Receptors are one of the important targets for antidiabetic drug development. Ace Therapeutics is a preclinical contract research organization specializing in diabetes. Our core competency lies in the provision of drug discovery and development services targeting diabetes receptor targets. By leveraging our expertise in diabetes modeling and advanced drug development, we can assist our clients in the development of innovative drugs targeting specific diabetes receptor pathways. Our diabetes experts and drug development team are dedicated to helping you develop innovative antidiabetic drugs that effectively control blood glucose levels while maintaining pancreatic β-cell function and survival.

Receptor Targets in Antidiabetic Drug Development

The successful development of numerous drugs targeting membrane or intracellular receptors has revealed the important role of these receptors and their downstream signaling networks in the disease process. A number of different structures and classes of diabetes-related receptors have been identified, which are associated with highly diverse, complex and interconnected signaling pathways that control β-cell function and/or survival. Currently, the glucagon-like peptide-1 receptor (GLP-1R) and gastric inhibitory peptide receptor (GIPR) are popular targets for the treatment of type 2 diabetes. A GLP-1R/GIPR dual agonist, tirzepatide, has been successfully developed for this purpose.

Fig. 1 Tirzepatide action in islet endocrine cells. (Dalle, S. et al., 2024)

Below is a list of different receptors that are currently known to play a role in regulating β-cell function/dysfunction and/or survival/death. These receptors reveal important new therapeutic targets for antidiabetic drug development.

How Can We Support Your Receptor-Targeted Antidiabetic Drug Development Plan?

Ace Therapeutics offers drug discovery services focused on key diabetes-related receptor targets. Our comprehensive solution encompasses a range of aspects related to antidiabetic drug discovery, including pharmacodynamic studies, pharmacokinetic analyses, and safety assessments.

Screening and optimization of receptor-targeted antidiabetic drug

We specialize in the construction of high-throughput screening systems based on the receptor target of interest, with the objective of assisting our clients in the rapid identification of potential antidiabetic drug candidates. Furthermore, we can optimize the structure of the drug in question, based on the screening results, with a view to improving its specificity and efficacy.

In vivo and in vitro pharmacodynamic assessment services

Ace Therapeutics has a robust in vivo and in vitro diabetes model portfolio that enables comprehensive evaluation of anti-diabetic drug efficacy and activity. We select the most appropriate species, modelling methodology and customized efficacy assessment strategy for our clients' drug development needs. Our efficacy assessment tests include, but are not limited to, the following:

Pharmacokinetic profiling services

Our comprehensive pharmacokinetic profiling services provide in vivo absorption, distribution, metabolism, and excretion characteristics (ADME) of antidiabetic drugs, as well as half-life parameters associated with drug elimination. These quantitative analysis results and key pharmacokinetic parameters provide reliable insights for the subsequent development of antidiabetic drugs.

Preclinical safety assessment services

We evaluate the potential toxicity and safety of antidiabetic drug candidates to help clients identify potential drug safety risks and side effects. This may include acute, sub-chronic and chronic toxicity studies, genotoxicity testing, carcinogenicity assessments, etc.

Features of Our Receptor-Targeted Antidiabetic Drug Discovery Services

• Multiple receptors and signaling pathways controlling β-cell function and survival as targets for antidiabetic drug development.
• We offer one-stop services from early drug screening and structure optimization to preclinical efficacy and safety assessment.
• Our experienced R&D team provides ongoing support in the development of anti-diabetic drugs. They utilize rigorous experimental design, cutting-edge R&D technology, standardized project management and efficient communication to drive the process forward.

Ace Therapeutics is committed to providing professional services and customized solutions to help address your unmet needs in antidiabetic drug development. Contact us for more details about our receptor-targeted antidiabetic drug development services. Our experts will collaborate with you in your development to advance your innovations in the field of diabetes.

References

1. Dalle, S.; et al. Receptors and Signaling Pathways Controlling Beta-Cell Function and Survival as Targets for Anti-Diabetic Therapeutic Strategies. Cells. 2024, 13(15): 1244.
2. Campbell, J. E.; et al. GIPR/GLP-1R dual agonist therapies for diabetes and weight loss-chemistry, physiology, and clinical applications. Cell Metabolism. 2023.
3. Dahlén, A. D.; et al. Trends in antidiabetic drug discovery: FDA approved drugs, new drugs in clinical trials and global sales. Frontiers in Pharmacology. 2022, 12: 807548.

• Enzyme-Targeted Antidiabetic Drug Development
• Transporter-Targeted Antidiabetic Drug Development
• GPCR119-Targeted Drug Development for Diabetes
• GIP-Targeted Drug Development for Diabetes
• THR-Targeted Drug Development for Diabetes
• GR-Targeted Drug Development for Diabetes
• PPARγ-Targeted Drug Development for Diabetes
• FFAR1-Targeted Drug Development for Diabetes
• GLP-1-Targeted Drug Development for Diabetes

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