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

Ting Yang; Qian Liu; Yaobang Cheng; Wei Cai; Yingli Ma; Liuqing Yang; Qianqian Wu; Lisa A. Orband‐Miller; Ling Zhou; Zhijun Xiang; Melanie Huxdorf; Wei Zhang; Jing Zhang; Jia‐Ning Xiang; Stewart Leung; Yang Qiu; Zhong Zhong; John D. Elliott; Xichen Lin; Yonghui Wang

doi:10.1021/ml4003875

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Abstract

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 exploration and rational design led to the discovery of more potent indole-based RORγt inverse agonists.

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Yang et al. (2013) studied this question.

synapsesocial.com/papers/6aa8edc6d8988d935da336b5 https://doi.org/10.1021/ml4003875

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

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

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