Overview

GIP is an enteric insulinotropic hormone composed of several amino acids. As an important metabolic hormone, it is secreted by K-cells following nutrient intake and stimulates insulin secretion through activation of the GIP receptor (GIPR), which affects food intake, nutrient absorption, blood flow, etc. GIP is found to have important effects on adipocytes and the promotion of tissue fat deposition, etc. GIPR is expressed in specific cell types, many of which play a direct or indirect role in the control of body weight. It is a potential target for anti-obesity drugs. Anti-obesity therapies targeting GIPR have been developed to investigate their effects on obesity. With profound research on the physiology and anti-obesity of GIP, Protheragen offers a high-quality development service for GIPR-targeting anti-obesity therapies. We aim to provide professional and reliable support to our clients through reliable laboratory solutions.

Unlocking Innovative Therapies Research: Experience GIPR-Targeting Anti-Obesity Therapy Development Service

We are committed to working closely with our clients to leverage our expertise in GIPR, obesity physiology, etc., to facilitate effective, innovative anti-obesity therapy research. Specific services include the following:

Anti-Obesity Therapy Development

• Anti-obesity drug development
  Computer-aided Drug Design: Our molecular simulation team has many years of experience in anti-obesity drug design. We apply various computational tools to screen compounds that interact with GIPR. Their activity, potency, selective metabolic stability, safety, etc., are also computationally evaluated to provide valuable information for the design and optimization of anti-obesity drugs.
  GIPR-modulating compounds: With pharmacological optimization, the role of GIPR-modulating compounds in anti-obesity and diabetes is gradually being revealed. In preclinical models, both GIPR agonists and antagonists have been found to have metabolic benefits and exert some anti-obesity effects by reducing body weight due to overnutrition. Based on our deep understanding of the mechanism of action of GIPR-regulated compounds, we develop anti-obesity therapies centered on GIPR agonism and antagonism.
  
  • GIPR agonism: Combination therapies based on GIP and Glucagon-Like Peptide 1 (GLP-1) have been developed and shown to have significant weight loss benefits in animal models. We develop dual agonists or triple agonists targeting GIPR, GLP-1 receptor (GLP-1R), etc., and evaluate their anti-obesity effects.
  • GIPR antagonism: Reducing or blocking GIPR signaling is a novel strategy for the treatment of insulin resistance, obesity, and diabetes. Various studies have been conducted to evaluate the beneficial effects of GIPR antagonists in the fight against obesity and diabetes. We develop various compounds that block GIPR signaling, including the following:
    • Peptide GIPR antagonists: Two GIPs are found to exhibit GIPR antagonism when used at supraphysiological concentrations. We modify the GIPs and evaluate their potential in the treatment of obesity.
    • GIPR antagonists with low molecular weight: A disadvantage of peptide-based therapies is the need for parenteral administration. This difficulty is avoided by using low molecular weight GIPR-inhibiting compounds. We develop low molecular weight GIPR antagonists and analyze changes in metabolism, lipid accumulation, insulin sensitivity, body weight, etc., in animal models after administration.
• Anti-Obesity Gene Therapy development
  Gipr knockout mouse is found to reduce weight gain after being fed a high-fat diet. We use various gene editing strategies to knockout Gipr in pancreatic islets, adipocytes, etc., and evaluate the anti-obesity effects of such strategies.
• Anti-Obesity Antibody Therapy Development
  Several studies have shown that active immunization against GIP improves metabolic status and glycaemic control in obese diabetic animals. Passive immunization by administering antibodies specific to the GIP molecule or GIPR may also be a strategy to eliminate GIPR signaling. We also develop anti-GIPR antibodies and evaluate their effects on body weight, food intake, and metabolic improvement in obese models.

Preclinical Studies of Anti-Obesity Therapies

GIP receptor regulatory compounds have effects on different tissues, weight loss, and other metabolic diseases. Further studies are needed to understand the mechanism of action of these regulatory compounds in anti-obesity.

• Obesity Models: We have many types of In Vivo and In Vitro Obesity Models, including diet-induced obesity models, Gene Editing Models, and others. We select appropriate models for anti-obesity studies based on specific experimental objectives to accelerate the exploration of anti-obesity therapies targeting GIPRs.
• Evaluation of anti-obesity therapies: We develop comprehensive preclinical study protocols to analyze the molecular mechanisms of GIPR-regulated compounds or gene editing strategies in the treatment of obesity. Based on our extensive preclinical research experience, we evaluate the efficacy of various anti-obesity therapies through detailed in vitro and in vivo safety, pharmacokinetic, pharmacodynamic, and other biological analyses.

  Pharmacodynamics Study	Food/Water Intake Assessment Quantitative Analysis of Body Fat Distribution Energy Expenditure Monitoring Measurement of Ectopic Fat Accumulation Molecular Biomarker Analysis
  Pharmacokinetics Study	DMPK Study of Anti-Obesity Drugs ADME Study of Anti-Obesity Drugs
  Bioanalysis	Biological Analysis of Macromolecular Drugs Bioanalysis of Small Molecule Drugs
  Safety Assessment	Safety Pharmacology Studies Toxicology Studies

Workflow

Applications

• The development of innovative anti-obesity therapies targeting GIPRs provides new ideas for obesity intervention strategy research.
• The development of innovative anti-obesity therapies targeting GIPR provides valuable information for diabetes treatment research.
• The development of innovative anti-obesity therapies targeting GIPR provides new ideas for research on obesity-related cardiovascular disease treatment strategies.

Advantages

• We provide full-service and reliable support at all stages of anti-obesity drug development (design, synthesis, and preclinical analyses) targeting the GIPR.
• We have extensive experience in medicinal chemistry, and custom synthesis to support the development of various GIPR modulators.
• As a high-tech industry, we have a comprehensive portfolio of in vivo and in vitro obesity models to facilitate preclinical studies of anti-obesity therapies targeting GIPR.

Innovative and Distinctive Services

Our team is at the forefront of exploring the mysteries of obesity and seeking new paths to anti-obesity treatments, providing innovative solutions and comprehensive support to researchers. We analyze the influence of genetic code and environmental factors on obesity and provide diagnostic tests and obesity prediction services with the help of diversified technologies and models. We also specialize in extracting reliable clues to obesity mechanisms through biomarker, microbiome, and pathology analyses, deepening the understanding of obesity and laying a solid foundation for the development of therapeutic strategies. Our gene editing technology also provides reliable support for obesity research. Our weight loss and weight management technologies are also unique, enabling effective management through scientifically guided weight control.

Publication

Frequently Asked Questions

In which tissues and cells is GIPR expressed?

GIPR is expressed in specific cell types throughout the body, including in pancreatic cells, stomach, small intestine, adipose tissue, heart, pituitary gland, heart, lungs, and spleen. In pancreatic islets, only α and β cells express GIPR. GIPR regulates the expression of downstream protein genes through multiple signals by activating G proteins to increase intracellular cyclic adenosine monophosphate (cAMP) levels and Ca²⁺ levels.

How to achieve Gipr knockdown?

We have a variety of gene editing techniques with high accuracy and specificity, and have been widely used for gene function studies, modeling, and so on. Common knockdown strategies include single sgRNA-mediated knockdown and double sgRNA-mediated knockdown. Combined with our rich experience in gene editing, we realize the knockdown of Gipr gene and verify the anti-obesity effect of this strategy.

Protheragen leverages its deep knowledge of GIPR and obesity to provide innovative anti-obesity therapeutic development services targeting GIPR. We are the best partner for anti-obesity studies based on strict quality norms and transparency at all study stages. Welcome to contact us to tell us about your specific research needs, if you are interested or in need in this area.

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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