Constitutively Active Thyrotropin and Thyrotropin-Releasing Hormone Receptors and Their Inverse Agonists
Open accessAbstract
Receptors for thyrotropin-releasing hormone (TRH) and thyrotropin (thyroid-stimulating hormone-TSH) are important regulators of the function of the TSH-producing cells of the anterior pituitary gland and the thyroid gland, respectively, and thereby play a central role in thyroid hormone homeostasis. Although the roles of TRH- and TSH-stimulated signaling in these endocrine glands are well understood, these receptors are expressed in other sites and their roles in these extraglandular tissues are less well known. Moreover, one of the two subtypes of TRH receptors (TRH-R2) and the single TSH receptor (TSHR) exhibit constitutive signaling activity and the roles of constitutive signaling by these receptors are poorly understood. One approach to studying constitutive signaling is to use inverse agonists. In this chapter, we will describe the experimental procedures used to measure constitutive signaling by TRH-R2 and TSHR and the effects of their specific inverse agonists.
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The hypothyroid state is mild to moderate in most patients with acquired central hypothyroidism, as the pituitary TSH reserve is rarely completely depleted.
“The hypothyroid state is mild to moderate in most patients with acquired CeH, as the pituitary TSH reserve is rarely completely depleted [40, 41].”
From 2018 European Thyroid Association (ETA) Guidelines on the Diagnosis and Management of Central Hypothyroidism (2018) · cites this paper as [40]
The Introduction describes how pituitary TSH secretion regulates thyroid hormone production, but it does not discuss the severity of acquired central hypothyroidism or whether pituitary TSH reserve is usually preserved. Searches for those clinical claims found no relevant passage in our copy; page numbers were not available. (LLM, conf=0.76)
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Особливості діагностики та лікування вторинного гіпотиреозу
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- Authors
- Neumann, S., Raaka, B. M., & Gershengorn, M. C.
- Affiliations
- National Institutes of Health (US)
- Venue
- Methods in Enzymology
- Publisher
- Elsevier
- Published
- 2010
- Volume
- 485
- Pages
- 147-160
- ISSN
- 0076-6879 (ISSN-L)
- PMC
- PMC6284803
- OpenAlex
- W342788886
- Cited by
- 19
- References
- 15
- Citations by year
- 2025: 1 · 2024: 1 · 2021: 2 · 2020: 2 · 2019: 3 · 2018: 2 · 2017: 1 · 2016: 2 · 2014: 1 · 2012: 2
- FWCI
- 1.55
- Type
- book chapter
- Language
- en
- Open access
- green
- europepmc.org
- Locations
- Methods in enzymology on CD-ROM/Methods in enzymology (publishedVersion)
- PubMed (publishedVersion)
- Europe PMC (PubMed Central) (acceptedVersion)
- PubMed Central (acceptedVersion)
- Funders
- National Institutes of Health
- National Institute of Diabetes and Digestive and Kidney Diseases (Z01DK047045)
- Topics
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Receptor Mechanisms and Signaling
- Health Sciences › Medicine › Endocrinology, Diabetes and Metabolism › Thyroid Disorders and Treatments
- Life Sciences › Neuroscience › Cellular and Molecular Neuroscience › Neuropeptides and Animal Physiology
- Keywords
- thyrotropin-releasing hormone receptor, TSH receptor, inverse agonists, thyroid-stimulating hormone, thyroid hormone homeostasis, anterior pituitary
- MeSH terms
- Animals, Cell Line, Cells, Cultured, Drug Evaluation, Preclinical, Humans, Immunoassay, Midazolam, Protein Kinase C, Receptors, Thyrotropin, Thyroid Gland, Transfection, Gene Expression, Genes, Reporter, Receptors, Thyrotropin-Releasing Hormone, Reverse Transcriptase Polymerase Chain Reaction, Drug Inverse Agonism
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