The glucagon-like peptide-1 (GLP-1) receptor is currently one of the most prominent drug targets for treating Type 2 diabetes and obesity. Ace Therapeutics focuses on key incretin targets in diabetes drug research and development, empowering the entire preclinical development process for innovative drugs. We are committed to providing comprehensive services for global clients during the early stages of GLP-1 receptor-agonist（GLP-1 RA drug development. Our extensive expertise in preclinical research, validated diabetic models, and customized bioanalytical testing ensure efficient solutions to support breakthroughs in our clients' GLP-1 RA drug development efforts.

Why Focus on GLP-1R Agonists?

The GLP-1 receptor, known as GLP-1R, is a vital component of the G protein-coupled receptor (GPCR) family and is found primarily on the surfaces of various cell types within the human body. This receptor specifically interacts with GLP-1, a key hormone that plays an integral role in regulating blood glucose levels, lipid metabolism, and several other crucial biological functions.

In recent years, GLP-1-based therapies have emerged as a central focus in diabetes drug development due to their innovative treatment mechanisms, significant therapeutic efficacy, and broad development prospects. Globally marketed GLP-1 receptor agonists (e.g., semaglutide, liraglutide) demonstrate multifaceted benefits, including glycemic regulation, weight management, and cardiovascular protection. However, current therapies still face challenges such as short half-lives, gastrointestinal side effects, and inter-individual variability in treatment responses, necessitating innovative molecular design and precision-driven preclinical evaluation to overcome these limitations.

Fig. 1 Optical appearance and properties of pen injection devices for approved GLP-1 receptor agonists.(Nauck, M. A., et al., 2021)

Ace Therapeutics' GLP-1R-Targeted Antidiabetic Drug Development Services

Ace Therapeutics accelerates the development of innovative therapies for its clients' GLP-1 receptor agonists by developing preclinical models of diabetes, establishing quantitative analysis systems and customizing preclinical research protocols.

Multi-target co-development services

We offer comprehensive development services for GLP-1R single target, GLP-1R/GIPR, GLP-1R/GCGR dual targets, and GLP-1R/GIPR/GCGR triple targets, covering mechanism exploration, drug design optimization, and preclinical efficacy and safety evaluation.

High-throughput in vitro analysis services

Our high-throughput in vitro evaluation system supports the following services:

• Target-specific binding analysis: our platform employs fluorescence resonance energy transfer (FRET) technology to assess GLP-1R conformational activation states and screen for high-affinity ligands.
• Multidimensional functional activity validation: we comprehensively assessed GLP-1R-related functional metrics, including cAMP signaling pathway activation analysis, β-arrestin recruitment activity assays, and receptor internalization kinetic studies.
• Multi-target cross-interaction studies: we optimize the binding kinetic properties of drugs by monitoring the synergistic activation effects of dual/triple-target drugs in real time via surface plasmon resonance (SPR).

Lead compound optimization services

We offer clients the following professional services leveraging GLP-1R high-resolution crystal structures and AI-aided drug design:

• Long-acting modification: we employ fatty acid chain conjugation and antibody fusion technologies to prolong drug half-life.
• Targeted delivery optimization: we design molecular structures with low renal clearance to improve bioavailability.
• Safety assessment: we evaluate potential cardiovascular and immunotoxicity risks through in vitro hERG channel inhibition assays and cytokine release syndrome (CRS) risk profiling.

Preclinical efficacy and safety assessment services

Ace Therapeutics offers established GLP-1 in vivo efficacy models, enabling comprehensive pharmacological, pharmacodynamic, pharmacokinetic and safety evaluations.

• We employ humanized GLP-1R transgenic mice, ZDF rats, and other validated models to assess multi-dimensional metabolic regulation, including glycemic control, glucagon suppression, and gastric emptying modulation.
• We provide comprehensive preclinical safety assessments:
• Repeat dosing toxicity tests (4-week rodent studies and 13-week non-rodent studies）.
• Immunogenicity testing (anti-drug antibody ADA analysis).

Advantages of GLP-1R Agonists Development Services

• One-stop solution from target validation to preclinical testing.
• AI-driven molecular design, virtual screening, organoid modeling and other pre-research technologies.
• Strict experimental design and quality control to ensure reliable data for our clients.

Ace Therapeutics is committed to delivering end-to-end solutions for GLP-1 receptor-targeted drug development, from molecular design to preclinical studies. Leveraging validated disease models, advanced screening platforms, and deep mechanistic insights, we have successfully accelerated multiple antidiabetic programs toward clinical translation. Contact our scientific team today to explore how we can empower your research.

References

1. Nauck, M. A., et al. GLP-1 receptor agonists in the treatment of type 2 diabetes-state-of-the-art. Molecular metabolism. 46 (2021): 101102.
2. Zheng, Z.; et al. Glucagon-like peptide-1 receptor: mechanisms and advances in therapy. Signal Transduction and Targeted Therapy. 9.1 (2024): 234.

• GPCR119-Targeted Drug Development for Diabetes
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• THR-Targeted Drug Development for Diabetes
• GR-Targeted Drug Development for Diabetes
• PPARγ-Targeted Drug Development for Diabetes
• FFAR1-Targeted Drug Development for Diabetes

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