Progress in discovery of RORγt inverse agonists for the treatment of autoimmune diseases

LU Lixue; WANG Yonghui

doi:10.11665/j.issn.1000-5048.2023121303

Journal of China Pharmaceutical University > 2024 > 55(1): 87-102. > DOI: 10.11665/j.issn.1000-5048.2023121303

LU Lixue, WANG Yonghui. Progress in discovery of RORγt inverse agonists for the treatment of autoimmune diseases[J]. J China Pharm Univ, 2024, 55(1): 87 − 102. DOI: 10.11665/j.issn.1000-5048.2023121303

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Progress in discovery of RORγt inverse agonists for the treatment of autoimmune diseases

LU Lixue,
WANG Yonghui^,

Department of Medicinal Chemistry, School of Pharmacy, Fudan University, Shanghai 201203, China

Funds: This work was supported by the National Natural Science Foundation of China (No.81874287); and Shanghai Bio-pharmaceutical Science and Technology Supporting Plan (No.19431900100)

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Received Date: December 12, 2023
Available Online: March 05, 2024

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Abstract

Abstract

As a Th17 cell-specific transcription factor, retinoic acid receptor-related orphan receptor γt (RORγt), can induce differentiation of Th17 cells and production of inflammatory factor IL-17, playing an important role in inflammation and autoimmune diseases. RORγt inverse agonists have become a research hotspot in both academia and pharmaceutical companies around the world in recent years, with great development potential. A variety of skeletal structure types have been reported, including orthosteric and allosteric inverse agonists. In this paper, the structure and functions of RORγt are introduced, and RORγt inverse agonists in clinical and preclinical studies are reviewed in order to provide reference for further research and development of RORγt inverse agonists.
- autoimmune diseases,
- Th17 cells,
- RORγt inverse agonists

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References (71)

References

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Progress in discovery of RORγt inverse agonists for the treatment of autoimmune diseases