Abstract
G protein receptor kinase 2 (GRK2) has been for years mainly considered the negative regulator of the cardiac β adrenergic signaling. However GRK2 is a ubiquitous molecule and its kinase activity and scaffold properties brought to several investigations which have evidenced its involvement in pathophysiology of extra-cardiac diseases. Later discoveries, moreover, indicated that this molecule is also able to influence other pathways such as insulin signaling by an inhibitory role similar to what described years before on βAR signaling. The importance of this novel function is in particular related to the possibility that this molecule can regulate the cellular metabolism, modifying the ability of cells to utilize different substrates. This hypothesis has been recently investigated in animal model of Heart Failure, evidencing that upregulation of GRK2 leads to alterations of cardiac glucose metabolism in the early stages of the disease. However GRK2 shows increased level also in the early stages of others chronic disease such as Alzheimers Disease, indicating that these findings could be possibly applied to others cellular system and supporting the emerging idea of GRK2 as master regulator of cellular metabolism.
Keywords: Metabolism, glucose, insulin signaling, chronic disease, G protein receptor kinase 2 (GRK2), Alzheimer's Disease, Myocardial ischemia, hypertension, energy homeostasis, oxidative stress
Current Pharmaceutical Design
Title: GRK2 at the Control Shaft of Cellular Metabolism
Volume: 18 Issue: 2
Author(s): Michele Ciccarelli, Ersilia Cipolletta and Guido Iaccarino
Affiliation:
Keywords: Metabolism, glucose, insulin signaling, chronic disease, G protein receptor kinase 2 (GRK2), Alzheimer's Disease, Myocardial ischemia, hypertension, energy homeostasis, oxidative stress
Abstract: G protein receptor kinase 2 (GRK2) has been for years mainly considered the negative regulator of the cardiac β adrenergic signaling. However GRK2 is a ubiquitous molecule and its kinase activity and scaffold properties brought to several investigations which have evidenced its involvement in pathophysiology of extra-cardiac diseases. Later discoveries, moreover, indicated that this molecule is also able to influence other pathways such as insulin signaling by an inhibitory role similar to what described years before on βAR signaling. The importance of this novel function is in particular related to the possibility that this molecule can regulate the cellular metabolism, modifying the ability of cells to utilize different substrates. This hypothesis has been recently investigated in animal model of Heart Failure, evidencing that upregulation of GRK2 leads to alterations of cardiac glucose metabolism in the early stages of the disease. However GRK2 shows increased level also in the early stages of others chronic disease such as Alzheimers Disease, indicating that these findings could be possibly applied to others cellular system and supporting the emerging idea of GRK2 as master regulator of cellular metabolism.
Export Options
About this article
Cite this article as:
Ciccarelli Michele, Cipolletta Ersilia and Iaccarino Guido, GRK2 at the Control Shaft of Cellular Metabolism, Current Pharmaceutical Design 2012; 18 (2) . https://dx.doi.org/10.2174/138161212799040493
DOI https://dx.doi.org/10.2174/138161212799040493 |
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
-
Hydrogen Sulphide in Heart and Systemic Circulation
Inflammation & Allergy - Drug Targets (Discontinued) Endothelin Receptor Antagonists: A New Therapeutic Option for Improving the Outcome after Solid Organ Transplantation?
Current Vascular Pharmacology Atrial Fibrillation: Biomarkers Determining Prognosis
Current Medicinal Chemistry Immunoadsorption Therapy for Patients with Dilated Cardiomyopathy and Heart Failure
Current Cardiology Reviews Mitochondrial Dysfunction in the Pathophysiology of Bipolar Disorder: Effects of Pharmacotherapy
Mini-Reviews in Medicinal Chemistry Wide Pulse Pressure in the Elderly
Current Cardiology Reviews Fibrosis as a Therapeutic Target Post-Myocardial Infarction
Current Pharmaceutical Design Re-Wiring the Circuit: Mitochondria as a Pharmacological Target in Liver Disease
Current Medicinal Chemistry Stiff Left Atrial Syndrome; Prospects and Possibilities. Retrospective Analysis and Review of the Literature
Current Hypertension Reviews Recent Progress in Research on Ribosome Inactivating Proteins
Current Protein & Peptide Science PET Imaging and Coronary Circulatory Function: Non-Invasive Mechanistic Insights and Cardiovascular Prognosis
Current Cardiology Reviews Gene Therapy in Lung Transplantation
Current Gene Therapy Peptide Biomarkers: Exploring the Diagnostic Aspect
Current Protein & Peptide Science Signal Transduction Pathways and Transcription Factors as Therapeutic Targets in Inflammatory Disease: Towards Innovative Antirheumatic Therapy
Current Pharmaceutical Design The Association of Palmitoylethanolamide with Luteolin Decreases Neuroinflammation and Stimulates Autophagy in Parkinson's Disease Model
CNS & Neurological Disorders - Drug Targets Pharmacological Therapy of Parkinson’s Disease: Current Options and New Avenues
Recent Patents on CNS Drug Discovery (Discontinued) Methylene Blue and Vasoplegia: Who, When, and How?
Mini-Reviews in Medicinal Chemistry Troika of the Mouse Blastocyst: Lineage Segregation and Stem Cells
Current Stem Cell Research & Therapy Antihypertensive Treatment with Beta-Blockers in the Metabolic Syndrome: A Review
Current Diabetes Reviews Inotropic and Vasoactive Drugs in Pediatric ICU
Current Drug Targets