靶向FIGNL1-FIRRM-MACIR复合体的抑制剂在制备肿瘤药物中的应用及其组合物

By targeting the FIGNL1-FIRRM-MACIR complex, the problem of platinum-based drug resistance in tumors such as ovarian cancer has been solved. MACIR promotes the dissociation of RAD51 filaments, thereby enhancing the efficacy of chemotherapy.

CN122005808BActive Publication Date: 2026-07-17NAT HEALTH COMMISSION INST OF SCI & TECH

Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
NAT HEALTH COMMISSION INST OF SCI & TECH
Filing Date
2026-04-09
Publication Date
2026-07-17

AI Technical Summary

Technical Problem

Existing technologies have difficulty effectively targeting the FIGNL1-FIRRM-MACIR complex, leading to drug resistance issues in platinum-based drugs in tumors such as ovarian cancer, thus affecting the efficacy of chemotherapy.

Method used

Develop inhibitors targeting the FIGNL1-FIRRM-MACIR complex, knock down MACIR with small molecule compounds or siRNA to enhance the sensitivity of ovarian cancer cells to platinum-based drugs, and utilize MACIR as a bridge-like adaptor subunit of FIGNL1-FIRRM unfolding enzyme to promote the dissociation of RAD51 filament structure and DNA damage repair.

Benefits of technology

It significantly enhanced the cytotoxicity of ovarian cancer cells to platinum-based drugs, improved the sensitivity and efficacy of chemotherapy, and solved the problem of platinum resistance.

✦ Generated by Eureka AI based on patent content.

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Abstract

本发明提供靶向FIGNL1‑FIRRM‑MACIR复合体的抑制剂在制备肿瘤药物中的应用及其组合物。本研究鉴定MACIR为FIGNL1‑FIRRMAAA+ATP酶复合体的桥梁样适配亚基。MACIR通过直接结合FIRRM和DNA,促进FIGNL1介导的RAD51丝状结构解折叠,从而促进醛类或铂类药物诱导的DNA链间交联(ICLs)损伤修复并维持基因组稳定性。对FIGNL1‑FIRRM‑MACIR复合体进行药理学抑制,包括使用两种针对FIGNL1‑FIRRM‑MACIR复合体的抑制剂4‑{2‑[(5‑氯‑2‑甲氧基苯胺基)羰基]苯胺基}‑4‑氧代丁酸和2‑{[5‑(2‑乙氧基乙基)‑4‑羟基‑6‑氧代‑1,6‑二氢‑2‑嘧啶基]硫基}‑N‑(3‑甲氧基苯基)乙酰胺,可显著增强铂类药物在卵巢癌中的细胞毒效应。
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