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Two steps, one ligand: How PPARγ binds small-molecule agonists
Structure ( IF 4.4 ) Pub Date : 2021-09-02 , DOI: 10.1016/j.str.2021.08.005
James J Siclari 1 , Kevin H Gardner 2
Affiliation  

In this issue of Structure, Shang and Kojetin (2021) present insights into the binding mechanism of artificial agonists to the PPARγ nuclear receptor. These data support a two-step model with induced fit and conformational selection aspects. This mechanism may exist in related receptors, providing new opportunities for drug development.



中文翻译:

两步,一个配体:PPARγ如何结合小分子激动剂

在本期Structure 中, Shang 和 Kojetin (2021) 对人工激动剂与 PPARγ 核受体的结合机制提出了见解。这些数据支持具有诱导拟合和构象选择方面的两步模型。这种机制可能存在于相关受体中,为药物开发提供了新的机遇。

更新日期:2021-09-02
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