The development of antidiabetic drugs targeting thyroid hormone receptor (THR) has become a promising direction in metabolic disease research. Ace Therapeutics provides comprehensive thyroid hormone-targeted drug development services to help clients accelerate their antidiabetic drug discovery and development process.

Thyroid Hormones Receptors as Potential Targets for Antidiabetic Drugs

Thyroid hormone receptor (THR) belongs to the nuclear receptor superfamily and is involved in the regulation of energy metabolism, glucose-lipid metabolism, and insulin sensitivity through the modulation of gene expression. There are two isoforms of THR: α and β. Notably, THR β is highly expressed in the liver, and is closely related to cholesterol metabolism and insulin resistance. Thyroid hormone (T3/T4) can ameliorate mitochondrial dysfunction and insulin resistance by binding to THR and activating downstream signaling pathways, highlighting THRs as promising therapeutic targets for type 2 diabetes and metabolic syndrome.

Ace Therapeutics' THR-Targeted Antidiabetic Drug Development Services

We provide comprehensive thyroid hormone-targeted drug development services, covering the entire process from target validation to preclinical studies. With our professional technical team, advanced experimental platforms and customized solutions, we are committed to providing our clients with efficient and reliable thyroid hormone-targeted drug development support to help them accelerate their antidiabetic drug discovery and development process.

Target validation and molecular mechanism studies

• THR ligand screening (agonist/antagonist): High-throughput screening based on radioligand binding assays and reporter gene systems.
• Molecular mechanism study: To clarify the role of THR in metabolic regulation by detecting the activation or inhibition of downstream signaling pathways (e.g. PI3K/Akt, MAPK, etc.).

Lead optimization services

• Structure optimization: computer-aided drug design (CADD) for THR ligand binding domains.

Preclinical pharmacodynamic evaluation services

We conduct comprehensive preclinical efficacy evaluations of antidiabetic drugs targeting thyroid hormone receptor using diabetic animal models such as db/db mice and ZDF rats.

Our evaluation parameters include:

• Improvement in fasting glucose and insulin resistance (HOMA-IR).
• Activity assays of key hepatic gluconeogenesis enzymes (PEPCK, G6Pase).
• Lipid metabolism markers, including FFA and LDL-C levels.

Advantages of Our Thyroid Hormone Receptor Targeted Drug Development Services

• We provide customized antidiabetic drug development solutions based on our clients' specific needs and project objectives.
• Ace Therapeutics' experts are well versed in the biology of thyroid hormone receptors and the complexities of antidiabetic drug development. We ensure scientific rigor and strategic alignment throughout the drug development process.
• Our advanced technology platform supports comprehensive target screening, bioactivity testing, and safety evaluation for THR-targeting antidiabetic therapies.

Ace Therapeutics is committed to helping our clients develop a new generation of antidiabetic drugs with metabolic modulation through precisely targeted therapeutic strategies. Please contact us for a specific service plan.

References

1. Wang, K.; et al. Drug discovery targeting thyroid hormone receptor β (THRβ) for the treatment of liver diseases and other medical indications. Acta Pharmaceutica Sinica B. 2024.
2. Raza, S.; et al. Current treatment paradigms and emerging therapies for NAFLD/NASH. Frontiers in bioscience (Landmark edition). 2021, 26: 206.

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