Abstract
G protein coupled receptors (GPCRs) are membrane proteins coupled with G proteins through which they transmit signals to the cytoplasm. Approximately 30% of pharmaceuticals target these receptors, even though crystal structures were scarce at the time. Furthermore, an additional 15% of GPCRs have yet to be exploited for therapeutic intervention. An overview of structural information is presented, with emphasis on rearrangements occurring during activation,in light of recently resolved activated state crystal structures. Computational efforts over recent years are also highlighted.
Keywords: G Protein Coupled Receptors, Homology Modeling, Virtual Screening, Model-Building, Critical Assessment of Structure Prediction, Docking, Structure-Based Drug Design, Activation Mechanisms, Conserved Motifs.
Current Topics in Medicinal Chemistry
Title:G Protein Coupled Receptors And Structure-Based Advances
Volume: 16 Issue: 13
Author(s): Maria Kontoyianni
Affiliation:
Keywords: G Protein Coupled Receptors, Homology Modeling, Virtual Screening, Model-Building, Critical Assessment of Structure Prediction, Docking, Structure-Based Drug Design, Activation Mechanisms, Conserved Motifs.
Abstract: G protein coupled receptors (GPCRs) are membrane proteins coupled with G proteins through which they transmit signals to the cytoplasm. Approximately 30% of pharmaceuticals target these receptors, even though crystal structures were scarce at the time. Furthermore, an additional 15% of GPCRs have yet to be exploited for therapeutic intervention. An overview of structural information is presented, with emphasis on rearrangements occurring during activation,in light of recently resolved activated state crystal structures. Computational efforts over recent years are also highlighted.
Export Options
About this article
Cite this article as:
Kontoyianni Maria, G Protein Coupled Receptors And Structure-Based Advances, Current Topics in Medicinal Chemistry 2016; 16 (13) . https://dx.doi.org/10.2174/1568026615666150915121324
DOI https://dx.doi.org/10.2174/1568026615666150915121324 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
Call for Papers in Thematic Issues
Chemistry Based on Natural Products for Therapeutic Purposes
The development of new pharmaceuticals for a wide range of medical conditions has long relied on the identification of promising natural products (NPs). There are over sixty percent of cancer, infectious illness, and CNS disease medications that include an NP pharmacophore, according to the Food and Drug Administration. Since NP ...read more
Current Trends in Drug Discovery Based on Artificial Intelligence and Computer-Aided Drug Design
Drug development discovery has faced several challenges over the years. In fact, the evolution of classical approaches to modern methods using computational methods, or Computer-Aided Drug Design (CADD), has shown promising and essential results in any drug discovery campaign. Among these methods, molecular docking is one of the most notable ...read more
Drug Discovery in the Age of Artificial Intelligence
In the age of artificial intelligence (AI), we have witnessed a significant boom in AI techniques for drug discovery. AI techniques are increasingly integrated and accelerating the drug discovery process. These developments have not only attracted the attention of academia and industry but also raised important questions regarding the selection ...read more
From Biodiversity to Chemical Diversity: Focus of Flavonoids
Flavonoids are the largest group of polyphenols, plant secondary metabolites arising from the essential aromatic amino acid phenylalanine (or more rarely from tyrosine) via the phenylpropanoid pathway. The flavan nucleus is the basic 15-carbon skeleton of flavonoids (C6-C3-C6), which consists of two phenyl rings (A and B) and a heterocyclic ...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
-
Proteasome Inhibition in Transplantation-Focusing on the Experience with Bortezomib
Current Pharmaceutical Design Resveratrol: A New Potential Therapeutic Agent for Melanoma?
Current Medicinal Chemistry Electrotransfer into Skeletal Muscle for Protein Expression
Current Gene Therapy Interaction of Drug or Food with Drug Transporters in Intestine and Liver
Current Drug Metabolism Arnica compositum, Hekla lava and Acidum Nitricum Together are Superior to Arnica compositum Alone in the Local Treatment of Symptomatic Calcific Periarthritis of the Shoulder: A Pilot Study
Reviews on Recent Clinical Trials The Synergistic Effects of DNA-Targeted Chemotherapeutics and Histone Deacetylase Inhibitors As Therapeutic Strategies for Cancer Treatment
Current Medicinal Chemistry Hyper-Coagulable Profile with Elevated Pro-Thrombotic Biomarkers and Increased Cerebro- and Cardio-Vascular Disease Risk Exist Among Healthy Dyslipidemic Women
Current Neurovascular Research Aspirin: from a Historical Perspective
Recent Patents on Cardiovascular Drug Discovery HIV-1 Tat Protein Exposure Potentiates Ethanol Reward and Reinstates Extinguished Ethanol-Conditioned Place Preference
Current HIV Research Tumor Necrosis Factor-a Blockade in Rheumatoid Arthritis: Responders Vs Non Responders
Medicinal Chemistry Reviews - Online (Discontinued) Bioactivities of Iridoids
Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry Meet Our Editor:
Inflammation & Allergy - Drug Targets (Discontinued) An Update on the Other Telomerase Inhibitors: Non-G-Quadruplex Interactive Agent, Non-Antisense, Non-Reverse Transcriptase Telomerase Inhibitors
Medicinal Chemistry Reviews - Online (Discontinued) Chemical Crosslinking: Role in Protein and Peptide Science
Current Protein & Peptide Science Purines as Neurotransmitters and Neuromodulators in Blood Vessels
Current Vascular Pharmacology Pilot Study of the Reducing Effect on Amyloidosis In Vivo by Three FDA Pre-Approved Drugs Via the Alzheimers APP 5Untranslated Region
Current Alzheimer Research A Descriptive Analysis of Post-Chemotherapy Development of Interstitial Lung Disease Using Spontaneous Reporting Data in Japan
Current Drug Safety Noradrenaline-mediated Inhibition of Inflammatory Cytokines is Altered in Macrophages from Obese Zucker Rats: Effect of Habitual Exercise
Endocrine, Metabolic & Immune Disorders - Drug Targets γ-Secretase as a Target for Alzheimers Disease
Current Topics in Medicinal Chemistry Impact of Cellular Senescence in Aging and Cancer
Current Pharmaceutical Design