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 |
- 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
-
Safety of Nanoparticles in Medicine
Current Drug Targets Polymeric Carriers for Gene Delivery: Chitosan and Poly(amidoamine) Dendrimers
Current Pharmaceutical Design Signal Transduction Therapy Targeting Apoptosis Pathways in Cancers
Current Signal Transduction Therapy A Novel Information Theoretic Approach to Gene Selection for Cancer Classification Using Microarray Data
Current Bioinformatics Pharmacophores for Ligand Recognition and Activation / Inactivation of the Cannabinoid Receptors
Current Pharmaceutical Design MIIP, a Cytoskeleton Regulator that Blocks Cell Migration and Invasion, Delays Mitosis, and Suppresses Tumorogenesis
Current Protein & Peptide Science Plausible Improvements for Selective Targeting of Dopamine Receptors in Therapy of Parkinson’s Disease
Mini-Reviews in Medicinal Chemistry Ras-Induced Resistance to Lapatinib is Overcome by MEK Inhibition
Current Cancer Drug Targets Novobiocin and Additional Inhibitors of the Hsp90 C-Terminal Nucleotide- binding Pocket
Current Medicinal Chemistry Structure, Roles and Inhibitors of a Mitotic Protein Kinase Haspin
Current Medicinal Chemistry Role of Glucocorticoids in Breast Cancer
Current Pharmaceutical Design Pathophysiological Roles of Transglutaminase - Catalyzed Reactions in the Pathogenesis of Human Diseases
Inflammation & Allergy - Drug Targets (Discontinued) Histone and Non-Histone Targets of Dietary Deacetylase Inhibitors
Current Topics in Medicinal Chemistry Cell Surface Nucleolin as a Target for Anti-Cancer Therapies
Recent Patents on Anti-Cancer Drug Discovery The Immunoregulatory Protein Human B7H3 is a Tumor-Associated Antigen that Regulates Tumor Cell Migration and Invasion
Current Cancer Drug Targets Multi-targeting the Entrance Door to Block HIV-1
Current Drug Targets - Infectious Disorders P53 Family: At the Crossroads in Cancer Therapy
Current Medicinal Chemistry Hemoglobin Neurotoxicity is Attenuated by Inhibitors of the Protein Kinase CK2 Independent of Heme Oxygenase Activity
Current Neurovascular Research Immune System Modulates the Function of Adult Neural Stem Cells
Current Immunology Reviews (Discontinued) Mitochondria-Targeting Therapeutic Strategies for Overcoming Chemoresistance and Progression of Cancer
Current Medicinal Chemistry