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Nuclear receptors (NRs) are transcription factors (TFs) involved in diverse biological activities, such as cell proliferation, embryogenesis, differentiation, homeostasis, metabolism, and immunity. The NR superfamily has been implicated in many pathologies such as cancer, cardiovascular disease, inflammation, and reproductive abnormalities. The expression of different NRs has been well explored in various cancers, and they have been shown to have oncogenic or tumor-suppressive functions. NRs associated with cancer include retinoic acid receptor (RAR), retinoid X receptor (RXR), peroxisome proliferator-activated receptor gamma (PPARγ), and vitamin D receptor (VDR). Due to their physiological activation via low-molecular-mass ligands, many NRs have been recognized as tractable small-molecule therapeutic targets through extensive studies.
Our Nuclear Receptor Stable Cell Lines
Stable cell lines are important tools for drug screening, gene function studies, or protein production. Creative Biogene has proven its success in the generation and validation of stable cell lines to accelerate your novel drug discoveries and biomedical research. Fully-validated, we have generated a unique collection of nuclear receptor stable cell lines to provide powerful assay platforms for all research projects.
Key Features of Our Nuclear Receptor Stable Cell Lines
To date, 48 different NRs have been discovered in humans. NR recognizes and binds small molecules, including steroid and thyroid hormones, vitamins, and fatty acids and their derivatives. Members of this family contain an N-terminal transactivation domain, a highly conserved central region zinc-finger DNA-binding domain, and a C-terminal ligand-binding domain. Binding of a ligand to its associated nuclear receptor results in transactivation of specific genes within the target tissue. Multiple members of the NR superfamily are involved in a variety of diseases, making this class of transcription factors extremely attractive to the pharmaceutical industry.
Figure 1. Assembly of nuclear receptors and their interaction partners. (Kronenberger T, et al., 2015)
The use of nuclear receptor stable cell lines in biomedical research has revolutionized the study of nuclear receptor signaling pathways and their role in human health and disease. These cell lines are engineered to express specific nuclear receptor genes, providing researchers with valuable tools to study the molecular mechanisms of receptor activation, gene regulation, and identification of novel receptor ligands.
Applications for nuclear receptor stable cell lines include:
Case Study 1
The nuclear receptor (NR) superfamily contains hormone-induced transcription factors that regulate many physiological and pathological processes by modulating gene expression. NR4A1 is a member of the NR family for which no endogenous ligand has yet been identified. Studies here show that NR4A1 protein expression decreases during tumor progression in mouse basaloid mammary tumors as well as in most human triple-negative breast cancer (TNBC) tumors. The researchers also demonstrated that expression of NR4A1 in MDA-MB-231 cells significantly inhibited the proliferation, viability, migration, and invasion of these cells in culture, as well as the growth and metastasis of these cell-derived tumors in mice.
The study found that the growth rate of NR4A1 overexpressing stable cells was reduced by more than 2 times compared with control cells. NR4A1 overexpressing stable cells formed 4-5 times fewer colonies than control cells. NR4A1 overexpressing stable cells were also much smaller in size and contained significantly fewer cells than colonies formed by control cells. The ability of NR4A1 overexpressing cells to migrate on culture plates and invade the Matrigel layer was also significantly reduced. These results indicate that the expression of NR4A1 in MDA-MB-231 TNBC cells can effectively inhibit cell proliferation, viability, motility, and invasion.
Figure 2. NR4A1 expression inhibits the growth, viability, migration and invasion of MDA-MB-231 cells. Stable MDA-MD-231 cell lines with NR4A1 expression (designated as 231-NR4A1#1 and 231-NR4A1#2 cells) and their control cells (designated as 231-Ctrl cells). (Wu H, et al., 2017)
Q: What are Nuclear Receptors?
A: Nuclear receptors are a class of proteins found within cells that are capable of binding to specific molecules, such as hormones, vitamins, or drugs. They function as transcription factors, meaning they can regulate the expression of genes by controlling the production of messenger RNA (mRNA) from DNA.
Q: What diseases are implicated with dysregulation of nuclear receptor signaling?
A: Dysregulation of nuclear receptor signaling has been implicated in a wide range of diseases including cancer, diabetes, and cardiovascular disorders.
Q: What types of host cells can be used to generate stable cell lines?
A: Host cells can include immortalized cell lines, primary cells, or stem cells, depending on the research objectives.
Q: What is the main advantage of using stable cell lines over transient transfection models?
A: The main advantage of using stable cell lines over transient transfection models is the stability of receptor expression, which allows for long-term studies without the need for repeated transfection experiments. This stability is achieved through the integration of the exogenous gene into the host cell genome, ensuring sustained and consistent receptor expression.
Q: Can nuclear receptor stable cell lines be used for high-throughput screening?
A: Yes, stable cell lines provide a platform for high-throughput screening of potential receptor ligands. By using these cell lines in automated screening assays, researchers can rapidly identify compounds that modulate receptor activity. This approach has been particularly successful in the discovery of agonists or antagonists for nuclear receptors, which can be further developed as potential therapeutics for various diseases.
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