Binding of ligands to the aryl hydrocarbon receptor: An overview of methods

Kód výsledku v IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F61989592%3A15310%2F25%3A73631533" target="_blank" >RIV/61989592:15310/25:73631533 - isvavai.cz</a>

Výsledek na webu

<a href="https://www.sciencedirect.com/science/article/pii/S0378427425000098" target="_blank" >https://www.sciencedirect.com/science/article/pii/S0378427425000098</a>

DOI - Digital Object Identifier

<a href="http://dx.doi.org/10.1016/j.toxlet.2025.01.003" target="_blank" >10.1016/j.toxlet.2025.01.003</a>

Jazyk výsledku

angličtina

Název v původním jazyce

Binding of ligands to the aryl hydrocarbon receptor: An overview of methods

Popis výsledku v původním jazyce

The aryl hydrocarbon receptor (AhR) is a ligand-activated transcription factor, which plays numerous and pivotal roles in human physiology and pathophysiology. Therefore, pharmacotherapeutic targeting of the AhR is a highly pertinent issue. The identification of new AhR ligands and the characterization of the interactions between the AhR ligands and AhR protein requires appropriate methodology. In spite the AhR is monomeric intracellular soluble receptor, the full-length human AhR protein has not been crystallized so far, and its isolation in a form applicable in the binding assays is highly challenging. Recent advances, including crystallization of AhR fragments, recombinant protein technologies, and cryogenic electron microscopy, allowed for exploitation of diverse experimental techniques for studying interactions between ligands and the AhR. In the current paper, we review existing AhR ligand binding assays, including their description, applicability and limitations.

Název v anglickém jazyce

Binding of ligands to the aryl hydrocarbon receptor: An overview of methods

Popis výsledku anglicky

The aryl hydrocarbon receptor (AhR) is a ligand-activated transcription factor, which plays numerous and pivotal roles in human physiology and pathophysiology. Therefore, pharmacotherapeutic targeting of the AhR is a highly pertinent issue. The identification of new AhR ligands and the characterization of the interactions between the AhR ligands and AhR protein requires appropriate methodology. In spite the AhR is monomeric intracellular soluble receptor, the full-length human AhR protein has not been crystallized so far, and its isolation in a form applicable in the binding assays is highly challenging. Recent advances, including crystallization of AhR fragments, recombinant protein technologies, and cryogenic electron microscopy, allowed for exploitation of diverse experimental techniques for studying interactions between ligands and the AhR. In the current paper, we review existing AhR ligand binding assays, including their description, applicability and limitations.

Druh

J_imp - Článek v periodiku v databázi Web of Science

CEP obor

—

OECD FORD obor

30108 - Toxicology

Projekt

<a href="/cs/project/GA23-04662S" target="_blank" >GA23-04662S: Monoterpenoidy jako nová třída negativních alosterických modulátorů aryl uhlovodíkového receptoru v terapii kolorektálního karcinomu</a><br>

Návaznosti

P - Projekt vyzkumu a vyvoje financovany z verejnych zdroju (s odkazem do CEP)<br>S - Specificky vyzkum na vysokych skolach

Rok uplatnění

2025

Kód důvěrnosti údajů

S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

Název periodika

TOXICOLOGY LETTERS

ISSN

0378-4274

e-ISSN

1879-3169

Svazek periodika

404

Číslo periodika v rámci svazku

FEB

Stát vydavatele periodika

IE - Irsko

Počet stran výsledku

10

Strana od-do

37-46

Kód UT WoS článku

001407494600001

EID výsledku v databázi Scopus

2-s2.0-85215417650