Diabetes Drug R&D Services ace

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* Services or Products of Interest DGAT-Targeted Drug Development for Diabetes
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* 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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DGAT-Targeted Drug Development for Diabetes

Diacylglycerol acyltransferase (DGAT) is a key regulator in diabetes and obesity, representing a potential therapeutic target for antidiabetic drug development. Ace Therapeutics delivers comprehensive antidiabetic drug development solutions-from target identification to preclinical studies-leveraging our robust diabetes models to develop potent and safe DGAT inhibitors.

DGAT as a Potential Antidiabetic Drug Target

Diacylglycerol O-acyltransferase (DGAT) is an enzyme that plays a key role in triglyceride synthesis. Several DGAT inhibitors have been developed and tested in preclinical and clinical studies, with promising results. As promising agents in antidiabetic drug development, DGAT inhibitors act through the following mechanisms:

Regulation of lipid metabolism：Reduction of lipid accumulation in liver and adipose tissues.
Improvement of insulin sensitivity：Reduction of lipid accumulation and subsequent restoration of insulin signaling pathway function.
Protection of β-cells：Prevention of lipid-induced apoptosis in pancreatic β-cells.

DGATs' functional roles and therapeutic relevance in metabolic disorders. Fig. 1 The functions of DGATs along with their importance as therapeutic targets for the treatment of metabolic disorders. (Naik, R. et al., 2014)

DGAT-Targeted Antidiabetic Drug Development Services

With a full spectrum of diabetes models (e.g., HFD/STZ rats, Db/db mice) and preclinical research platforms, Ace Therapeutics supports clients in advancing DGAT inhibitors with optimized efficacy and safety profiles from target discovery to IND-enabling studies.

DGAT target validation and functional studies

Testing Program	Testing Technology	Introduction
Gene expression analysis	RT-PCR/Western blot	Detection of DGAT expression levels in diabetic animal models and determination of their correlation with diabetes.
Knockout and overexpression assays	CRISPR/Cas9 technology	Utilization of DGAT knockout or overexpression cell lines or animal models to observe the effects on diabetes-related parameters such as blood glucose and insulin sensitivity, and to verify the effectiveness of DGAT as a target.

Screening and optimization of DGAT inhibitors

We employ structure-based drug design (SBDD) integrated with virtual screening and high-throughput screening (HTS) technologies to identify potential DGAT inhibitors from large-scale compound libraries.
Structural optimization of candidate DGAT inhibitors to improve their selectivity and affinity using quantitative structure-activity relationship (QSAR) modeling approach.
We screen natural product-derived DGAT ligands, including bioactive phytochemicals, to develop novel inhibitors with enhanced efficacy and reduced toxicity profiles.

Preclinical screening services for DGAT inhibitors

We help our clients evaluate the efficacy, potency and safety of their antidiabetic drug candidates through comprehensive in vitro and in vivo assays.

In vitro experiments: we validate the pharmacological activity of the drug candidates by cellular transactivation, competitive binding assays.
In vivo experiments: We help our clients screen potential DGAT inhibitors by evaluating their effects on glycemic control, insulin sensitivity and β-cell function.

Advantages of Our DGAT-Targeted Antidiabetic Drug Development Services

Comprehensive in vitro and in vivo diabetes models.
We employ virtual screening and high-throughput screening techniques to accelerate the identification of antidiabetic drug candidates.
We accelerate the screening of antidiabetic drugs through molecular pharmacology and computer-aided techniques.

Ace Therapeutics is committed to delivering customized solutions to accelerate drug development programs. Leveraging our specialized expertise, we provide efficient and safe DGAT-targeted antidiabetic drug development support to advance type 2 diabetes research. Please contact us for more details and we will be happy to assist you.

References

Tomimoto, D.; et al. JTT-553, a novel Acyl CoA: diacylglycerol acyltransferase (DGAT) 1 inhibitor, improves glucose metabolism in diet-induced obesity and genetic T2DM mice. Journal of pharmacological sciences. 129.1 (2015): 51-58.
Naik, R.; et al. Therapeutic strategies for metabolic diseases: small‐molecule diacylglycerol acyltransferase (DGAT) inhibitors. ChemMedChem.9.11 (2014): 2410-2424.

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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