MetAP2-Targeted Drug Development for Diabetes

MetAP2-Targeted Drug Development for Diabetes

MetAP2 is a promising therapeutic target for type 2 diabetes. Ace Therapeutics provides one-stop drug development services from target validation to preclinical efficacy testing. Leveraging our expertise in both in vivo and in vitro diabetic models and proven experience in preclinical drug development, we empower clients to rigorously evaluate MetAP2-targeted antidiabetic therapeutics. Our platform technology and translational research services will help clients optimize and accelerate their antidiabetic drug development programs.

Potential of MetAP2 as an Antidiabetic Drug Target

Methionine aminopeptidase 2 (MetAP2), an intracellular metalloprotease, has emerged as a promising therapeutic target due to its critical role in regulating lipid metabolism, energy balance, and protein synthesis. Inhibitors targeting MetAP2 are used in the treatment of type 2 diabetes. ZGN-1061 is a novel MetAP2 inhibitor under investigation for the treatment of both diabetes and obesity. In vivo experiments demonstrated that subcutaneous injection of ZGN-1061 reduced body weight and improved metabolic parameters such as blood glucose and insulin in diet-induced obese (DIO) insulin-resistant mice. Thus, MetAP2 inhibitors bring new therapeutic options for type 2 diabetes.

A model of N - myristoylation which is MetAP2 - dependent and its function in T2DM.Fig. 1 A model of MetAP2-dependent N-myristoylation and its role in T2DM. (Moon, D. O., 2024)

MetAP2-Targeted Antidiabetic Drug Development Services

Ace Therapeutics provides comprehensive support for the development of diabetes drugs targeting MetAP2, covering target biology studies, inhibitor design optimization, and preclinical efficacy/safety evaluations.

Mechanistic studies of MetAP2

  • We elucidate the regulatory network of MetAP2 in lipid metabolism, insulin sensitivity and energy homeostasis through gene editing, protein interaction analyses and metabolic pathway studies.
  • We combine cellular models (e.g., adipocytes, hepatocytes) and disease-related signaling pathway analysis to reveal the targets and downstream effects of MetAP2 inhibitors.

Target validation of MetAP2

  • We used knockout/knockdown (CRISPR, RNAi) technology to validate the criticality of MetAP2 in metabolic disorders and assess its feasibility as a therapeutic target.
  • We test the inhibitory effect and specificity of the drug candidates on MetAP2 activity by in vitro enzyme activity assay, cell proliferation and metabolic phenotyping.

Preclinical efficacy evaluation

  • We assess the effect of MetAP2 inhibitors on metabolic improvement, including key parameters such as body weight regulation, blood glucose levels, and insulin resistance through a diet-induced obesity (DIO) mouse model.
  • We provide comprehensive pharmacokinetic (PK) and toxicology study services to help our clients evaluate the safety of their antidiabetic drug candidates.

Advantages of Our MetAP2-Targeted Antidiabetic Drug Development Services

  • Precision and efficiency: We integrate multi-omics technologies and disease models to provide a comprehensive analysis of target mechanism and efficacy.
  • Customized solutions: We design experiments according to clients' needs and support multiple development paths such as small molecule inhibitors and antibody drugs.
  • Professional team: Our experienced scientific team provides one-stop support from experimental design to data interpretation.

Ace Therapeutics helps clients accelerate drug development targeting MetAP2 through our integrated services. Please contact us for more details. Our experts are ready to help advance your program.

Reference

  1. Moon, D. O. MetAP2 as a Therapeutic Target for Obesity and Type 2 Diabetes: Structural Insights, Mechanistic Roles, and Inhibitor Development. Biomolecules. 2024, 14(12): 1572.
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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Ace Therapeutics has a team of experts in the field of endocrine and metabolic research, aiming to provide innovative preclinical contract research solutions to cope with diabetes and its complications. We provide customized solutions and technical support, enabling the transformation of promising concepts into innovative treatments, thus accelerating the drug development process of diabetes.

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