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Nuclear receptors: what and why nuclear receptors are valuable and unique factors in the development of medicine?10th May Lam Thi Phuong Nguyen
Natural science is a potential that has been developed and explored all over the world. In the field of molecular biology and pharmacology, nuclear receptors are a unique element that calls for the discovery and exploitation of scientists. In addition, these nuclear capsules are being widely used in the preparation of drugs. This article will give the reader the most general, simplest view of the nuclear receptors. You do not need to be a scientific researcher to know about this nuclear receptor, you just follow my blog to update your own scientific dictionary!
What is nuclear receptors?
Classification of nuclear receptors
"I AM ONE OF A KIND"WHY ARE NUCLEAR RECEPTORS UNIQUE? An unique property of nuclear receptors that distinguish them from other classes of receptors is the direct interaction and control of the DNA
expression of the genome. NR of the steroid hormones in the cell in association with the heat-shock protein (hsp). Hsp has the effect of maintaining the receptor in the inactive state. In the presence of the substrate (the corresponding
Nuclear receptors (NRs) include receptors located in the cytoplasm that attach to the substrate after the substrate crosses the cell's lipophilic ligands. The receptor-ligand complex moves into the cell nucleus and interacts with the DNA leading to the expression of the target genes for each substrate. Because the final effect of hormonal influences is only made when the receptor-ligand complex interacts with the DNA in the nucleus, the receptor group is called the nuclear receptor (NRs). NRs are considered ligand-mediated transcription factors.
By the expression of a large number of genes from xenobiotic endocrine disruptors which is regulated by nuclear receptors, the ligands activating these receptors which have profound effects on the organism. Hormone-receptor complexes through the hocmon response element lead to the transcription, decoding of genes and expression in the maintenance, development and functioning of organs. Many controlled genes are associated with a variety of diseases, which explains why the molecular targets of about 13 percent of FDA approved drugs are nuclear receptors.
hormones or hormone analogs), the substrate will bind to the receptor causing the hsp to be released. The receptor-ligand receptor complexes through the nuclear membrane interact with the DNA through the receptor
binding site
(DNA binding domain) and the hormone response (HRE) on DNA and play a role starter (promoter) for the synthesis of mRNA. The mRNA promotes the synthesis of specific proteins for each hormone in the cytoplasm with the involvement of the cellular protein synthesizer. NRs play important roles in cellular physiology as well as pathological processes including cancer, metabolic disorders, endocrine disorders, heart disease.
Xenobiotic endocrine disruptors - A lipophilic substance bind to and activate nuclear receptors
Selective Androgen Receptor Modulators (SARMs) - Androgenic drug - Drug class works through nuclear receptors
LAST BUT NOT LEAST! NRs are currently being explored in many biomedical fields to find out the causes and treatments for the disease. Research on substrates (angiotensin-converting enzyme) in these tissues, but resistance to the same hormone (other antagonists) in the tissue are called selective agents. For the nuclear receptor (selective nuclear receptor modulators) for the treatment of
SRMs work by promoting a well-balanced balance of receptors between neo-liberalism and resistance. In tissues where the concentration of coactivator proteins is higher than that of the cores, the equilibrium is shifted in the direction of the agonist. In contrast to the tissues, where the dominant elements dominate, the ligand acts as a villain.This drug has the same effect as sedative drugs such as anabolic steroids but are more selective of their actions, allowing them to be used for more clinical indications than relatively limited legal use. Anabolic steroids are currently approved.
Drugs work through nuclear receptors that express the agonist response in some tissues and react in different tissues. This behavior can have significant benefits as it may allow the desired beneficial effects of a drug to be retained while minimizing unwanted side effects.
Up to now, 100 NRs have been identified and belong to the following groups: Group 1: Includes substrate dependent receptors and has two homologous protein components (homodimer), such as most steroid hormone receptors. Group 2 consists of substrate dependent receptors but may have two homodimer or heterodimer components, such as retinoid X receptor (RXR), thyroid receptor (TR), vitamin D receptor (VDR) .Group 3: Including receptors whose substrate has not been identified or orphan receptors.
hormone dependent diseases such as breast cancer, prostate cancer, metabolic disorders .... is one of many applications from the knowledge on NRs.
ReferencesHörlein, A., Näär, A., Heinzel, T., Torchia, J., Gloss, B., Kurokawa, R., Ryan, A., Kamei, Y., Söderström, M., Glass, C. and Rosenfeld, M. (1995). Ligand-independent repression by the thyroid hormone receptor mediated by a nuclear receptor co-repressor. Nature, 377(6548), pp.397-404.Makishima, M. (1999). Identification of a Nuclear Receptor for Bile Acids. Science, 284(5418), pp.1362-1365.Makishima, M. (1999). Identification of a Nuclear Receptor for Bile Acids. Science, 284(5418), pp.1362-1365.Mangelsdorf, D., Thummel, C., Beato, M., Herrlich, P., Schütz, G., Umesono, K., Blumberg, B., Kastner, P., Mark, M., Chambon, P. and Evans, R. (1995). The nuclear receptor superfamily: The second decade. Cell, 83(6), pp.835-839.
