Liver Receptor Homolog-1 (LRH-1; NR5A2)

Liver Receptor Homolog-1 Background

LRH-1 is a nuclear receptor that is an essential regulator of gene transcription, critical for early cellular development and imperative for the proper functions of the liver, pancreas, and intestines during the adult life. In the liver, LRH-1 regulates the expression of key genes involved in bile acid synthesis, cholesterol homeostasis and transport. Because of its decisive role in cell differentiation, LRH-1 is linked to multiple developmental pathways. LRH-1 activity is linked to breast and endometrial cancers as well as intestinal tumors and cancer of the pancreas.

This nuclear receptor assay system utilizes proprietary non-human mammalian cells engineered to provide high-level expression of a hybrid form of the Human Liver Receptor Homolog-1 (NR5A2), commonly called LRH-1. The N-terminal DNA binding domains (DBD) of the native LRH-1 has been substituted with that of the yeast GAL4-DBD. The reporter gene is beetle luciferase functionally linked to the GAL4 upstream activation sequence (UAS).

As is true in vivo, these reporter cells express LRH-1 that is constitutively active in the (putative) absence of ligand binding. A ligand binding event may diminish the constitutive activity of the receptor (an inverse-agonist response), or further elevates the already high constitutive activity of LRH-1 (an agonist response).

For more information on LRH-1, visit the Nuclear Receptor Resource.