一种真核生物I型拓扑异构酶抑制剂及其应用
By designing and synthesizing G-quadruplex-double-stranded complexes to target Topo I, the shortcomings of existing nucleic acid-based Topo I inhibitors have been overcome, achieving highly efficient and stable inhibition of Topo I, which is suitable for the development of anticancer drugs.
CN115873857BActive Publication Date: 2026-07-17NANJING FORESTRY UNIV
Patent Information
- Authority / Receiving Office
- CN · China
- Patent Type
- Patents(China)
- Current Assignee / Owner
- NANJING FORESTRY UNIV
- Filing Date
- 2022-08-25
- Publication Date
- 2026-07-17
AI Technical Summary
Technical Problem
Current research on inhibitors of eukaryotic type I topoisomerases mainly focuses on small organic molecule compounds, while research on nucleic acid Topo I inhibitors is limited and lacks effective inhibitory effects and stability.
Method used
We designed and synthesized a G-quadruplex-double-stranded complex with G-quadruplex and Topo I binding sites, and optimized its inhibitory ability on Topo I by targeting Topo I to form a closed cyclic nucleotide complex.
Benefits of technology
It achieves highly targeted inhibition of Topo I, exhibits good thermal stability and nuclease resistance, and has a half-maximal inhibitory concentration (IC50) of 54.8 nM, making it suitable for the preparation of anticancer drugs.
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Figure CN115873857B_ABST
Abstract
本发明公开了一种真核生物I型拓扑异构酶抑制剂及其应用，涉及抗癌药物领域，所述抑制剂为具有G‑四链体和Topo I结合位点的G‑四链体‑双链复合体，所述G‑四链体‑双链复合体为闭合环状核苷酸复合体，所述G‑四链体‑双链复合体的核苷酸序列如SEQ ID NO.1所示。本发明的I型拓扑异构酶抑制剂，具有良好的热稳定性和核酸酶耐受性，细胞摄取率高并且对真核生物I型拓扑异构酶具有高度靶向性，对真核生物I型拓扑异构酶的活性具有较高的抑制效果，半抑制浓度IC50值为54.8nM。
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