Other Receptor Research

The nuclear receptor superfamily can be generally divided into four major subfamilies based on their DNA-binding properties and dimerization preferences. However, this classification is rather broad and does not take into account of any evolutionary relationship between nuclear receptors. Therefore, a new phylogeny-based nomenclature approved by the Nuclear Receptor Nomenclature 

Thyroid hormone receptor TRa NR1A1 thyroid hormone 

Retinoic acid receptor RARa NR1B1 retinoic acid 

Peroxisome proliferator- PPARa NR1C1 fatty acids, 

Reverse erbA Rev-erba NR1D1 prostaglandin J2 orphan 

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The harmful effects of air pollutants on human beings have been the major reason for efforts to understand and control their sources. During the past two decades, research on acidic deposition on water-based ecosystems has helped to reemphasize the importance of air pollutants in other receptors, such as soil-based ecosystems (1). When discussing the impact of air pollutants on ecosystems, the matter of scale becomes important. We will discuss three examples of elements which interact with air, water, and soil media on different geographic scales. These are the carbon cycle on a global scale, the sulfur cycle on a regional scale, and the fluoride cycle on a local scale. 

The second major difficulty is that cells and tissues in the body are exposed to numerous metabolites displaying different structures compared to the parent molecules present in plant foods. For example, it has been suggested that the metabolites of lycopene may be responsible for reducing the risk of developing prostate cancer. These metabolites may interact with nuclear receptors such as PPARs, LXR, and others. " Future research is needed to produce metabolites (enzymatically or chemically) in order to elucidate their cellular mechanisms and thus clarify their effects on human health. 

The search for an effective non-peptide oxytocin antagonist has become a major goal of a number of pharmaceutical companies because of the poor pharmacokinetic properties and especially the lack of oral bioavailability associated with peptidic antagonists. Early research in this field was dominated by Merck, but in recent years significant research efforts at GlaxoSmithKline and Serono have been published. A number of other companies, notably Sanofi-Aventis, Yamanouchi and Wyeth, have had a major presence in vasopressin receptor research and oxytocin is frequently included in patent claims for the molecules. Occasionally, oxytocin-selective compounds have been reported, usually derived by adaptation of the vasopressin antagonist template. 

Certain biomolecules can be added into the bead or be attached to its surface. These mostly include such recognition elements as antibodies, oligonucleotides or other receptors such as conconovalin A. Enzymes can be used to design biosensors (e.g., for glucose) on a microscale but this research is still in its infancy. Finally, fluorescent proteins can be used as alternative to the dyes. The same refers to quantum dots which can also be used in principle. 

In line with the situation found previously for the other receptor families, several classification schemes coexist for nuclear receptors. In particular, beyond the NC-IUPHAR system described above, an alternative nomenclature system has been proposed and is currently widely accepted and used by the research community working in this family. This annotation scheme consists of a 3-character code. The first character is a number that designates... 

Many researchers have come to believe that schizophrenia is a complex disease, possibly with a number of different causes or courses. PET studies of schizophrenia have found possible contributions of other receptors, including the dopamine D receptor as well as receptors for other neurotransmitters such as glutamate. Genetic researchers are searching for the genes involved in the expression and regulation of these receptors, any or all of which may be involved in some number of patients. 

One possibility would be to use labeled octopamine, itself, and to perform ligand binding studies of the type which are frequently used in mammalian neurotransmitter receptor research. The problem with this approach is that octopamine binds, to a large extent, to octopamine receptors other than those associated with adenylate cyclase. Thi is shown by the fact that the binding affinity reported for H-octopamine in insect nerve tissue is in the low... 

Two other novel approaches have recently been reported in the field of ER ligand discovery. The potential of compounds as pathway-selective ligands and antiinflammatory agents was studied by the use of NFKB-driven reporter assays [64], A second relatively recent focus for ER-directed drug discovery is related to the fact that there are two subtypes of this receptor, ERa and ER 1, which derive from two separate genes [65, 66], Stimulated by the specific tissue distribution pattern of these two related receptors, research to find ER subtype-selective modulators for the treatment... 

A major problem in ct receptor research is the lack of specific ligands as most of these agents bind at other receptor systems including serotonin 5-HT2, dopamine D2, PCP, and muscarinic receptors, thus making it unclear whether their pharmacological properties are due to the interaction with cr sites. Some specific compounds are emerging here two examples are quoted NE 100, which also displays an cr,/o 2 selectivity ratio of 55, reported to... 

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