Presence of a putative steroidal allosteric site on glycoprotein hormone receptors

Rossi, Mario; Dimida, Antonio; Ferrarini, Eleonora; Silvano, Elena; Marco, Giuseppina De; Agretti, Patrizia; Aloisi, Gabriella; Simoncini, Tommaso; Bari, Lorenzo Di; Tonacchera, Massimo; Giorgi, Franco; Maggio, Roberto

doi:10.1016/j.ejphar.2009.09.029

Cited by 22 publications

(10 citation statements)

References 28 publications

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“…Some pesticides have long been banned in many countries but are still present in the environment, such as DDT, HCB and chlorpyrifos (CPF), and many of these have been examined and investigated for their thyroid-disrupting abilities (Pearce & Braverman 2009). In vitro studies on DDT exposure showed that DDT inhibits TSH release, mainly by affecting cAMP production at the post-receptor step (Santini et al 2003), and DDT can inhibit the activity of TSHR (Rossi et al 2007(Rossi et al , 2009(Rossi et al , 2018. In addition, it has been demonstrated that, in rats, a low dose of DDT increases the concentration of T3 and reduces the level of TSH (Yaglova & Yaglov 2014).…”

Section: Pesticidesmentioning

confidence: 99%

Thyroid function disruptors: from nature to chemicals

Oliveira

Chiamolera

Giannocco

et al. 2019

Journal of Molecular Endocrinology

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The modern concept of thyroid disruptors includes man-made chemicals and bioactive compounds from food that interfere with any aspect of the hypothalamus-pituitary-thyroid axis, thyroid hormone biosynthesis and secretion, blood and transmembrane transport, metabolism and local action of thyroid hormones. This review highlights relevant disruptors that effect populations through their diet: directly from food itself (fish oil and polyunsaturated fatty acids, pepper, coffee, cinnamon and resveratrol/grapes), through vegetable cultivation (pesticides) and from containers for food storage and cooking (bisphenol A, phthalates and polybrominated diphenyl ethers). Due to the vital role of thyroid hormones during every stage of life, we review effects from the gestational period through to adulthood, including evidence from in vitro studies, rodent models, human trials and epidemiological studies.

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Section: Pesticidesmentioning

confidence: 99%

Thyroid function disruptors: from nature to chemicals

Oliveira

Chiamolera

Giannocco

et al. 2019

Journal of Molecular Endocrinology

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“…1, 1, 1-trichloro-2,2-bis( p -chlorophenyl) ethane and Aroclor1254 (a complex mixture of polychlorinated biphenyls) were shown to have inverse agonist activity [62,63] but lacked specificity because of their ability to activate the cell by a post-receptor mechanism. Efforts towards a more selective molecule started in 2008 with the identification of a neutral antagonist (NIDDK-CEB-52) to the TSHR derived by chemical modification of the agonist NCG0016870 (Table 3) [64].…”

Section: Development Of Small Molecule Tsh Antagonistsmentioning

confidence: 99%

Targeting the thyroid-stimulating hormone receptor with small molecule ligands and antibodies

Davies¹,

Latif²

2015

Expert Opinion on Therapeutic Targets

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Introduction The thyroid-stimulating hormone receptor (TSHR) is the essential molecule for thyroid growth and thyroid hormone production. Since it is also a key autoantigen in Graves’ disease and is involved in thyroid cancer pathophysiology, the targeting of the TSHR offers a logical model for disease control. Areas covered We review the structure and function of the TSHR and the progress in both small molecule ligands and TSHR antibodies for their therapeutic potential. Expert opinion Stabilization of a preferential conformation for the TSHR by allosteric ligands and TSHR antibodies with selective modulation of the signaling pathways is now possible. These tools may be the next generation of therapeutics for controlling the pathophysiological consequences mediated by the effects of the TSHR in the thyroid and other extrathyroidal tissues.

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“…In experimental studies, rats exposed to DDE exposure exhibit lower free T 4 levels. One target of DDT action on thyroid metabolism may be through the inhibition of TSH-stimulated intracellular accumulation of cyclic adenosine monophosphate (cAMP) by the action of DDT on the TSH receptor ( 184 , 185 , 186 , 187 ). The highly lipophilic DDT may also interfere indirectly with the TSH receptor by altering the phosphor-lipid composition of the thyroid cell membrane, rendering the TSH receptor unable to internalise and instead be released extracellularly in vesicle forms in the presence of DDT ( 188 ).…”

Section: Pesticidesmentioning

confidence: 99%

Thyroid-disrupting chemicals and brain development: an update

Mughal

Fini

Demeneix

2018

Endocrine Connections

139

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This review covers recent findings on the main categories of thyroid hormone–disrupting chemicals and their effects on brain development. We draw mostly on epidemiological and experimental data published in the last decade. For each chemical class considered, we deal with not only the thyroid hormone–disrupting effects but also briefly mention the main mechanisms by which the same chemicals could modify estrogen and/or androgen signalling, thereby exacerbating adverse effects on endocrine-dependent developmental programmes. Further, we emphasize recent data showing how maternal thyroid hormone signalling during early pregnancy affects not only offspring IQ, but also neurodevelopmental disease risk. These recent findings add to established knowledge on the crucial importance of iodine and thyroid hormone for optimal brain development. We propose that prenatal exposure to mixtures of thyroid hormone–disrupting chemicals provides a plausible biological mechanism contributing to current increases in the incidence of neurodevelopmental disease and IQ loss.

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Presence of a putative steroidal allosteric site on glycoprotein hormone receptors

Cited by 22 publications

References 28 publications

Thyroid function disruptors: from nature to chemicals

Thyroid function disruptors: from nature to chemicals

Targeting the thyroid-stimulating hormone receptor with small molecule ligands and antibodies

Thyroid-disrupting chemicals and brain development: an update

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