基本信息:
- 专利标题： caspase-3抑制剂及用途
- 专利标题（英）：CASPASE-3 INHIBITOR AND USE THEREOF
- 申请号：PCT/CN2019/126196 申请日：2019-12-18
- 公开(公告)号：WO2021097980A1 公开(公告)日：2021-05-27
- 发明人： 郝海平 , 曹丽娟 , 许万峰 , 张权
- 申请人： 中国药科大学
- 申请人地址： 中国江苏省南京市鼓楼区童家巷24号, Jiangsu 210009
- 专利权人： 中国药科大学
- 当前专利权人： 中国药科大学
- 当前专利权人地址： 中国江苏省南京市鼓楼区童家巷24号, Jiangsu 210009
- 代理机构： 南京苏高专利商标事务所（普通合伙）
- 优先权： CN201911161593.9 2019-11-22
- 主分类号： C07K5/113
- IPC分类号： C07K5/113 ; A61K38/07 ; A61P1/16
Disclosed are a caspase-3 inhibitor and the use thereof. The caspase-3 inhibitor comprises two molecule forms, the core function regions thereof are respectively DMPD (aspartic acid-methionine-proline-aspartic acid) and DMLD (aspartic acid-methionine-leucine-aspartic acid) polypeptide fragments, and the two ends thereof are respectively subjected to chemical modification to be used for improving the biological characteristics, activity and druggability of a polypeptide. The inhibitor can be directly bound to active caspase-3 to inhibit the enzymic activity thereof, and effectively inhibit apoptosis mediated by caspase-3/PARP and apoptotic necrosis, and apoptosis mediated by caspase-3/GSDME. The caspase-3 inhibitor can be used for preparing tool molecules or reagents related to resisting cell death, and powerful medicines against cell death or diseases associated with necrosis of tissues and organs.
IPC结构图谱:
| C | 化学；冶金 |
| --C07 | 有机化学 |
| ----C07K | 肽 |
| ------C07K5/00 | 在完全确定的序列中含有最多4个氨基酸的肽；其衍生物 |
| --------C07K5/02 | .至少含有1个非正常肽键 |
| ----------C07K5/06 | ..二肽 |
| ------------C07K5/113 | ...第一位氨基酸侧链所含的羧基基团数目多于所含氨基基团数目，或其衍生物，例如Asp、Glu、Asn |