Endogenous and Exogenous Ligands of Aryl Hydrocarbon Receptor: Current State of Art.

02:13 EDT 22nd September 2014 | BioPortfolio

Summary of "Endogenous and Exogenous Ligands of Aryl Hydrocarbon Receptor: Current State of Art."

Aryl hydrocarbon receptor (AhR) is an important transcriptional regulator of drug metabolizing enzymes that dominantly controls the expression of cytochrome P450 CYP1 family genes and some phase II enzymes. AhR also has many endogenous functions including cell cycle control, immune response, and cell differentiation. In addition, AhR is well-known to be involved in chemicallyinduced carcinogenesis. AhR is activated by a variety of endogenous and exogenous ligands. While exogenous activation of AhR has deleterious effects on human organism, sustained activation of AhR by endogenous ligands is indispensable for proper cell functions. Therefore, the effects of exogenous and endogenous ligands on AhR resemble the Dr. Jekyll and Mr. Hyde story. The aim of the current paper is to summarize and update the knowledge on exogenous and endogenous AhR ligands.

Affiliation

Department of Pharmacology and Toxicology, Faculty of Pharmacy in Hradec Kralove, Heyrovskeho 1203, Hradec Kralove 50005, Czech Republic. petr.pavek@faf.cuni.cz.

Journal Details

This article was published in the following journal.

Name: Current drug metabolism
ISSN: 1875-5453
Pages:

Links

PubMed Articles [21652 Associated PubMed Articles listed on BioPortfolio]

A tryptophan metabolite, kynurenine, promotes mast cell activation through aryl hydrocarbon receptor.

Tryptophan metabolites have been suggested to play a role in immune modulation, wherein those have recently been shown to be endogenous ligands of aryl hydrocarbon receptor (AhR; a unique cellular che...

Identification of Cinnabarinic Acid as a Novel Endogenous Aryl Hydrocarbon Receptor Ligand That Drives IL-22 Production.

The aryl hydrocarbon receptor (AHR) binds to environmental toxicants including synthetic halogenated aromatic hydrocarbons and is involved in a diverse array of biological processes. Recently, the AHR...

Aryl hydrocarbon receptor exogenous ligand 3-methylchoranthrene inhibited endometrial cancer cells proliferation.

Endometrial cancer (EC) is the most prevalent gynecologic malignancy among women worldwide. Increasing evidence has disclosed the potential role of aryl hydrocarbon receptor (AhR) in the cancer develo...

In vivo application of the pure aryl hydrocarbon receptor antagonist GNF-351 is limited to the gastrointestinal track.

GNF-351 is a potent aryl hydrocarbon receptor (AHR) antagonist with the ability to inhibit dioxin response element-dependent and independent activities. The present study aimed to investigate the abso...

Endogenous aryl hydrocarbon receptor promotes basal and inducible expression of tumor necrosis factor target genes in MCF-7 cancer cells.

The aryl hydrocarbon receptor (AHR) is a ligand-activated transcription factor that upon activation by the toxicant 2,3,7,8 tetrachlorodibenzo-p-dioxin (TCDD) stimulates gene expression and toxicity. ...

Clinical Trials [2199 Associated Clinical Trials listed on BioPortfolio]

Exogenous Reinfection of Tuberculosis in Taiwan

we hypothesize that exogenous reinfection is very important in the Taiwan endemic. Therefore, we design a series of studies to evaluate the individual contribution of exogenous reinfection...

GPR 119 Stimulated GLP-1 Secretion

The purpose of this study is to evaluate the impact of different ligands of GPR 119 (a G protein-coupled receptor in the intestine) on the secretion of the incretin hormones, GLP-1 and GIP...

Effects of Ghrelin on the Sleep-EEG and Nocturnal Secretion of Hormones

Ghrelin, an acylated peptide consisting of 28 amino acids, is the endogenous ligand of the growth hormone secretagogue receptor (GHS-R). It is synthesized predominantly in the stomach but ...

Role of CXCR2 Ligands/CXCR2 Biological Axis in Pancreatic Cancer

The investigators hypothesize that the CXCR2 ligands/CXCR2 biological axis plays an important role in promoting angiogenesis in PC; and that the genetic changes and the microenvironment of...

Study of Endogenous Inhibitory Modulation During Gastric and Somatic Stimulation

Visceral hypersensitivity as evidence of central sensory sensitization is evident in many patients with functional disorders such as functional dyspepsia (FD) and irritable bowel syndrome ...

Medical and Biotech [MESH] Definitions

Aryl hydrocarbon receptor nuclear translocator is a basic HELIX-LOOP-HELIX MOTIF containing protein that forms a complex with DIOXIN RECEPTOR. The complex binds xenobiotic regulatory elements and activates transcription of a variety of genes including UDP GLUCURONOSYLTRANSFERASE. AhR nuclear translocator is also a subunit of HYPOXIA-INDUCIBLE FACTOR 1.

Cell membrane proteins that bind opioids and trigger intracellular changes which influence the behavior of cells. The endogenous ligands for opioid receptors in mammals include three families of peptides, the enkephalins, endorphins, and dynorphins. The receptor classes include mu, delta, and kappa receptors. Sigma receptors bind several psychoactive substances, including certain opioids, but their endogenous ligands are not known.

Cytoplasmic proteins that bind certain aryl hydrocarbons, translocate to the nucleus, and activate transcription of particular DNA segments. AH receptors are identified by their high-affinity binding to several carcinogenic or teratogenic environmental chemicals including polycyclic aromatic hydrocarbons found in cigarette smoke and smog, heterocyclic amines found in cooked foods, and halogenated hydrocarbons including dioxins and polychlorinated biphenyls. No endogenous ligand has been identified, but an unknown natural messenger with a role in cell differentiation and development is suspected.

Drugs that bind to but do not activate GABA-B RECEPTORS thereby blocking the actions of endogenous or exogenous GABA-B RECEPTOR AGONISTS.

Drugs that bind to but do not activate GABA-A RECEPTORS thereby blocking the actions of endogenous or exogenous GABA-A RECEPTOR AGONISTS.

Search BioPortfolio:
Loading
Advertisement

Relevant Topic

Pharmacy
Latest News Clinical Trials Research Drugs Reports Corporate
Pharmacy is the science and technique of preparing as well as dispensing drugs and medicines. It is a health profession that links health sciences with chemical sciences and aims to ensure the safe and effective use of pharmaceutical drugs. The scope of...

Advertisement