Abstract
Accumulating evidence has confirmed the existence and functional significance of GPCR and other types of receptor homodimers and heterodimers. However, many aspects of the biology and pharmacology of the dimerization process remain unclear. Several crystal structures of the dimerized proteins or protein-ligand complex have provided useful insights to the understanding of such process. As a common phenomenon of most receptors, homodimerization and heterodimerization have added a new dimension to characterize the receptor different from the traditional way, and open a new avenue to rational drug design and discovery.
Keywords: Homodimer, heterodimer, monomer, oligomerization, bivalent ligand, GPCR
Current Topics in Medicinal Chemistry
Title: Receptor Dimerization - Rationale for the Design of Bivalent Ligands
Volume: 7 Issue: 4
Author(s): Ao Zhang, Zhili Liu and Ying Kan
Affiliation:
Keywords: Homodimer, heterodimer, monomer, oligomerization, bivalent ligand, GPCR
Abstract: Accumulating evidence has confirmed the existence and functional significance of GPCR and other types of receptor homodimers and heterodimers. However, many aspects of the biology and pharmacology of the dimerization process remain unclear. Several crystal structures of the dimerized proteins or protein-ligand complex have provided useful insights to the understanding of such process. As a common phenomenon of most receptors, homodimerization and heterodimerization have added a new dimension to characterize the receptor different from the traditional way, and open a new avenue to rational drug design and discovery.
Export Options
About this article
Cite this article as:
Zhang Ao, Liu Zhili and Kan Ying, Receptor Dimerization - Rationale for the Design of Bivalent Ligands, Current Topics in Medicinal Chemistry 2007; 7 (4) . https://dx.doi.org/10.2174/156802607779941279
DOI https://dx.doi.org/10.2174/156802607779941279 |
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
-
Modular Nanotransporters for Targeted Intracellular Delivery of Drugs: Folate Receptors as Potential Targets
Current Pharmaceutical Design GqPCR-mediated Signalling in the Spotlight: From Visualization Towards Dissection and Quantification
Current Pharmaceutical Biotechnology Antiproliferative Effects of Molecular Iodine in Cancers
Current Chemical Biology Recent Advances in Biotransformation by Cunninghamella Species
Current Drug Metabolism The Heat Shock Protein 90 Chaperone Complex: An Evolving Therapeutic Target
Current Cancer Drug Targets Mitochondrial Superoxide Dismutase: A Promising Target for New Anticancer Therapies
Current Medicinal Chemistry Targeting Class IIa HDACs: Insights from Phenotypes and Inhibitors
Current Medicinal Chemistry Amyloidogenicity and Aggregate Cytotoxicity of Human Glucagon-Like Peptide-1 (hGLP-1)
Protein & Peptide Letters Therapy in Prion Diseases
Current Topics in Medicinal Chemistry Hypoxia Inducible Factor-1 as a Therapeutic Target in Cerebral Ischemia
Current Signal Transduction Therapy Current Pathogenesis of Alzheimer’s Disease and Plants Derived Neuroprotective Phytoconstituents: A Comprehensive Review
Current Psychopharmacology Suppression of Cancer Invasiveness by Dietary Compounds
Mini-Reviews in Medicinal Chemistry Topotecan and Irinotecan in the Treatment of Pediatric Solid Tumors
Current Pediatric Reviews HIV-1 Subtypes B and C Tat Differentially Impact Synaptic Plasticity Expression and Implicates HIV-Associated Neurocognitive Disorders§
Current HIV Research The Brain Protective Effect of rTMS (Repetitive Transcranial Magnetic Stimulation) in Depression: A Mini-Review in Animal Studies
Medicinal Chemistry Novel Approaches for Modulating dUTPase and Uracil-DNA Glycosylase: Potential Uses for Cancer and Viral Chemotherapy
Drug Design Reviews - Online (Discontinued) Circulating Levels of Soluble Angiogenic Factors in Multiple Myeloma: Correlation with Parameters of Disease Activity and Prognosis
Current Angiogenesis (Discontinued) The Role of RNA Modifications and RNA-modifying Proteins in Cancer Therapy and Drug Resistance
Current Cancer Drug Targets Amyloid Precursor Protein Processing in Vivo - Insights from a Chemically- Induced Constitutive Overactivation of Protein Kinase C in Guinea Pig Brain
Current Medicinal Chemistry MiRNAs in Human Cancers: The Diagnostic and Therapeutic Implications
Current Pharmaceutical Design