Abstract
Thyroid hormones regulate fundamental genes involved in the metabolism, development and homeostasis of vertebrates. The endogenous hormones, L-3, 5, 3-triiodo-L-thyronine (T3) and L-3, 5, 3, 5-tetraiodo-L-thyronine (T4), are of limited use in pharmacological intervention, mainly due to cardiovascular liabilities. There exist two subtypes of thyroid hormone receptors (TR), α and β, unequally distributed in the body. As TRα is most abundant in the heart and most effects of thyroid hormones on the heart are mediated through TRα, a reasonable strategy is the development of TR agonists that either are tissue selective or that interact selectively with TRβ. The prospects for the treatment of metabolic diseases with such ligands are considerable and this review describes the massive efforts of the academic and industrial communities during the last decade. It is, however, the authors view that the development of selective ligands only is in its infancy, an opinion highlighted by the limited chemical structural variation of TR ligands as well as the present lack of TR ligands for the treatment of metabolic diseases in clinical phases.
Keywords: thyroid hormones, thyroid hormone receptors, dyslipidemia, diabetes, hypothyroidism, obesity, atherosclerosis, metabolic diseases
Current Pharmaceutical Design
Title: Thyroid Hormone Ligands and Metabolic Diseases
Volume: 10 Issue: 28
Author(s): Johan Malm
Affiliation:
Keywords: thyroid hormones, thyroid hormone receptors, dyslipidemia, diabetes, hypothyroidism, obesity, atherosclerosis, metabolic diseases
Abstract: Thyroid hormones regulate fundamental genes involved in the metabolism, development and homeostasis of vertebrates. The endogenous hormones, L-3, 5, 3-triiodo-L-thyronine (T3) and L-3, 5, 3, 5-tetraiodo-L-thyronine (T4), are of limited use in pharmacological intervention, mainly due to cardiovascular liabilities. There exist two subtypes of thyroid hormone receptors (TR), α and β, unequally distributed in the body. As TRα is most abundant in the heart and most effects of thyroid hormones on the heart are mediated through TRα, a reasonable strategy is the development of TR agonists that either are tissue selective or that interact selectively with TRβ. The prospects for the treatment of metabolic diseases with such ligands are considerable and this review describes the massive efforts of the academic and industrial communities during the last decade. It is, however, the authors view that the development of selective ligands only is in its infancy, an opinion highlighted by the limited chemical structural variation of TR ligands as well as the present lack of TR ligands for the treatment of metabolic diseases in clinical phases.
Export Options
About this article
Cite this article as:
Malm Johan, Thyroid Hormone Ligands and Metabolic Diseases, Current Pharmaceutical Design 2004; 10 (28) . https://dx.doi.org/10.2174/1381612043382873
DOI https://dx.doi.org/10.2174/1381612043382873 |
Print ISSN 1381-6128 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4286 |
Call for Papers in Thematic Issues
"Tuberculosis Prevention, Diagnosis and Drug Discovery"
The Nobel Prize-winning discoveries of Mycobacterium tuberculosis and streptomycin have enabled an appropriate diagnosis and an effective treatment of tuberculosis (TB). Since then, many newer diagnosis methods and drugs have been saving millions of lives. Despite advances in the past, TB is still a leading cause of infectious disease mortality ...read more
Current Pharmaceutical challenges in the treatment and diagnosis of neurological dysfunctions
Neurological dysfunctions (MND, ALS, MS, PD, AD, HD, ALS, Autism, OCD etc..) present significant challenges in both diagnosis and treatment, often necessitating innovative approaches and therapeutic interventions. This thematic issue aims to explore the current pharmaceutical landscape surrounding neurological disorders, shedding light on the challenges faced by researchers, clinicians, and ...read more
Emerging and re-emerging diseases
Faced with a possible endemic situation of COVID-19, the world has experienced two important phenomena, the emergence of new infectious diseases and/or the resurgence of previously eradicated infectious diseases. Furthermore, the geographic distribution of such diseases has also undergone changes. This context, in turn, may have a strong relationship with ...read more
Melanoma and Non-Melanoma Skin Cancer Treatment: Standard of Care and Recent Advances
In this thematic issue, we aim to provide a standard of care of the diagnosis and treatment of melanoma and non-melanoma skin cancer. The editor will invite authors from different countries who will write review articles of melanoma and non-melanoma skin cancers. The Diagnosis, Staging, Surgical Treatment, Non-Surgical Treatment all ...read more
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
- Announcements
Related Articles
-
Pharmacotherapy of Aortic Stenosis-Success or Failure?
Current Pharmaceutical Biotechnology Drug Delivery to CNS: Challenges and Opportunities with Emphasis on Biomaterials Based Drug Delivery Strategies
Current Pharmaceutical Design A Comprehensive Literature Review of COPD-Related Fatigue
Current Respiratory Medicine Reviews Towards a Better Understanding of Cardiac and Vascular Disease in Patients with Chronic Kidney Disease
Current Cardiology Reviews Pharmacogenomics: Integration into Drug Discovery and Development
Current Topics in Medicinal Chemistry 58-Year Old Men with Non-Stenotic Carotid Artery Plaques and the Relationship with Cardiovascular Risk Factors and Future Cardiovascular Events
Vascular Disease Prevention (Discontinued) The Critical Roles of HSC70 in Physiological and Pathological Processes
Current Pharmaceutical Design Editorial: Vascular Calcification, Cardiovascular Risk and microRNAs
Current Vascular Pharmacology Emerging Therapies for Type 2 Diabetes
Current Drug Therapy Chinese Herbal Medicine for Hyperlipidaemia: A Review Based on Data Mining from 1990 to 2016
Current Vascular Pharmacology Impact of Chronic Kidney Disease on Risk for Vascular Events
Current Vascular Pharmacology Angiotensin-Converting Enzyme 2 Roles in the Pathogenesis of COVID-19
Current Hypertension Reviews Physiological Functions of Heat Shock Proteins
Current Protein & Peptide Science The Role of Orexin System in Antipsychotics Induced Weight Gain
Current Psychiatry Reviews Supramolecular Chiro-Biomedical Aspect of β-Blockers in Drug Development
Current Drug Targets The Application of Minerals in Managing Alcohol Hangover: A Preliminary Review
Current Drug Abuse Reviews Editorial: The Interplay between TSH and Lipids. What Should Clinicians Know?
Current Vascular Pharmacology Editorial: Time for Earlier and More Intensive Preventive Therapy
Current Vascular Pharmacology Effects of Statins on Blood Pressure: A Review of the Experimental and Clinical Evidence.
Current Vascular Pharmacology Vascular Oxidative Stress: A Key Factor in the Development of Hypertension Associated with Ethanol Consumption
Current Hypertension Reviews