| 研究実績の概要 |
We successfully established a thiopeptide/mRNA display platform that enables the de novo discovery of natural product-like thiopeptides with potential bioactivity and high metabolic stability. This powerful selection platform identified a series of thiopeptide candidates with excellent binding affinity and kinase inhibitory activity against a cancer related protein, TNIK. Additionally, the platform was re-engineered to incorporate more nonproteinogenic amino acids, resulting in thiopeptides with significantly improved metabolic stability while maintaining high bioactivity in vitro. These works have been published in J. Am. Chem. Soc., 2024, 146, 12, 8058-8070.; Org. Lett., 2022, 24, 43, 7894-7899.; J. Am. Chem. Soc., 2022, 144 (44), 20332-20341. And we also submitted the patent PCT/JP2023/035472.
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