Natural endogenous peptides exhibit desirable medicinal properties but are often limited in applications by rapid proteolysis and insufficient membrane permeability. Editing of naturally occurring peptide sequences to develop peptidomimetic analogs thus creates a promising class of therapeutic approaches. CD BioSciences is committed to providing peptidomimetic development services to facilitate related basic research and therapeutic development.
Overview of Peptidomimetics
Over the past few decades, a large number of bioactive peptides have been discovered and characterized that influence intercellular communication and control a range of important functions due to their interaction with their membrane-bound receptors. As a result, many bioactive peptides have been prepared on a large scale and tested pharmacologically and clinically, allowing the development of new therapies for various pathologies.
The need for peptidomimetic development stems from the limitations of peptides as potential therapeutics, including:
- Limited stability towards proteolysis, resulting in a half time in the order of minutes in the gastrointestinal tract and in serum.
- Poor transport properties to the blood and across the blood-brain barrier due to high molecular weight and lack of specific transport systems.
- Rapid excretion through the liver and kidneys.
- Intrinsic flexibility enables the interaction with multiple proteins besides the target, and thus resulting in undesired side effects.
The structure and function of peptidomimetics have been significantly improved compared with the parent starting peptide, so peptidomimetics have become one of the most potential therapeutic methods.
Fig. 1 Advantages of peptidomimetics over peptides. (Lenci, E., & Trabocchi, A., 2020)
Definition and Classification of Peptidomimetics
Peptidomimetics have been defined as "compounds whose essential elements (pharmacophore) mimic a natural peptide or protein in 3D space and which retain the ability to interact with the biological target and produce the same biological effect". Its latest classification is as follows:
Fig. 2 Classification of peptidomimetics. (Pelay-Gimeno, et al., 2015)
Our Services
CD BioSciences has long been committed to providing peptidomimetic development services for global customers, using our advanced PepDomTM platform to design and synthesize peptidomimetics according to the specific requirements of customers. Our services include but are not limited to:
Selecting novel and effective targets is the primary task of drug development. Rational peptidomimetic design can be carried out based on the targets revealed in life science research, or their endogenous ligands and chemical structural characteristics of natural substrates. Discover drug lead compounds that selectively act on targets.
The development of therapeutic drugs based on the functional properties of peptides holds great promise. Rational peptidomimetic design can be rationally altered and modified based on the functional properties of the initial peptide to obtain desirable stability or other characteristics, as a lead compound for new drug development.
Principles of Design
- Replacing the peptide backbone with a non-peptide framework, which is particularly important for improved bioavailability.
- Retained side chains involved in biological activity, as they constitute structural elements of the pharmacophore.
- Maintain the flexibility of the first generation peptidomimetics.
- Appropriate targets are selected based on the pharmacophore hypothesis.
Features of Our Services
★ Comprehensive Solutions
Provide professional solutions from peptidomimetic design to validation of each link.
★ Wide Range of Application Scenarios
Provide peptidomimetic development services covering scientific research, pharmaceutical and other research fields.
★ Diverse Product Options
Provide peptidomimetic development services based on diverse functionalities or mechanisms of action.
CD BioSciences is always ready to provide the best services to each of our customers. If you are interested in our services or have any specific requirements, please feel free to contact us for more details.
References
- Lenci, E., & Trabocchi, A. (2020). Peptidomimetic toolbox for drug discovery. Chemical Society Reviews, 49(11), 3262–3277.
- Pelay-Gimeno, M., Glas, A., Koch, O., & Grossmann, T. N. (2015). Structure-Based Design of Inhibitors of Protein-Protein Interactions: Mimicking Peptide Binding Epitopes. Angewandte Chemie International Edition, 54(31), 8896–8927.
All of our services are intended for preclinical research use only and cannot be used to diagnose, treat or manage patients.
