Identification of Marine-Derived SLC7A11 Inhibitors: Molecular Docking, Structure-Based Virtual Screening, Cytotoxicity Prediction, and Molecular Dynamics Simulation

被引:1
作者
Chen, Jiaqi [1 ]
Li, Xuan [1 ]
Tao, Jiahua [1 ]
Luo, Lianxiang [2 ]
机构
[1] Guangdong Med Univ, Clin Coll 1, Zhanjiang 524023, Peoples R China
[2] Guangdong Med Univ, Marine Biomed Res Inst Guangdong Zhanjiang, Sch Ocean & Trop Med, Zhanjiang 524023, Peoples R China
关键词
ferroptosis; marine natural compound; virtual screening; fragment substitution; molecular dynamics simulation; LEAST-SQUARES PLS; FERROPTOSIS; METABOLISM; QSAR;
D O I
10.3390/md22080375
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The search for anticancer drugs that target ferroptosis is a promising avenue of research. SLC7A11, a key protein involved in ferroptosis, has been identified as a potential target for drug development. Through screening efforts, novel inhibitors of SLC7A11 have been designed with the aim of promoting ferroptosis and ultimately eliminating cancer cells. We initially screened 563 small molecules using pharmacophore and 2D-QSAR models. Molecular docking and ADMET toxicity predictions, with Erastin as a positive control, identified the small molecules 42711 and 27363 as lead compounds with strong inhibitory activity against SLC7A11. Further optimization resulted in the development of a new inhibitor structure (42711_11). Molecular docking and ADMET re-screening demonstrated successful fragment substitution for this small molecule. Final molecular dynamics simulations also confirmed its stable interaction with the protein. These findings represent a significant step towards the development of new therapeutic strategies for ferroptosis-related diseases.
引用
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页数:20
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