Diabetes Drug R&D Services ace

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

Fructose-1,6-bisphosphatase (FBPase) provides an effective therapeutic target for the development of novel antidiabetic drugs. Ace Therapeutics specializes in providing one-stop service from target validation to preclinical candidate development. With our extensive diabetes modeling and pharmacology platform, we help our clients accelerate the development of antidiabetic drugs against the key diabetes target of fructose-1,6-bisphosphatase (FBPase).

FBPase as an Antidiabetic Drug Target

Fructose 1,6-bisphosphatase (FBPase) is a key enzyme in gluconeogenesis. Inhibition of fructose 1,6-bisphosphatase (FBPase) has drawn extensive global interest because of its ability to inhibit endogenous glucose produced by hepatic gluconeogenesis, which is considered a novel pharmacological approach to managing high blood glucose levels. The attractiveness of FBPase as a drug target is mainly based on its position in the gluconeogenesis pathway, which enables inhibition of gluconeogenesis from all gluconeogenesis substrates while avoiding direct effects on glycogenolysis, glycolysis, and the tricarboxylic acid cycle.

This target is particularly applicable to type 2 diabetes mellitus (T2DM), especially in groups with insulin resistance or fasting hyperglycemia. Currently, breakthroughs have been made in the development of FBPase inhibitors:

The first-generation inhibitors (e.g., CS-917) were eliminated due to insufficient bioavailability, but its subsequent optimized product, VK0612 (MB07803), has significantly improved its stability and half-life through structural modification, and has completed six Phase I and one Phase II clinical trials, demonstrating excellent glucose-lowering potential.
Mutagenic inhibitors (e.g., MB05032) provide a promising new direction for the development of oral antidiabetic drugs by targeting the AMP-binding site of FBPase (IC50 of 16 nM) to achieve efficient and selective inhibition.

Fig. 1 Fructose-1,6-bisphosphatase inhibitors as an effective therapeutic strategy for type 2 diabetes. (Kaur, Ramandeep.; et al., 2017)

FBPase-Targeted Antidiabetic Drug Development Services

Construction and validation of diabetic animal models

Genetically engineered models: including FBPase function-deficient models for evaluating target specificity and long-term safety.

Metabolic phenotyping: simulating human T2DM pathology through spontaneous diabetes models such as ZDF rats, for precise detection of blood glucose, glycosylated hemoglobin (HbA1c) and hepatic gluconeogenic markers.

Screening and optimization of fructose-1,6-bisphosphatase (FBPase) inhibitors

High-throughput screening platform: rapid screening of small molecule libraries, natural products and antibody candidates based on enzyme activity assays and cell modeling.

Structure-activity relationship (SAR) studies: optimize potency, selectivity and pharmacokinetic properties of inhibitors through molecular docking, conformational analysis and chemical modification.

Preclinical pharmacodynamics and safety evaluation

Efficacy verification: We evaluate improvements in fasting glucose, postprandial glucose and glucose tolerance by the inhibitor in rodent models.

Pharmacokinetic profiling: We provide comprehensive pharmacokinetic analysis services to support drug development, including absorption, distribution, metabolism, and excretion (ADME) profiling, bioavailability/bioequivalence studies, and PK/PD modeling.

Advantages of Our Technology

Interdisciplinary integration: Combine enzyme kinetics, metabolomics, and computational biology to precisely analyze the regulatory network of FBPase.
Full process compliance: Compliance with regulatory standards ensures data traceability and international registration filing requirements.

Ace Therapeutics is committed to leveraging its expertise and platform technologies to develop innovative antidiabetic drugs targeting fructose-1,6-bisphosphatase (FBPase). Please contact us for more details.

Reference

Kaur, Ramandeep.; et al. Fructose-1, 6-bisphosphatase inhibitors: a new valid approach for management of type 2 diabetes mellitus. European journal of medicinal chemistry. 141 (2017): 473-505.

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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