Identification and evaluation of constitutively active thyroid stimulating hormone receptor mutations
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Joaquin Lado-Abeal1, Leah R Quisenberry, Isabel Castro-Piedras
1Department of Internal Medicine, Tech University Health Sciences Center-SOM, Lubbock, Texas, USA.
Abstract:
Thyroid stimulating hormone receptor (TSHR) is a guanine nucleotide-binding protein-coupled seven-transmembrane-domain receptor that controls the differentiation, growth, and function of the thyroid gland through stimulation of adenylyl cyclase and phospholipase C pathways. Thyroid stimulating hormone (TSH) is the main TSHR ligand, and unliganded receptor remains silent due to the interaction of its large extracellular domain with the extracellular loops of the serpentine. The TSHR gene is highly mutagenic and constitutively active mutations have been extensively described. Naturally occurring TSHR-activating mutations can affect any part of the receptor, but most activating mutations affect the serpentine region, and the majority of these are located in the third intracellular loop or transmembrane domain six. We describe several simple and relatively cheap methods used in our laboratory to study constitutive TSHR mutations that include (1) screening of TSHR gene mutations in paraffin-embedded thyroid tissue samples, (2) measurement of TSHR constitutive activity in vitro, (3) measurement of TSHR expression at cell surface by flow cytometry analysis, (4) TSH binding to TSHR, and (5) TSHR phosphorylation analysis.
Insights
Constitutive mutations in the thyroid stimulating hormone receptor (TSHR) gene can cause thyroid dysfunction. This study details cost-effective methods for analyzing these TSHR mutations and their functional impacts.
Area of Science:
- Endocrinology
- Molecular Biology
- Genetics
Background:
- The thyroid stimulating hormone receptor (TSHR) is a G protein-coupled receptor regulating thyroid gland function.
- TSHR activation is typically mediated by thyroid stimulating hormone (TSH); however, mutations can lead to constitutive activity.
- Constitutively active TSHR mutations are frequently found in the serpentine region, particularly the third intracellular loop or transmembrane domain six.
Purpose of the Study:
- To describe simple and cost-effective laboratory methods for studying TSHR constitutive mutations.
- To investigate the molecular mechanisms and functional consequences of TSHR activating mutations.
Main Methods:
- Screening TSHR gene mutations in paraffin-embedded thyroid tissue.
- In vitro measurement of TSHR constitutive activity.
- Flow cytometry analysis for cell surface TSHR expression.
- Analysis of TSH binding to TSHR.
- TSHR phosphorylation assays.
Main Results:
- The study presents a suite of accessible methods for TSHR mutation analysis.
- These methods allow for the comprehensive study of TSHR constitutive activity, expression, ligand binding, and phosphorylation.
Conclusions:
- The described methods provide a practical approach to investigating the genetic and functional aspects of TSHR mutations.
- These techniques facilitate the study of thyroid diseases associated with constitutively active TSHR.
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