Ligand efficacy shifts a nuclear receptor conformational ensemble between transcriptionally active and repressive states

Abstract Nuclear receptors (NRs) are thought to dynamically alternate between transcriptionally active and repressive conformations, which are stabilized upon ligand binding. Most NR ligand series exhibit limited bias, primarily consisting of transcriptionally active agonists or neutral antagonists,...

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Bibliographic Details
Main Authors: Brian S. MacTavish, Di Zhu, Jinsai Shang, Qianzhen Shao, Yuanjun He, Zhongyue J. Yang, Theodore M. Kamenecka, Douglas J. Kojetin
Format: Article
Language:English
Published: Nature Portfolio 2025-02-01
Series:Nature Communications
Online Access:https://doi.org/10.1038/s41467-025-57325-4
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