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Journal Article•DOI•

Estrogenic Activities of 517 Chemicals by Yeast Two-Hybrid Assay

Tsutomu Nishihara1, Jun-ichi Nishikawa, Tomohiko Kanayama1, Fumi Dakeyama1, Koichi Saito2, Masayoshi Imagawa, Satoshi Takatori, Yoko Kitagawa, Shinjiro Hori, Hideo Utsumi3 •
Osaka University1, Nagoya City University2, Kyushu University3
01 Aug 2000-Journal of Health Science (The Pharmaceutical Society of Japan)-Vol. 46, Iss: 4, pp 282-298
TL;DR: A simple and rapid screening method using the yeast two-hybrid system based on the ligand-dependent interaction of nuclear hormone receptors with coactivators to test the estrogenic activity of chemicals.
Abstract: One of the urgent tasks in understanding endocrine disruptors (EDs) is to compile a list of suspected substances among the huge number of chemicals by using the screening test method. We developed a simple and rapid screening method using the yeast two-hybrid system based on the ligand-dependent interaction of nuclear hormone receptors with coactivators. To date, we have tested the estrogenic activity of more than 500 chemicals including natural substances, medicines, pesticides, and industrial chemicals. 64 compounds were evaluated as positive, and most of these demonstrated a common structure; phenol with a hydrophobic moiety at the para-position without bulky groups at the ortho-position. These results are expected to facilitate further risk assessment of chemicals.

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Citations
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Journal Article•DOI•
Effects of 2,4-dichlorophenol exposure on zebrafish: Implications for the sex hormone synthesis

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Yan Hu1, Dong Li1, Xuan Ma1, Rongjian Liu1, Yongmei Qi1, Cong Yuan1, Dejun Huang1 •
Lanzhou University1
16 May 2021-Aquatic Toxicology
TL;DR: In this article, the effect of 2,4-Dichlorophenol (2,4DCP) exposure on the synthesis of sex hormones in zebrafish was investigated.

10 citations

Dissertation•
Molecular quantum similarity in QSAR: applications in computer-aided molecular design

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Ana Gallegos Saliner
29 Jun 2004
TL;DR: The present tesi esta centrada en lus de la Teoria de Semblanca Quantica per a calcular descriptors moleculars as discussed by the authors, where descriptors s'utilitzen com a parametres estructurals per a derivar correlacions entre l'estructura i the funcio o activitat experimental per a conjunt de compostos.
Abstract: La present tesi esta centrada en l'us de la Teoria de Semblanca Quantica per a calcular descriptors moleculars. Aquests descriptors s'utilitzen com a parametres estructurals per a derivar correlacions entre l'estructura i la funcio o activitat experimental per a un conjunt de compostos. Els estudis de Relacions Quantitatives Estructura-Activitat son d'especial interes per al disseny racional de molecules assistit per ordinador i, en particular, per al disseny de farmacs. Aquesta memoria consta de quatre parts diferenciades. En els dos primers blocs es revisen els fonaments de la teoria de semblanca quantica, aixi com l'aproximacio topologica basada en la teoria de grafs. Ambdues teories es fan servir per a calcular els descriptors moleculars. En el segon bloc, s'ha de remarcar la programacio i implementacio de programari per a calcular els anomenats indexs topologics de semblanca quantica. La tercera seccio detalla les bases de les Relacions Quantitatives Estructura-Activitat i, finalment, el darrer apartat recull els resultats d'aplicacio obtinguts per a diferents sistemes biologics.

10 citations

Cites background or methods from "Estrogenic Activities of 517 Chemic..."

  • ...The first postulate of quantum mechanics [111-113] states that every state of a quantum object, i....

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  • ...They may encode either general features of the entire molecule or local features of a specific site [111-112]....

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  • ...42 3.5 Fitted Density Function ......................................................................................... 42 3.5.1 Atomic Shell Approximation (ASA) ................................................................ 44 3.5.2 Promolecular Atomic Shell Approximation (PASA)........................................ 46 3.5.3 ASA adjustment method ................................................................................... 49 4 Molecular Quantum similarity Measures (MQSM) ....................................................... 52 4.1 General Definition of MQSM ............................................................................... 52 4.2 Types of Molecular Quantum Similarity Measures .................................................

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  • ...On one hand, the Atomic Shell Approximation (ASA) [112-117], developed by Constans [120] and optimised by Amat [121-122], computes approximated molecular electronic density functions....

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  • ...Conventional Molecular Quantum Similarity Measures (MQSM) were computed by employing the preexisting software [64-65,89- 90], implemented by Robert [117] and Gironés [118], by using the Atomic Shell Approximation (ASA) [119-123] for the electronic densities, and the maximum similarity alignment rule [124] or the Topo-Geometrical Superposition Algorithm (TGSA) [125] for the molecular superposition....

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Other•DOI•
Alkylphenols, other endocrine-active chemicals, and fish responses in three streams in Minnesota - Study design and data, February-September 2007

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Kathy E. Lee, Heiko L. Schoenfuss, Nathan D. Jahns, Greg K. Brown, Larry B. Barber 
01 Jan 2008
TL;DR: In this paper, the authors propose a solution to solve the problem of the problem: this paper...,.. ].. ).. )... ;.
Abstract: ..........................................................................................................................................................

10 citations

Journal Article•DOI•
A critical review finds styrene lacks direct endocrine disruptor activity.

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Heinz-Peter Gelbke, Marcy I. Banton1, Edgar Leibold, Mark Pemberton, Susan L. Samson2 •
LyondellBasell1, Baylor College of Medicine2
19 Aug 2015-Critical Reviews in Toxicology
TL;DR: Unspecific acute workplace-related stress is proposed as an alternative mode of action for elevated PRL levels in workers because a neuroendocrine disruption of PRL regulation cannot be deduced from a large experimental database.
Abstract: The European Commission lists styrene (S) as an endocrine disruptor based primarily on reports of increased prolactin (PRL) levels in S-exposed workers. The US Environmental Protection Agency included S in its list of chemicals to be tested for endocrine activity. Therefore, the database of S for potential endocrine activity is assessed. In vitro and in vivo screening studies, as well as non-guideline and guideline investigations in experimental animals indicate that S is not associated with (anti)estrogenic, (anti)androgenic, or thyroid-modulating activity or with an endocrine activity that may be relevant for the environment. Studies in exposed workers have suggested elevated PRL levels that have been further examined in a series of human and animal investigations. While there is only one definitively known physiological function of PRL, namely stimulation of milk production, many normal stress situations may lead to elevations without any chemical exposure. Animal studies on various aspects of dopamine (DA), the PRL-regulating neurotransmitter, in the central nervous system did not give mechanistic explanations on how S may affect PRL levels. Overall, a neuroendocrine disruption of PRL regulation cannot be deduced from a large experimental database. The effects in workers could not consistently be reproduced in experimental animals and the findings in humans represented acute reversible effects clearly below clinical and pathological levels. Therefore, unspecific acute workplace-related stress is proposed as an alternative mode of action for elevated PRL levels in workers.

9 citations

Cites methods from "Estrogenic Activities of 517 Chemic..."

  • ...Nishihara et al. (2000) developed a rapid screening assay, the yeast two-hybrid assay, for estrogenic activity based on the binding of the test chemical to the hormone receptor that then interacts with a coactivator to activate transcription of a reporter gene, with the hormonal activity measured…...

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Journal Article•DOI•
Evaluation on estrogenicity and oxidative hepatotoxicity of fossil fuel industrial wastewater before and after the powdered activated carbon treatment

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Fu-An Chen, Meei-Fang Shue, Ting-Chien Chen
01 Jun 2004-Chemosphere
TL;DR: It is concluded that the industrial wastewater treatment plant using the PACT system in the Da-Hse Industrial District is suitable for removing estrogenic substances and oxidative hepatotoxic substances discharged from these industrial manufacturers.

9 citations

References
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Book•
Our Stolen Future

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Theo Colborn, Dianne Dumanoski, John Peterson Myers
01 Jan 1996
TL;DR: The cause of disruptions in animal breeding cycles, accompanied by increases in birth defects, sexual abnormalities and reproductive failure, is traced to the pervasive presence in the environment of chemicals that mimic hormones and trick the reproductive system.
Abstract: For years, scientists have noticed disruptions in animal breeding cycles, accompanied by increases in birth defects, sexual abnormalities and reproductive failure. Humans are not immune either, with sperm counts dropping by as much as 50% in recent decades and with women seeing a rise in hormone-related cancers, endometriosis and other disorders. This book traces the cause of these aberrations and diseases to the pervasive presence in the environment of chemicals that mimic hormones and trick the reproductive system. The conclusions are as obvious as they are inescapable - unless we make vital changes in the way we manufacture and employ the artefacts of our "good life", there will be no life at all.

917 citations

Related Papers (5)
The Estrogen Receptor Relative Binding Affinities of 188 Natural and Xenochemicals: Structural Diversity of Ligands

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01 Mar 2000-Toxicological Sciences
R. Blair, Hong Fang, William S. Branham, Bruce S. Hass, Stacey L. Dial, Carrie L. Moland, Weida Tong, Leming Shi, Roger Perkins, Daniel M. Sheehan 
The E-SCREEN assay as a tool to identify estrogens: an update on estrogenic environmental pollutants.

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01 Oct 1995-Environmental Health Perspectives
Ana M. Soto, Carlos Sonnenschein, Kerrie L. Chung, Mariana F. Fernández, Nicolás Olea, Fátima Olea Serrano 
Estrogenic activity of surfactants and some of their degradation products assessed using a recombinant yeast screen

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01 Mar 1996-Environmental Toxicology and Chemistry
Edwin J. Routledge, John P. Sumpter
Developmental effects of endocrine-disrupting chemicals in wildlife and humans.

[...]

01 Oct 1993-Environmental Health Perspectives
Theo Colborn, F S vom Saal, Ana M. Soto
A variety of environmentally persistent chemicals, including some phthalate plasticizers, are weakly estrogenic.

[...]

01 Jun 1995-Environmental Health Perspectives
Susan Jobling, Tracey Reynolds, Roger White, Malcolm G. Parker, John P. Sumpter