Drug discovery targeting thyroid hormone receptor β (THRβ) for the treatment of liver diseases and other medical indications.
10.1016/j.apsb.2024.07.025
- Author:
Kean WANG
1
;
Feiyang CHEN
2
;
Jiang WANG
2
;
Hong LIU
1
Author Information
1. School of Chinese Materia Medica, Nanjing University of Chinese Medicine, Nanjing 210023, China.
2. Lingang Laboratory, Shanghai 200031, China.
- Publication Type:Review
- Keywords:
MASH;
MASLD;
THRβ agonist;
Thyroid hormone;
Thyroid hormone β receptor
- From:
Acta Pharmaceutica Sinica B
2025;15(1):35-51
- CountryChina
- Language:English
-
Abstract:
Thyroid hormone receptors (THRs), a crucial nuclear receptor protein family, primarily consist of two categories: α receptors and β receptors. Among them, THRβ is the primary subtype of thyroid hormone that confers benefits to the liver. In the last two decades, there have been efforts to develop THRβ agonists that selectively yield beneficial effects on the liver, such as lowering triglycerides and cholesterol, while reducing adverse effects on the heart, muscle, and bone. This paper systematically reviews strategies to enhance the safety of THRβ agonists for the treatment of MASH, with a focus on improving the selectivity of THRα and increasing the distribution of the drug in the liver. Additionally, we explore the potential application of this target in addressing other medical indications.