nuclear receptor activity

Definition

Target type: molecularfunction

A DNA-binding transcription factor activity regulated by binding to a ligand that modulates the transcription of specific gene sets transcribed by RNA polymerase II. Nuclear receptor ligands are usually lipid-based (such as a steroid hormone) and the binding of the ligand to its receptor often occurs in the cytosol, which leads to its translocation to the nucleus. [GOC:txnOH-2018, PMID:23457262]

Nuclear receptors are a superfamily of transcription factors that regulate gene expression in response to a wide variety of ligands, including hormones, steroids, vitamins, and other small molecules. They play critical roles in a wide range of biological processes, including development, metabolism, reproduction, and immunity. Nuclear receptors are characterized by their modular structure, which consists of a DNA-binding domain (DBD), a ligand-binding domain (LBD), and an N-terminal domain that can contain an activation function (AF-1). The DBD binds to specific DNA sequences called hormone response elements (HREs) in the promoter regions of target genes. The LBD binds to the ligand, which triggers a conformational change in the receptor that activates its transcriptional activity. In the absence of ligand, nuclear receptors are typically located in the cytoplasm and are bound to chaperone proteins. Upon ligand binding, the receptor undergoes a conformational change and translocates to the nucleus, where it binds to HREs and activates gene transcription. The activation of gene transcription by nuclear receptors is a complex process that involves interactions with a variety of co-activators and co-repressors. Co-activators enhance the transcriptional activity of nuclear receptors, while co-repressors inhibit it. The specific co-activators and co-repressors that interact with a given nuclear receptor are often determined by the ligand that is bound to the receptor. In addition to their roles in gene transcription, nuclear receptors also participate in a variety of other cellular processes, including signal transduction, cell cycle regulation, and apoptosis. Nuclear receptors are essential for maintaining normal cellular function and their dysregulation is implicated in a wide range of human diseases, including cancer, diabetes, and cardiovascular disease. '
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Proteins (44)

Compounds (1,094)