Related Experiment Video
Updated: Feb 14, 2026

Quantifying Agonist Activity at G Protein-coupled Receptors
Published on: December 26, 2011
From RORγt Agonist to Two Types of RORγt Inverse Agonists
Yonghui Wang1, Wei Cai2, Ting Tang1
1School of Pharmacy, Fudan University, 826 Zhangheng Road, Pudong, Shanghai 201203, China.
Abstract:
Biaryl amides as new RORγt modulators were discovered. The crystal structure of biaryl amide agonist 6 in complex with RORγt ligand binding domain (LBD) was resolved, and both "short" and "long" inverse agonists were obtained by removing from 6 or adding to 6 a proper structural moiety. While "short" inverse agonist (8) recruits a corepressor peptide and dispels a coactivator peptide, "long" inverse agonist (9) dispels both. The two types of inverse agonists can be utilized as potential tools to study mechanisms of Th17 transcriptional network inhibition and related disease biology.
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