Golm1-targeted bufalin-based protac compounds, methods of making and medical uses thereof
By synthesizing PROTAC compounds based on bufotalin, the problems of narrow therapeutic window and insufficient tumor targeting of bufotalin in lung cancer treatment were solved, achieving effective targeted degradation of GOLM1 and lung cancer treatment effects.
CN122404468APending Publication Date: 2026-07-17GUANGZHOU MEDICAL UNIV +1
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Patent Information
- Authority / Receiving Office
- CN · China
- Patent Type
- Applications(China)
- Current Assignee / Owner
- GUANGZHOU MEDICAL UNIV
- Filing Date
- 2026-05-06
- Publication Date
- 2026-07-17
AI Technical Summary
Technical Problem
Existing technologies such as Bufotoxin have drawbacks in treating lung cancer, including a narrow therapeutic window, poor water solubility, low bioavailability, and insufficient tumor targeting. Furthermore, there is a lack of PROTAC compounds that target GOLM1.
Method used
PROTAC compounds based on bufotalin were designed and synthesized. Bufotalin and thalidomide were linked by a linker to form compounds with significantly reduced cytotoxicity and a wider therapeutic window, which can target and degrade GOLM1.
Benefits of technology
It effectively inhibits the proliferation, migration, and invasion of lung cancer cells, induces apoptosis, overcomes the shortcomings of bufotalin, and provides a new therapeutic mechanism for lung cancer.
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Figure CN122404468A_ABST
Abstract
本发明属于生物医药技术领域，公开了一类靶向GOLM1的华蟾毒精类PROTAC化合物及其制备方法与应用。本发明华蟾毒精类PROTAC化合物具体为通过连接子连接的丁二酸酐改性华蟾毒精和沙利度胺。相较于母体化合物华蟾毒精，本发明化合物具有显著降低的细胞毒性和更宽的治疗窗，且可有效靶向并降解GOLM1，有效抑制肿瘤细胞的增殖、迁移和侵袭，并诱导凋亡，从而达到治疗的效果，克服了华蟾毒精治疗窗口窄、肿瘤靶向性不足等缺陷。因此本发明基于华蟾毒精的PROTAC化合物或其药学上可接受盐在制备靶向GOLM1的产品、制备治疗GOLM1蛋白相关疾病药物及治疗肺癌疾病药物等领域中均具有广泛的应用前景。
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