Abstract
Lessons from viral hijacks of cells and cancer biology suggest that the activation of G protein-coupled receptors (GPCRs) often results in the modulation of various transcription factors and cofactors. Since drugs acting on GPCRs represent a significant portion of therapeutic agents currently in use, it is important to understand the actions of GPCRs on gene expression. GPCRs and their associated heterotrimeric G proteins are known to regulate gene transcription through complex signaling networks. The G protein-mediated signaling cascades have been extensively studied and accumulating evidence indicates that the four subfamilies of G proteins may utilize both common and unique pathways for transcriptional regulation. This review aims to provide a contemporary account of our understanding on the regulation of transcription factors by GPCRs, with a special emphasis on specific regulations of transcription factors such as STAT3 and NF-κB by individual G protein subfamilies. Functional impacts of the signal integration between different pathways and the contributions by other GPCR-interacting molecules will also be briefly discussed.
Keywords: GPCR, heterotrimeric G proteins, transcriptional regulation, signal integration
Current Molecular Pharmacology
Title: Regulation of Transcription Factors by Heterotrimeric G Proteins
Volume: 2
Author(s): M. K.C. Ho, Y. Su, W. W.S. Yeung and Y. H. Wong
Affiliation:
Keywords: GPCR, heterotrimeric G proteins, transcriptional regulation, signal integration
Abstract: Lessons from viral hijacks of cells and cancer biology suggest that the activation of G protein-coupled receptors (GPCRs) often results in the modulation of various transcription factors and cofactors. Since drugs acting on GPCRs represent a significant portion of therapeutic agents currently in use, it is important to understand the actions of GPCRs on gene expression. GPCRs and their associated heterotrimeric G proteins are known to regulate gene transcription through complex signaling networks. The G protein-mediated signaling cascades have been extensively studied and accumulating evidence indicates that the four subfamilies of G proteins may utilize both common and unique pathways for transcriptional regulation. This review aims to provide a contemporary account of our understanding on the regulation of transcription factors by GPCRs, with a special emphasis on specific regulations of transcription factors such as STAT3 and NF-κB by individual G protein subfamilies. Functional impacts of the signal integration between different pathways and the contributions by other GPCR-interacting molecules will also be briefly discussed.
Export Options
About this article
Cite this article as:
Ho K.C. M., Su Y., Yeung W.S. W. and Wong H. Y., Regulation of Transcription Factors by Heterotrimeric G Proteins, Current Molecular Pharmacology 2009; 2 (1) . https://dx.doi.org/10.2174/1874467210902010019
DOI https://dx.doi.org/10.2174/1874467210902010019 |
Print ISSN 1874-4672 |
Publisher Name Bentham Science Publisher |
Online ISSN 1874-4702 |
Call for Papers in Thematic Issues
Common mechanisms underpinning neurodevelopmental disorders and psychiatric diseases
A growing number of large-scale epidemiologic studies has strongly suggested that common mechanisms may be shared by aberrant brain development and psychiatric disorders. There is now an appreciation of synergic roles of genetic variants and environmental stress which profoundly affect the genome integrity and reshape brain development. This can lead ...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
-
Selective Inhibitors of Histone Deacetylase 10 (HDAC-10)
Current Medicinal Chemistry Fatty Acid Synthase: A Target for the Reversal of Liver Steatosis
Current Enzyme Inhibition Preparation and in-vitro Transfection Efficiency Evaluation of Modified Cationic Liposome-polyethyleneimine-plasmid Nanocomplexes as a Novel Gene Carrier
Current Drug Delivery Transcriptional Regulation of the p53 Tumor Suppressor Gene: A Potential Target for Cancer Therapeutics?
Recent Patents on DNA & Gene Sequences Folate Targeted Solid Lipid Nanoparticles of Simvastatin for Enhanced Cytotoxic Effects of Doxorubicin in Chronic Myeloid Leukemia
Current Nanoscience Overview of PCTK3/CDK18: A Cyclin-Dependent Kinase Involved in Specific Functions in Post-Mitotic Cells
Current Medicinal Chemistry Berberine Nanoencapsulation Attenuates Hallmarks of Scoplomine Induced Alzheimer's-Like Disease in Rats
Current Reviews in Clinical and Experimental Pharmacology Prostaglandin J2 Family and the Cardiovascular System
Current Vascular Pharmacology Role of miRNAs in Cancer Diagnostics and Therapy: A Recent Update
Current Pharmaceutical Design Proteasome Inhibitors Therapeutic Strategies for Cancer
Recent Patents on Anti-Cancer Drug Discovery Calcium Channel Subtypes and Exocytosis in Chromaffin Cells at Early Life
Current Molecular Pharmacology Function of miRNA in Controlling Drug Resistance of Human Cancers
Current Drug Targets A Cationic Nanomicellar Complex of the Quaternary Amphiphilic Amine RC16+ with Fenretinide as a New Multitasking System for Antitumor Therapy
Current Drug Delivery Signaling Mechanisms Underlying Aβ Toxicity: Potential Therapeutic Targets for Alzheimers Disease
CNS & Neurological Disorders - Drug Targets A Fluorescent Alkyllysophospholipid Analog Exhibits Selective Cytotoxicity Against the Hormone-Insensitive Prostate Cancer Cell Line PC3
Anti-Cancer Agents in Medicinal Chemistry The Role of the Osteoimmune Axis in the Inflammation of the Inner Auditory Ear and with Regard to the Putative Anticarcinogenetic Principle: Part 2
Inflammation & Allergy - Drug Targets (Discontinued) Targeting Mitochondria in Fighting Cancer
Current Pharmaceutical Design Current Understanding of HSP90 as a Novel Therapeutic Target: An Emerging Approach for the Treatment of Cancer
Current Pharmaceutical Design Immunology Behind Tumors: A Mini Review
Current Cancer Therapy Reviews Cyclin-Dependent Kinase as a Novel Therapeutic Target: An Endless Story
Current Chemical Biology