Abstract
Background: Family B G protein-coupled receptors (GPCRs) play an important role in many physiological and pathophysiological processes. They are plasma-membrane proteins containing an extracellular N-domain, an intracellular C-tail, seven transmembrane domains (TMs), three extracellular (ELs) and three intracellular (ILs) loops.
Objective: This review aims to summarize the current structural and functional information for family B GPCRs and their ligands, as well as, their physiological and pathophysiological role.
Methods: Α thorough search of bibliographic databases for peer-reviewed research literature was undertaken. Moreover, molecular models of family B GPCRs were constructed and a structural alignment of their amino acid sequences was performed to demonstrate common structural characteristics.
Results: In this review the family B GPCRs and their complexes with the receptor activity modifying proteins (RAMPs) were classified into five groups and the important physiological and pathophysiological role of these receptors was summarized. In addition, conserved residues of the Ndomain and the TMs of these receptors were numbered, thus making feasible the comparison of receptor structures and demonstrating common structural characteristics that are functionally important for all family B receptors. Molecular models created in this study were used to discuss the molecular mechanisms underlying ligand binding to family B GPCRs and receptor activation.
Conclusion: The findings of this review provide information about the structural-functional determinants of family B GPCRs and their ligands, thus boosting the design of novel drugs with better potencies and bioavailabilities, which might enrich the therapeutic armory for the treatment of a wide spectrum of family B GPCRs-related disorders.
Keywords: Family B GPCRs, ligands, binding, receptor activation, antagonists, structure, signaling, physiological/ pathophysiological role.
Current Medicinal Chemistry
Title:Family B G Protein-coupled Receptors and their Ligands: From Structure to Function
Volume: 24 Issue: 31
Author(s): George Liapakis*, Minos-Timotheos Matsoukas, Vlasios Karageorgos, Maria Venihaki and Thomas Mavromoustakos
Affiliation:
- Department of Pharmacology, School of Medicine, University of Crete, Voutes, Heraklion, 71003, Crete,Greece
Keywords: Family B GPCRs, ligands, binding, receptor activation, antagonists, structure, signaling, physiological/ pathophysiological role.
Abstract: Background: Family B G protein-coupled receptors (GPCRs) play an important role in many physiological and pathophysiological processes. They are plasma-membrane proteins containing an extracellular N-domain, an intracellular C-tail, seven transmembrane domains (TMs), three extracellular (ELs) and three intracellular (ILs) loops.
Objective: This review aims to summarize the current structural and functional information for family B GPCRs and their ligands, as well as, their physiological and pathophysiological role.
Methods: Α thorough search of bibliographic databases for peer-reviewed research literature was undertaken. Moreover, molecular models of family B GPCRs were constructed and a structural alignment of their amino acid sequences was performed to demonstrate common structural characteristics.
Results: In this review the family B GPCRs and their complexes with the receptor activity modifying proteins (RAMPs) were classified into five groups and the important physiological and pathophysiological role of these receptors was summarized. In addition, conserved residues of the Ndomain and the TMs of these receptors were numbered, thus making feasible the comparison of receptor structures and demonstrating common structural characteristics that are functionally important for all family B receptors. Molecular models created in this study were used to discuss the molecular mechanisms underlying ligand binding to family B GPCRs and receptor activation.
Conclusion: The findings of this review provide information about the structural-functional determinants of family B GPCRs and their ligands, thus boosting the design of novel drugs with better potencies and bioavailabilities, which might enrich the therapeutic armory for the treatment of a wide spectrum of family B GPCRs-related disorders.
Export Options
About this article
Cite this article as:
Liapakis George*, Matsoukas Minos-Timotheos, Karageorgos Vlasios, Venihaki Maria and Mavromoustakos Thomas, Family B G Protein-coupled Receptors and their Ligands: From Structure to Function, Current Medicinal Chemistry 2017; 24 (31) . https://dx.doi.org/10.2174/0929867324666170303162416
DOI https://dx.doi.org/10.2174/0929867324666170303162416 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
Call for Papers in Thematic Issues
Advances in Medicinal Chemistry: From Cancer to Chronic Diseases.
The broad spectrum of the issue will provide a comprehensive overview of emerging trends, novel therapeutic interventions, and translational insights that impact modern medicine. The primary focus will be diseases of global concern, including cancer, chronic pain, metabolic disorders, and autoimmune conditions, providing a broad overview of the advancements in ...read more
Cellular and Molecular Mechanisms of Non-Infectious Inflammatory Diseases: Focus on Clinical Implications
The Special Issue covers the results of the studies on cellular and molecular mechanisms of non-infectious inflammatory diseases, in particular, autoimmune rheumatic diseases, atherosclerotic cardiovascular disease and other age-related disorders such as type II diabetes, cancer, neurodegenerative disorders, etc. Review and research articles as well as methodology papers that summarize ...read more
Chalcogen-modified nucleic acid analogues
Chalcogen-modified nucleosides, nucleotides and oligonucleotides have been of great interest to scientific research for many years. The replacement of oxygen in the nucleobase, sugar or phosphate backbone by chalcogen atoms (sulfur, selenium, tellurium) gives these biomolecules unique properties resulting from their altered physical and chemical properties. The continuing interest in ...read more
Current advances in inherited cardiomyopathy
Describe in detail all novel advances in multimodality imaging related to inherited cardiomyopathy diagnosis and prognosis. Shed light to deeper phenotypic characterization. Acknowledge recent advances in genetics, genomics and precision medicineread 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
-
Recent Patents on Proteasome Inhibitors of Natural Origin
Recent Patents on Anti-Cancer Drug Discovery Cardiovascular Disease Risk Among the Poor and Homeless – What We Know So Far
Current Cardiology Reviews The Role of STAT 3 in Tissue Fibrosis
Current Chemical Biology Molecular Basis of Mineralocorticoid Receptor Action in the Nervous System
CNS & Neurological Disorders - Drug Targets Is It Possible to Apply Secondary Stroke Prevention Guidelines to Very Old Populations?
Cardiovascular & Hematological Disorders-Drug Targets Cardiovascular Effects of Losartan and Its Relevant Clinical Application
Current Medicinal Chemistry Blood Atherogenicity as a Target for Anti-atherosclerotic Therapy
Current Pharmaceutical Design A Comprehensive Study of Pharmacological Behaviors, Nano-Formulations, and Applications of Rosemary
The Natural Products Journal Myocardial Expression of TNF-α, IL-1β, IL-6, IL-8, IL-10 and MCP-1 After a Single MDMA Dose Administered in a Rat Model
Current Pharmaceutical Biotechnology Mechanical Circulatory Support of the Critically Ill Child Awaiting Heart Transplantation
Current Cardiology Reviews Targeted Drug Delivery for Breast Cancer Treatment
Recent Patents on Anti-Cancer Drug Discovery Modulation of Energy Intake and Expenditure Due to Habitual Physical Exercise
Current Pharmaceutical Design Recent Advances in Pulmonary Hypertension Therapy
Recent Patents on Cardiovascular Drug Discovery Intratubular Renin-Angiotensin System in Hypertension
Current Hypertension Reviews The Role of Renal Nerve Ablation for the Management of Resistant Hypertension and other Disease Conditions: Benefits and Concerns
Current Vascular Pharmacology Microvascular Alterations in Hypertension and Vascular Aging
Current Hypertension Reviews MicroRNAs as Diagnostic, Prognostic and Predictive Biomarkers of Cardiac Disease
Recent Patents on Biomarkers Synthetic Curcumin Analog UBS109 Inhibits the Growth of Head and Neck Squamous Cell Carcinoma Xenografts
Current Cancer Drug Targets Anti-proliferative Properties of miR-20b and miR-363 from the miR-106a-363 Cluster on Human Carcinoma Cells
MicroRNA Platelet-Derived Chemokines in Atherogenesis: What’s New?
Current Vascular Pharmacology