Development of nulecytoplasmic shuttlepeptide and its applicatution for controlling distribution of disease related protein

在一些难治性疾病中，可以观察到细胞核中与疾病相关的突变蛋白的积累。为了治疗这些疾病，从细胞核中消除突变蛋白被认为是适用的。因此，我们决定开发一种核细胞质穿梭肽，它在受到刺激之前在细胞核内跳动，但在受到刺激后返回细胞质，具有从细胞核中消除突变蛋白的潜在适用性。结果，我们成功地开发了几种刺激反应氨基酸，这些氨基酸可用于刺激控制肽基功能，并实现了刺激反应氨基酸的关键合成中间体的不对称合成。

Accumulation of a disease related mutated protein in a nucleus is observed in some intractable diseases. To treat these diseases, elimination of the mutated protein from nucleus is thought to be applicable. Therefore, we decided to develop a nucleocytoplasmic shuttle peptide, which beats inside a nucleus before exposure to a stimulus but it returns to a cytoplasm after exposure to a stimulus, with potential applicability to eliminate the mutated protein from a nucleus. As a results, we sucsessfully developed several stimulus-responsive amino acids which can be used for controlling a peptidyl function by a stimulus, and asymmetric synthesis of a key synthetic intermediate of the stimulus-responsive amino acids was achieved.