Visualizing the action of steroid hormone receptors in living cells

Abstract

Transcription controlled by Steroid Hormone Receptors (SHRs) plays a key role in many important physiological processes like organ development, metabolite homeostasis, and response to external stimuli. Understandably, the members of this family have drawn a lot of attention from the scientific community since their discovery, four decades ago. Still, after many years of research we are only beginning to unravel the complex nature of these receptors. The pace at which we do has improved significantly in recent years with the discovery of genetically encoded fluorescent probes, and the accompanying revival of biophysical approaches that allow more detailed study of SHRs. Here, we will look into the different aspects of SHR signalling, and discuss how biophysical techniques have contributed to visualizing their function in their native context, the living cell.

A multi‐parameter imaging assay identifies different stages of ligand‐induced androgen receptor activation

“…A similar principle was used on full length ER and AR, tagged with YFP and CFP at both termini (14,(50)(51)(52)(53). In the AR, the conformational change is a direct result of the ligandinduced AR N/C-interaction (14,52,53).…”

Thermodynamic Dissection of the Intrinsically Disordered N-terminal Domain of Human Glucocorticoid Receptor

“…GR is a hormone-dependent nuclear transcription factor in the steroid hormone receptor family that contains three modular domains: the ID NTD (GR 1-420), the DNA binding domain , and the ligand binding domain (GR 528 -777). The ID NTDs for steroid hormone receptors are extremely important for transcription regulation, serving as hubs to recruit co-regulators that form the final transcription complex (13)(14)(15). Within the human GR NTD, mutational mapping has identified a subregion, termed the activation function-1 (AF1) region, which comprises residues 77-262 and is essential for the full transcriptional activity of the receptor (16).…”

Hormone replacement therapy after treatment for a gynaecological malignancy

“…Ligand-binding results in a conformational change of the receptor followed by nuclear translocation [9]. In the nucleus, the steroid receptor binds to specific palindromic DNA sequences resulting in chromatin remodelling, recruitment of factors needed for transcription of specific genes in target cells [9][10][11].…”