2021 Fiscal Year Final Research Report
Innovative catalysts for the synthesis of large- and medium-sized molecules bearing glycopeptides
Project/Area Number |
16H06384
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Research Category |
Grant-in-Aid for Scientific Research (S)
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Allocation Type | Single-year Grants |
Research Field |
Chemical pharmacy
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Research Institution | Kyoto University |
Principal Investigator |
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Project Period (FY) |
2016-05-31 – 2021-03-31
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Keywords | 合成化学 / 医薬品化学 / 不斉合成 / 中分子 / 触媒 / 糖類 / ペプチド / 天然有機化合物 |
Outline of Final Research Achievements |
Small molecule drugs, which exhibit biological activity through key-hole interactions, are not good at multi-point molecular recognition of target proteins bearing wide recognition regions. In contrast, mid-molecular drugs are considered more effective and powerful in protein-protein interactions. These "large and medium molecules," which are generally composed of amino acids and sugars, are still not easy to synthesize chemically in large quantities and at low cost due to the size and complexity of their molecular structures. Therefore, we have developed various "artificial organocatalysts" necessary for the efficient synthesis of peptides, oligosaccharides, and glycopeptides composed of natural and unnatural amino acids and monosaccharides. We have established several fundamental technologies for the precision synthesis of new-modality drugs "large and medium-sized molecules", for which demand will increase in the future.
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Free Research Field |
有機合成化学
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Academic Significance and Societal Importance of the Research Achievements |
従来の医薬品は低分子が主流でしたが、年々分子量の増大と分子構造の複雑化が進んでいます。アミノ酸や糖類から構成される「大・中分子」を大量かつ安価に化学合成することは現在でも容易ではなく、多くの課題を残しています。我々はこれら課題を解決する手段として高性能な“合成触媒”を創製し、ペプチドや糖鎖合成に応用しました。今後はバイオ医薬やDDS志向医薬を含め今後需要が増すニューモダリティ医薬品の精密合成への応用が期待されます。
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