Dual-target inhibitors of colchicine binding site for cancer treatment

Eur J Med Chem. 2024 Aug 5:274:116543. doi: 10.1016/j.ejmech.2024.116543.

Lu Lu ¹, Keke Li ¹, Jiaxin Pu ¹, Shaochi Wang ², Tingting Liang ³, Jianhong Wang ⁴

Affiliations

1 Henan Key Laboratory of Natural Medicine Innovation and Transformation, Henan University, Kaifeng, Henan Province, 475004, China.
2 Translational Medicine Center, The First Affiliated Hospital of Zhengzhou University, Zhengzhou, Henan Province, 450052, China.
3 Henan Key Laboratory of Natural Medicine Innovation and Transformation, Henan University, Kaifeng, Henan Province, 475004, China; The Zhongzhou Laboratory for Integrative Biology, Henan University, Zhengzhou, Henan Province, 450000, China. Electronic address: [email protected].
4 Henan Key Laboratory of Natural Medicine Innovation and Transformation, Henan University, Kaifeng, Henan Province, 475004, China. Electronic address: [email protected].

PMID: 38823265 DOI: 10.1016/j.ejmech.2024.116543

Abstract

Colchicine binding site inhibitors (CBSIs) have attracted much attention due to their antitumor efficacies and the advantages of inhibiting angiogenesis and overcoming multidrug resistance. However, no CBSI has been currently approved for Cancer treatment due to the insufficient efficacies, serious toxicities and poor pharmacokinetic properties. Design of dual-target inhibitors is becoming a potential strategy for Cancer treatment to improve Anticancer efficacy, decrease adverse events and overcome drug resistance. Therefore, we reviewed dual-target inhibitors of colchicine binding site (CBS), summarized the design strategies and the biological activities of these dual-target inhibitors, expecting to provide inspiration for developing novel dual inhibitors based on CBS.

Keywords

Anticancer efficacy; Colchicine binding site; Drug resistance; Dual-target inhibitors.

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