Abstract
7TM receptors constitute one of the largest superfamilies of proteins in the human genome. They are involved in a large number of physiological and pathological processes and thus represent major and important drug targets for the pharmaceutical industry. Although the majority have been deorphanized, many remain orphan and these orphan receptors constitute a large pool of potential drug targets. This review focuses on one of these orphan targets, the Epstein-Barr Virus – induced receptor 2, EBI2 (or GPR183), together with two structurally related receptors, GPR17 and GPR18. The pharmacology and “druggability” of these three receptors are reviewed through a thorough description of their structural and functional properties and in vivo biology together with a status of currently available ligands for these receptors.
Keywords: GPCR, activation mechanism, 7TM receptors, EBI2, GPR18, GPR17, constitutive activity, deorphanization, orphan receptors, druggability, chromosomal region 13q32.3, chemogenomic analysis, pertussis toxin, –, dependent manner, phosphatidylinositol turnover, posttransplant lymphoproliferative diseases
Current Topics in Medicinal Chemistry
Title: EBI2, GPR18, and GPR17 – Three Structurally Related but Biologically Distinct 7TM Receptors
Volume: 11 Issue: 6
Author(s): Kristine Norregaard, Tau Benned-Jensen and Mette Marie Rosenkilde
Affiliation:
Keywords: GPCR, activation mechanism, 7TM receptors, EBI2, GPR18, GPR17, constitutive activity, deorphanization, orphan receptors, druggability, chromosomal region 13q32.3, chemogenomic analysis, pertussis toxin, –, dependent manner, phosphatidylinositol turnover, posttransplant lymphoproliferative diseases
Abstract: 7TM receptors constitute one of the largest superfamilies of proteins in the human genome. They are involved in a large number of physiological and pathological processes and thus represent major and important drug targets for the pharmaceutical industry. Although the majority have been deorphanized, many remain orphan and these orphan receptors constitute a large pool of potential drug targets. This review focuses on one of these orphan targets, the Epstein-Barr Virus – induced receptor 2, EBI2 (or GPR183), together with two structurally related receptors, GPR17 and GPR18. The pharmacology and “druggability” of these three receptors are reviewed through a thorough description of their structural and functional properties and in vivo biology together with a status of currently available ligands for these receptors.
Export Options
About this article
Cite this article as:
Norregaard Kristine, Benned-Jensen Tau and Marie Rosenkilde Mette, EBI2, GPR18, and GPR17 – Three Structurally Related but Biologically Distinct 7TM Receptors, Current Topics in Medicinal Chemistry 2011; 11 (6) . https://dx.doi.org/10.2174/1568026611109060618
DOI https://dx.doi.org/10.2174/1568026611109060618 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
- 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
-
Viral Vector-Mediated Gene Therapy for Hemophilia
Current Gene Therapy Herpesvirus / Retrovirus Chimeric Vectors
Current Gene Therapy Novel Marine-Derived Anti-Cancer Agents
Current Pharmaceutical Design Antiviral Drug Discovery Targeting to Viral Proteases
Current Pharmaceutical Design Expression and Functions of Vasoactive Substances Regulated by Hypoxia-Inducible Factor-1 in Chronic Hypoxemia
Cardiovascular & Hematological Agents in Medicinal Chemistry The Use of Cytokines and Chemokines in the Cancer Immunotherapy
Recent Patents on Anti-Cancer Drug Discovery Are KRAS/BRAF Mutations Potent Prognostic and/or Predictive Biomarkers in Colorectal Cancers?
Anti-Cancer Agents in Medicinal Chemistry Targeting Trail Towards the Clinic
Current Drug Targets Research Progress of Glycyrrhizic Acid on Antiviral Activity
Mini-Reviews in Medicinal Chemistry Evaluation of Non-Coding RNAs as Potential Targets in Head and Neck Squamous Cell Carcinoma Cancer Stem Cells
Current Drug Targets Bioactive Compounds Containing Benzoxadiazole, Benzothiadiazole, Benzotriazole
Current Bioactive Compounds Sinonasal Carcinoma: Updated Phenotypic and Molecular Characterization
Current Cancer Therapy Reviews Hepatocyte Growth Factor Signaling in Cancer Metastasis
Current Signal Transduction Therapy Substance Abuse, HIV-1 and Hepatitis
Current HIV Research Detection and Specific Targeting of Hypoxic Regions within Solid Tumors: Current Preclinical and Clinical Strategies
Current Medicinal Chemistry A Genetic Dissection of Antipsychotic Induced Movement Disorders
Current Medicinal Chemistry Editorial [Hot Topic: Molecular Targeted Therapy of Gastrointestinal Cancer (Guest Editor: Marcus W. Wiedmann)]
Current Cancer Drug Targets Lumiflavin Enhances the Effects of Ionising Radiation on Ovarian Cancer Stem-Like Cells by Inhibiting Autophagy
Anti-Cancer Agents in Medicinal Chemistry The Imaging of Apoptosis with the Radiolabelled Annexin A5: A New Tool in Translational Research
Current Clinical Pharmacology Dexamethasone Reduces Cell Adhesion and Migration of T47D Breast Cancer Cell Line
Anti-Cancer Agents in Medicinal Chemistry