A group of Professor Hisashi Yamamoto and his colleagues at Chubu University succeeded in developing an efficient new synthetic method for peptides (protein fragments), paving the way for cost reduction of medium-molecular-weight drugs that use peptides in their skeletons.

 While small molecule drugs, which are currently the mainstream, are inexpensive and easy to reach the affected area, they are likely to spread to areas other than the affected area and cause side effects.Therefore, in the future, it is expected that medium-molecular-weight peptide drugs that act only on the target and have the right size will play a leading role, but the high cost of peptide synthesis has become a bottleneck and has hardly been put into practical use. ..

 In this study, we have developed a synthetic method to obtain an overwhelmingly inexpensive and high-purity peptide by using a special catalyst called Lewis acid.Unlike the conventional linear solid-phase synthesis, we succeeded in the convergent liquid phase synthesis, so the number of steps could be significantly reduced and the production cost was less than 1000/1 of the conventional method.In addition, since "racemization" (the formation and mixing of foreign optical isomers), which could not be prevented until now, will not occur, it will be possible to provide a large amount of high-purity peptides to the market.In addition, it produces almost no environmentally-friendly waste such as wastewater and harmful substances that cannot be avoided by the conventional method, and it is an extremely environmentally friendly method.

 This result will not only lead to the full-scale commercialization of peptide drugs.The fields of application of peptides extend from general materials to electronic components.If inexpensive peptides become available, they are expected to be widely used in various materials, cosmetics, pesticides, and other industries in the future, in addition to peptide fibers, which are said to be stronger than iron and carbon fibers.

Paper information:[Journal of the American Chemical Society] Substrate-Directed Lewis-Acid Catalysis for Peptide Synthesis

Chubu University
Chubu University

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