Anti-Obesity Therapeutics
- Targeting Peroxisome Proliferator-Activated Receptors (PPARs) for Developing Anti-Obesity Therapeutics
- Targeting Serotonin (5-HT) Receptors for Developing Anti-Obesity Therapeutics
- Targeting Orexin Receptors (OX-1 and OX-2) for Developing Anti-Obesity Therapeutics
- Targeting Glucagon Receptor (GCGR) for Developing Anti-Obesity Therapeutics
- Targeting Gastric Inhibitory Polypeptide (GIP) Receptors for Developing Anti-Obesity Therapeutics
- Targeting Sodium-Glucose Cotransporter for Developing Anti-Obesity Therapeutics
At Protheragen, we promote anti-obesity therapies targeting the CB receptor on all fronts, based on our philosophy of client first and innovation. We specialize in technological innovation and undertake trials for the development and preclinical validation of anti-obesity therapies. Welcome to contact us to discuss the detailed process of each trial, if you are interested in this area.
Reference
- Sharma, M.K.; et al. New role of phenothiazine derivatives as peripherally acting CB1 receptor antagonizing anti-obesity agents. Scientific reports. 2018, 8(1): 1650.
All of our services and products are intended for preclinical research use only and cannot be used to diagnose, treat or manage patients.