Related Experiment Video
Updated: Jun 13, 2025
00:07
In Vivo Inhibition of MicroRNA to Decrease Tumor Growth in Mice
Published on: August 23, 2019
7.2K
Targeting Thyroid-Stimulating Hormone Receptor: A Perspective on Small-Molecule Modulators and Their Therapeutic
Yu Zhang1, Ye Tan1, Zian Zhang2,3
1Zhongshan Institute for Drug Discovery, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Zhongshan 528400, China.
Journal of Medicinal Chemistry
|September 13, 2024
Summary
Small molecules targeting the Thyroid-Stimulating Hormone Receptor (TSHR) show promise for treating various diseases. This review highlights recent advances in developing TSHR modulators for drug discovery.
Area of Science:
- Endocrinology
- Pharmacology
- Molecular Biology
Background:
- The Thyroid-Stimulating Hormone Receptor (TSHR) is crucial for thyroid function and implicated in numerous diseases.
- Aberrant TSHR activity is linked to conditions like Graves' disease, hypothyroidism, and cancer.
Purpose of the Study:
- To review the structure, function, and biological roles of TSHR.
- To summarize recent progress in developing small-molecule TSHR modulators for therapeutic applications.
Main Methods:
- Literature review of TSHR structure, function, and disease associations.
- Analysis of recent studies on small-molecule TSHR modulators, including agonists, antagonists, and inverse agonists.
Main Results:
- TSHR is a key target for treating thyroid-related disorders and other diseases.
- Advances in small-molecule TSHR modulators offer potential therapeutic strategies.
- Detailed insights into chemotypes, mechanisms of action, SAR, and preclinical data are presented.
Conclusions:
- Small-molecule TSHR modulators represent a promising avenue for drug discovery.
- Further research into TSHR modulation holds potential for novel therapeutic interventions.
- Addressing challenges and exploring new opportunities in TSHR research is crucial for future drug development.
Related Concept Videos
01:20Synthesis and Regulation of Thyroid Hormones
4.3K
Low blood levels of the thyroid hormones — triiodothyronine (T3) and thyroxine (T4) — signal the hypothalamus to release the thyrotropin-releasing hormone (TRH). TRH then reaches the pituitary gland and stimulates the release of thyroid-stimulating hormone(TSH) into the bloodstream.
Upon reaching the thyroid gland, TSH stimulates the follicular cells' active uptake of iodide ions from the blood. The ions diffuse to the apical surface of the cells and are oxidized to iodine. The...
Upon reaching the thyroid gland, TSH stimulates the follicular cells' active uptake of iodide ions from the blood. The ions diffuse to the apical surface of the cells and are oxidized to iodine. The...
4.3K
01:26Targets for Drug Action: Overview
6.1K
Drugs target macromolecules to modify ongoing cellular processes. Primary drug targets include receptors, ion channels, transporters, and enzymes.
Receptors are either membrane-spanning or intracellular proteins, which upon binding a ligand, get activated and transmit the signal downstream to elicit a response. Drugs bind receptors, either mimicking the action of endogenous ligands or blocking the receptor activity to bring about a modified response. Nearly 35% of approved drugs target the G...
Receptors are either membrane-spanning or intracellular proteins, which upon binding a ligand, get activated and transmit the signal downstream to elicit a response. Drugs bind receptors, either mimicking the action of endogenous ligands or blocking the receptor activity to bring about a modified response. Nearly 35% of approved drugs target the G...
6.1K
01:27Transducer Mechanism: Enzyme-Linked Receptors
2.4K
Enzyme-linked receptors are cell-surface receptors acting as an enzyme or associating with an enzyme intracellularly. They make excellent drug targets. Drugs can bind to the extracellular ligand-binding domain or directly affect their enzymatic domain and alter their activity.
Major types that are helpful drug targets include:
Major types that are helpful drug targets include:
2.4K
01:31Transducer Mechanism: Nuclear Receptors
1.3K
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:
About 48 different soluble family members of nuclear receptors are identified that can be divided into two main classes:
1.3K
02:57Targeted Cancer Therapies
7.5K
The targeted cancer therapies, also known as “molecular targeted therapies,” take advantage of the molecular and genetic differences between the cancer cells and the normal cells. It needs a thorough understanding of the cancer cells to develop drugs that can target specific molecular aspects that drive the growth, progression, and spread of cancer cells without affecting the growth and survival of other normal cells in the body.
There are several types of targeted therapies against...
There are several types of targeted therapies against...
7.5K
01:18Functions of Thyroid Hormones
2.6K
The thyroid hormone (TH) plays a pivotal role in the intricate orchestration of physiological processes, exerting profound effects on development, metabolism, and homeostasis throughout different life stages.
TH is indispensable for the normal development and maturation of the skeletal, muscular, and nervous systems during fetal and childhood growth. It facilitates bone mineral turnover and regulates protein synthesis in developing tissues, contributing significantly to overall growth and...
TH is indispensable for the normal development and maturation of the skeletal, muscular, and nervous systems during fetal and childhood growth. It facilitates bone mineral turnover and regulates protein synthesis in developing tissues, contributing significantly to overall growth and...
2.6K