Lead Optimization Service

Lead optimization or drug optimization aims at enhancing the chemical compounds from drug screening to improve potency, and reduce toxicity in humans. As an experienced drug discovery company, Ace Therapeutics can provide the lead optimization services related to for diabetes.

Overview of Lead Optimization

In drug discovery and development, once a chemical compound is identified, the following step is to evaluate its. And then, it comes to lead optimization to maintain favorable properties of lead compounds and improve other parameters.

Optimization Strategies

Optimization of Small Molecule Drug
Drug optimization aims to improve the properties of lead compounds including stability, potency, efficacy, exposure, safety, etc. Potential safety concerns about some lead compounds can be addressed at this stage by modifying or reducing deficiencies in its structure.
Optimization of Antibody Therapies
Reduction of a nonhuman antibody's immunogenicity in humans is a critical step of antibody optimization; otherwise, the therapeutic antibody candidate would induce anti-drug antibodies in humans. Antibody humanization and deimmunization strategies need to be performed.

Fig 3. The General Structure of a Human IgG Antibody The General Structure of a Human IgG Antibody (Wang, B.; et. al. Antibody Therapeutics, 2021)

Our Services

The compound which has the desired activity in a compound screen and whose activity is confirmed upon retesting. With the combination of computational and medicinal chemists as well as advanced technologies, Ace Therapeutics is capable of design customized lead optimization panels to meet your specific needs in lead optimization. Our services include but not limited to the followings.

Fig 4. Cell Optimization

Cell Optimization

Cell modification (enhancing the expression of specific trophic factors, etc.)
Cell pretreatment (hypoxic preconditioning, chemical treatment, etc.)
Using chemical or biomaterial to help improve cell survival

Fig 5. Gene Target Optimization

Gene Target Optimization

Viral vector optimization (providing advanced transcriptional and transductional targeting strategies)
Non-viral vector optimization (optimizing vector surface, optimizing transfection reagents, etc.)

Fig 6. Small Molecule Drug Optimization

Small Molecule Drug Optimization

Computer-aided drug lead optimization
Medicinal chemistry SAR, design, synthesis and optimization
Improving of ADMET-properties

Fig 7. Antibody Optimization

Antibody Therapy Optimization

Antibody humanization (structure modeling)
Antibody affinity maturation (random mutagenesis, targeted mutagenesis, chain shuffling and in silico approaches)
Fc effector function improvement (amino acid mutations, modification of the glycosylation, etc.)
Antibody pharmacokinetic improvement

Features of Our Services

Highly Customizable

One-stop Services

High Qualitys High Quality

Professional Team

Ace Therapeutics can accelerate the therapeutic development and drug discovery process about diabetes for our clients worldwide. Our assays are developed and processed with the highest standard and the results are delivered on time without compromising quality. Most of those assays are suitable for drug discovery. Please feel free to contact us.

References

Wang, Z. Z.; et al. Fragment-based drug design facilitates selective kinase inhibitor discovery. Trends in Pharmacological Sciences, 2021, 42(7), 551-565.
Wang, D.; et al. Adeno-associated virus vector as a platform for gene therapy delivery. Nature reviews Drug discovery. 2019, 18(5), 358-378.

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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