药效团
虚拟筛选
小分子
分子动力学
对接(动物)
细胞毒性
生物信息学
数量结构-活动关系
计算生物学
化学
组合化学
生物
生物化学
立体化学
计算化学
体外
基因
医学
护理部
作者
Jiaqi Chen,Xuan Li,Jiahua Tao,Lianxiang Luo
出处
期刊:Marine Drugs
[Multidisciplinary Digital Publishing Institute]
日期:2024-08-20
卷期号:22 (8): 375-375
被引量:1
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.
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