Liver receptor homolog-1: structures, related diseases, and drug discovery

  • Acta Pharmacol Sin. 2024 Aug;45(8):1571-1581. doi: 10.1038/s41401-024-01276-x.
Tong Wu  #  1  2 ,  Zhi-Fang Lu  #  1  2 ,  Hao-Nan Yu  2 ,  Xi-Shan Wu  2 ,  Yang Liu  3 ,  Yong Xu  4  5
Affiliations
  • 1. Key Laboratory of Structure-Based Drug Design and Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang, 110016, China.
  • 2. State Key Laboratory of Respiratory Disease, China-New Zealand Joint Laboratory of Biomedicine and Health, Guangdong Provincial Key Laboratory of Biocomputing, Center for Chemical Biology and Drug Discovery, Joint School of Life Sciences, Guangzhou Institutes of Biomedicine and Health, Chinese Academy of Sciences; Guangzhou Medical University, Guangzhou, China.
  • 3. Key Laboratory of Structure-Based Drug Design and Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang, 110016, China. [email protected].
  • 4. Key Laboratory of Structure-Based Drug Design and Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang, 110016, China. [email protected].
  • 5. State Key Laboratory of Respiratory Disease, China-New Zealand Joint Laboratory of Biomedicine and Health, Guangdong Provincial Key Laboratory of Biocomputing, Center for Chemical Biology and Drug Discovery, Joint School of Life Sciences, Guangzhou Institutes of Biomedicine and Health, Chinese Academy of Sciences; Guangzhou Medical University, Guangzhou, China. [email protected].
  • # Contributed equally.
PMID: 38632319 DOI: 10.1038/s41401-024-01276-x
Abstract

Liver receptor homolog-1 (LRH-1), a member of the Nuclear Receptor Superfamily, is a ligand-regulated transcription factor that plays crucial roles in metabolism, development, and immunity. Despite being classified as an 'orphan' receptor due to the ongoing debate surrounding its endogenous ligands, recent researches have demonstrated that LRH-1 can be modulated by various synthetic ligands. This highlights the potential of LRH-1 as an attractive drug target for the treatment of inflammation, metabolic disorders, and Cancer. In this review, we provide an overview of the structural basis, functional activities, associated diseases, and advancements in therapeutic ligand research targeting LRH-1.

Keywords
cancer; liver disease; liver receptor homolog 1; metabolic disorder; nuclear receptor; small molecule modulators.
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