Discovery of Tertiary Amine and Indole Derivatives as Potent RORγt Inverse Agonists

[Image: see text] A novel series of tertiary amines as retinoid-related orphan receptor gamma-t (RORγt) inverse agonists was discovered through agonist/inverse agonist conversion. The level of RORγt inhibition can be enhanced by modulating the conformational disruption of H12 in RORγt LBD. Linker ex...

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Detalhes bibliográficos
Main Authors: Yang, Ting, Liu, Qian, Cheng, Yaobang, Cai, Wei, Ma, Yingli, Yang, Liuqing, Wu, Qianqian, Orband-Miller, Lisa A., Zhou, Ling, Xiang, Zhijun, Huxdorf, Melanie, Zhang, Wei, Zhang, Jing, Xiang, Jia-Ning, Leung, Stewart, Qiu, Yang, Zhong, Zhong, Elliott, John D., Lin, Xichen, Wang, Yonghui
Formato: Artigo
Idioma:Inglês
Publicado em: American Chemical Society 2013
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC4027777/
https://ncbi.nlm.nih.gov/pubmed/24900774
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/ml4003875
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