Deuteration of Peptides Based on DCL™
Background & Overview
In recent years, in both academic and industrial settings, hydrogen isotope labeling techniques have become important tools for hit identification and lead optimization strategies in many drug discovery projects, as they provide important information about the biological metabolism of drug candidates and their metabolites. Deuterated substances are key compounds in drug discovery and development and are part of our ongoing work.
Deuterium-labeled peptides are critical for applications in biological experiments, such as ligand binding assays or absorption, distribution, metabolism, and excretion studies. While many homogeneous and heterogeneous catalysis methods for H/D exchange have been described, all of them require high temperatures (>50°C), which are generally not tolerant of unprotected peptides. Therefore, we have developed the innovative DCL™ technology platform to enable new deuterium labeling methods compatible with high sensitivity modalities such as large peptides.
Application of Deuterated Peptides
Stable isotope-labeled peptides and proteins, as "chemical labels" in quantitative proteomics, are widely used in the detection and tracing of biological samples.
Quantitative Proteomics
Stable isotope-labeled peptides are commonly used internal standard reagents for isotope dilution mass spectrometry, and can be used in dairy product quality control, absolute protein quantification, protein sequencing, and drug metabolism studies. For example, using enzyme-digested stable isotope-labeled peptides as internal standards, adding labeled peptides with enzyme-cleaving sites before enzymolysis can reduce the error of absolute quantitative analysis of proteins, make the determination results closer to the true value, and effectively improve the reproducibility of analytical results.
Food Allergen Testing
At present, allergic diseases have become a new global problem, so screening and accurate quantification of food allergens is of great significance. Biomarker peptides can be used as internal standards to identify and quantify food allergens.
Existing Strategy for the Synthesis of Deuterated Peptides
Biosynthesis and chemical synthesis are the two main methods for synthesizing stable isotope-labeled polypeptides. Among them, the biosynthesis method is to mark the target site in the physiological metabolism process of animals, plants, enzymes or microorganisms; while the chemical synthesis method is based on the principle of conventional chemical reactions, by using stable isotope-labeled conventional reagents instead of non-labeled basic reagents, then using chemical synthesis to prepare the labeled target compound.
DCL™ in Deuteration of Peptides
With the continuous development of isotope mass spectrometry technology and its wide application in protein detection, the development of stable isotope-labeled peptides has been continuously promoted. The wide application of labeled peptides can further promote their rapid development in new drug research and development, clinical pathology, proteomics, food safety and other fields.
Our DCL™ technology platform provides advanced solutions for deuterium-labeled peptides. Our reactions are highly selective and tolerant to many functional groups and have been successfully applied to the deuteration of many peptide-derived drugs, both simple and more complex. We believe that our method enables faster access to complex, unprotected, radiolabeled peptides.
References
- Legros F, et al. Photoredox‐Mediated Hydrogen Isotope Exchange Reactions of Amino‐Acids, Peptides, and Peptide‐Derived Drugs. Chemistry–A European Journal. 2020, 26(56): 12738-12742.
- Wen Sun, et al. Synthesis and Application of Stable Isotope labeled Peptides. Journal of Isotopes. 2018, 31(06): 390.
Customer Intellectual Property Protection
BOC Sciences has always regarded intellectual property as the most valuable asset of the company and its customers. We have signed non-disclosure agreements with customers and employees before the project starts, and provide synthetic route design and synthesis services in strict accordance with the terms of the non-disclosure agreement, striving to provide customers with target compounds in the shortest time possible.
