Abstract
本发明公开了一种靶向Beclin1的订书肽、药物组合物，其中，所述订书肽包含的氨基酸序列与Beclin1氨基酸残基191‑205至少有66.7％相同，所述订书肽中的E195氨基酸残基和N202氨基酸残基被一个全碳氢链连接起来以稳定其α‑螺旋结构。本发明将全碳氢链放置在订书肽中离Beclin 1卷曲螺旋域‑订书肽结合界面更近的位置，可使其与Beclin1的结合亲和力提高10‑30倍。与其他自噬诱导剂如雷帕霉素和Tat‑Beclin 1肽相比，本发明优化的订书肽在HER2阳性癌细胞中不仅能诱导自噬，还能显著增强细胞表面致癌受体EGFR和HER2的内体‑溶酶体降解。
| Translated title of the contribution | Beta-globin 1-targeted staple peptide and pharmaceutical composition |
|---|---|
| Original language | Chinese (Simplified) |
| Patent number | 2021105185860 |
| Filing date | 12/05/21 |
| Publication status | Published - 17 May 2022 |
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