Related Experiment Video

Updated: Apr 17, 2026

Author Spotlight: Investigating Physiological Functions of Vitamin A Transporters Using HPLC-Based Vitamin A Profiling
05:03

Author Spotlight: Investigating Physiological Functions of Vitamin A Transporters Using HPLC-Based Vitamin A Profiling

Published on: December 27, 2024

1.9K

Triorganotin compounds--ligands for "rexinoid" inducible transcription factors: biological effects

J Brtko1, Z Dvorak2

  • 1Laboratory of Molecular Endocrinology, Institute of Experimental Endocrinology, Slovak Academy of Sciences, Vlarska 3, 83306 Bratislava, Slovak Republic.

Toxicology Letters
|February 17, 2015
PubMed

Insights

Trialkyltin and triaryltin compounds activate nuclear retinoid X receptors (RXR), influencing gene transcription. These organotins exhibit obesogenic, developmental, and toxic effects, impacting reproduction and endocrine systems.

Area of Science:

  • Organometallic chemistry
  • Endocrinology
  • Toxicology

Background:

  • Organometallic compounds, specifically trialkyltin and triaryltin, are identified as nuclear retinoid X receptors (RXR) agonists.
  • Retinoid X receptors (RXR) play a crucial role in transcriptional regulation, primarily functioning as heterodimers with various nuclear receptors.
  • These heterodimers are involved in a broad molecular mechanism governing transcriptional responses in target genes.

Purpose of the Study:

  • To review the mechanisms by which trialkyltin and triaryltin compounds act as RXR agonists.
  • To explore the diverse toxicological and endocrine-disrupting effects of organotin compounds.
  • To summarize the impact of organotins on hepatic P450s and aromatase activity.

Main Methods:

  • Literature review of studies on trialkyltin and triaryltin compounds.
  • Analysis of their binding to RXR ligand-binding domains.
  • Examination of their effects on gene transcription and various biological pathways.

Main Results:

  • Trialkyltin and triaryltin compounds bind to RXR, activating transcription.
  • Tributyltin causes developmental abnormalities in aquatic organisms and promotes adipocyte differentiation in mammals.
  • Organotins exhibit immunotoxicity, neurotoxicity, and adverse effects on reproduction and development.

Conclusions:

  • Organotin compounds are potent RXR agonists with significant endocrine-disrupting capabilities.
  • Their environmental presence poses risks due to obesogenic, developmental, and reproductive toxicity.
  • Further research is warranted to understand the full spectrum of organotin toxicity and their interactions with metabolic enzymes.
Keywords:
Antiproliferative effectsCytochrom P-450Environmental obesogenLigand inducible transcription factorMetabolismNuclear receptorOrganotin compoundsRetinoid X receptorToxicity

More Related Videos

Author Spotlight: Unraveling Vitamin A Transport Mechanisms — Linking Liver Receptors to Vision Health Through RBPR2 and RBP4 Interactions08:18

Author Spotlight: Unraveling Vitamin A Transport Mechanisms — Linking Liver Receptors to Vision Health Through RBPR2 and RBP4 Interactions

Published on: October 4, 2024

1.6K
An In Vitro Enzymatic Assay to Measure Transcription Inhibition by GalliumIII and H3 5,10,15-trispentafluorophenylcorroles09:00

An In Vitro Enzymatic Assay to Measure Transcription Inhibition by GalliumIII and H3 5,10,15-trispentafluorophenylcorroles

Published on: March 18, 2015

12.2K

Related Concept Videos

Transducer Mechanism: Nuclear Receptors01:31

Transducer Mechanism: Nuclear Receptors

Nuclear receptors, or NRs, are unique transcription factors that regulate gene transcription and affect the cellular pathways involved in reproduction, development, or metabolism. Their ability to be stimulated by small lipophilic ligands and control vital cellular processes makes them ideal drug targets. Nearly 10-15% of currently prescribed drugs target these receptors.
About 48 different soluble family members of nuclear receptors are identified that can be divided into two main classes:
6.5K
Eukaryotic Transcription Inhibitors01:52

Eukaryotic Transcription Inhibitors

Certain biochemical processes, such as embryonic development and cell growth regulation, depend on the repression of specific genes. DNA binding proteins known as eukaryotic transcription inhibitors regulate the repression of gene expression in eukaryotes. The presence of these inhibitors at the required location and time in the cell is triggered by the presence of hormones and additional signals from other cells.
Eukaryotic transcription inhibitors usually contain two distinct domains, a...
11.7K
Signal Transduction: Overview01:26

Signal Transduction: Overview

Cells respond to many types of information, often through receptor proteins positioned on the membrane. They respond to chemical signals, such as hormones, neurotransmitters, and other signaling molecules, initiating a series of molecular reactions to produce an appropriate response. This is called signal transduction. Cells also coordinate different responses elicited by the same signaling molecule via mediators, allowing molecular cross-talk.
Typically, signal transduction involves three...
13.1K
Receptor Tyrosine Kinases01:26

Receptor Tyrosine Kinases

Receptor tyrosine kinases or RTKs are membrane-bound receptors that phosphorylate specific tyrosine on protein substrates. RTKs regulate cellular growth, differentiation, survival, and migration. They contain an extracellular ligand binding domain, a transmembrane domain, and a cytosolic tail with intrinsic kinase activity. Several extracellular signaling molecules activate RTKs in one or more ways and relay the signal downstream. Ligands such as platelet-derived growth factor (PDGF) or...
21.2K
TGF - β Signaling Pathway01:16

TGF - β Signaling Pathway

The TGF-β signaling pathway regulates cell growth, differentiation, adhesion, motility, and development. TGF-β ligands that induce TGF-β signaling are synthesized in their latent form. Several proteases or cell surface receptors such as integrins act upon the latent form, releasing the active ligand. There are three types of mammalian TGF-βs: (TGF-β1, TGF-β2, and TGF-β3) that bind as homodimers or heterodimers to TGF-β receptors. The TGF-β receptors...
11.1K
Co-activators and Co-repressors02:04

Co-activators and Co-repressors

Gene transcription is regulated by the synergistic action of several proteins that form a complex at a gene regulatory site. This is observed in eukaryotes, where the regulation of gene expression is a complex process. Regulatory proteins in eukaryotes can broadly be classified into two types – regulators that bind directly to specific DNA sequences and co-regulators that associate with regulatory proteins but cannot directly bind to the DNA. These co-regulators are further divided into...
9.1K