Searchable abstracts of presentations at key conferences in endocrinology

ea0041ep774 | Nuclear receptors and Signal transduction | ECE2016

Optical isomers of statins enantiospecifically activate pregnane X receptor PXR and induce CYP2A6, CYP2B6 and CYP3A4 in human hepatocytes

Stepankova Martina , Dvorak Zdenek

Statins are drugs used for the treatment of hypercholesterolemia. Statins have two chiral centers in their molecules, thus they form four enantiomers (3R5R-, 3R5S-, 3S5R- and 3S5S-). Regarding the most frequently prescribed statins, following enantiopure formulations are used in the clinics: 3R5R-atorvastatin, 3R5S-rosuvastatin and 3R5S-fluvastatin. Individual enantiomers of one drug can qualitatively and quantitatively differ in their biological activities. In some cases, onl...

ea0037ep149 | Reproduction, endocrine disruptors and signalling | ECE2015

Stereoselective effects of statins on xenobiotic-metabolising pathways

Korhonova Martina , Dvorak Zdenek

Several of currently used drugs are chiral compounds. Majority of them are clinically administered as a racemic (equimolar) mixture of enantiomers. Individual enantiomers of one drug can qualitatively and quantitatively differ in their biological activities (pharmacology, toxicology, pharmacokinetics, etc.). Therefore, enantiopure drugs have been developed and introduced to the therapy. Statins are drugs used to lower cholesterol levels by inhibiting the enzyme HMG-CoA reducta...

ea0037ep193 | Reproduction, endocrine disruptors and signalling | ECE2015

PZ-TR: a novel human luciferase reporter cell line for assessment of thyroid receptor transcriptional activity

Illes Peter , Dvorak Zdenek

Regulation of gene expression mediated by thyroid hormones (THs) plays an essential role in variety of physiological processes. It is known that large group of natural and synthetic compounds, generally termed endocrine disruptors, can interfere with endocrine system and thus disrupt homeostasis of hormonal regulation processes in human organism. In order to screen for substances with potential disrupting effects on TH pathway, we developed and characterized human luciferase r...

ea0049ep805 | Nuclear receptors and Signal transduction | ECE2017

Effects of human interleukins on transcriptional activity of vitamin D receptor in transgenic gene reporter cell lines IZ-VDRE and IZ-CYP24

Bartonkova Iveta , Grycova Aneta , Dvorak Zdenek

Vitamin D receptor (VDR) signalling can be affected with a variety of compounds, both endo- or exogenous. However, any disruption of VDR transcriptional activity can exert severe physiological or pathophysiological outcomes. It is therefore of a great importance to have a reliable in vitro screening technique that would provide a tool for efficient identification of agonists and activators of human VDR. In the current work, we described two novel human reporter cell l...

ea0041ep775 | Nuclear receptors and Signal transduction | ECE2016

The impact of mycophenolate mofetil on androgen receptor activity in prostate cancer cells 22Rv1

Zenata Ondrej , Dvorak Zdenek , Vrzal Radim

Mycophenolate mofetil (MYC) is widely used in transplant medicine as an immunosuppressant drug to prevent rejection in organ transplantation. In this work we investigated the effect of MYC on the activity of androgen receptor (AR) by employing gene reporter assay (GRA) and PCR in prostate cancer cell line 22Rv1.Slight but significant activation of AR was observed for cells treated with MYC in stably transfected 22Rv1 cells (AIZ-AR). Moreover, significant...

ea0041ep776 | Nuclear receptors and Signal transduction | ECE2016

Effect of anthocyanidins on trascriptional activities of steroid and nuclear receptors

Pastorkova Barbora , Illes Peter , Dvorak Zdenek

Anthocyanidins are aglycons of anthocyanins, which are plant pigments responsible for floral and fruits color. Anthocyanidins possess beneficial pharmacological properties such as antioxidant, anti-inflammatory, anti-tumor and anti-diabetic. Anthocyanidins are contained in normal diet and might play role in food-drug interactions.The aim of current study was to evaluate the effects of cyanidin, delphinidin, malvidin, pelargonidin and peonidin on the tran...

ea0037ep655 | Pituitary: basic and neuroendocrinology | ECE2015

Transgenic human gene reporter cell line for evaluating interactions between androgen receptor and xenobiotics

Bartonkova Iveta , Novotna Aneta , Dvorak Zdenek

Androgen receptor (AR, NR3C4) is a 110-kDa ligand-activated transcriptional factor that belongs to the steroid hormone receptor superfamily. It has broad developmental effects and its mutations may have a great impact on pubertal development, genesis of prostatic hyperplasia, and even prostate cancer. Commonly known endogenous ligands of AR are testosterone and 5α-dihydrotestosterone (DHT). In the last years, several drugs and environmental pollutants were identified to a...