Human Glucocorticoid Receptor (GR, NR3C1) Stable Cells (Mitochondria Specific)

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Nuclear hormone receptors (NHRs) are a superfamily of transcription factors that function as powerful metabolic regulators to control a variety of systemic processes in physiology. They also play key roles in the pathophysiology of many major disease states, such as diabetes, obesity, inflammation, atherosclerosis and heart failure. To date, this superfamily has provided a rich source of drug design targets and it is continuing to be one of the hottest areas for pharmaceutical research.

Humimmu now provides a comprehensive set of NHR expressing cell lines to the research community. These high-quality, Flag and/or HA-tagged NHR-expressing cell lines aim to facilitate further biochemical and molecular studies of their functions and hence encourage new strategies for drug design.

Glucocorticoids (GCs) are steroid hormones that allow us to cope with environmental and physiological stresses. Although GCs are widely used as anti-inflammatory agents in several clinical areas, long-term use of those steroids causes problems instead. Full achievement of the clinical potential of GCs necessitates limiting the side effects of these drugs.

The lipophilic nature of GCs allows them to readily diffuse into the cells, where they bind to a cytosolic receptor, the Glucocorticoid Recetpor (GR) to exert their mechanism of action. Without ligand binding, GR is predominantly localized in cytoplasm, whereas upon ligand binding it rapidly translocates to nucleus where it can both positively and negatively regulate gene expression. GR belongs to the nuclear receptor superfamily of ligand-activated transcription factors that function as powerful metabolic regulators. Several studies have shown that GR also translocates to the mitochondrial in addition to its nuclear translocation in response to GC treatment. The mitochondrial GR translocation has been shown to be positively correlated with GC-induced apoptosis, although the mechanism is unclear.

The mitochondrial-specific GR (Flag and HA tagged)/HEK293 cell line was created by stable transfection of HEK293 cells with a plasmid expressing Flag and HA tagged GR protein with a mitochondrial localization signal.

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