Abstract
The receptor mimetic and mast cell degranulating peptide mastoparan (MP) translocates cell membranes as an amphipathic α-helix, a feature that is undoubtedly a major determinant of bioactivity through the activation of heterotrimeric G proteins. Chimeric combinations of MP with G protein-coupled receptor (GPCR) ligands has produced peptides that exhibit biological activities distinct from their composite components. Thus, chimeric peptides such as galparan and M391 differentially modulate GTPase activity, display altered binding affinities for appropriate GPCRs and possess disparate secretory properties. MP and MP-containing chimerae also bind and modulate the activities of various other intracellular protein targets and are valuable tools to manipulate and study enzymatic activity, calcium homeostasis and apoptotic signalling pathways. In addition, charge delocalisation within the hydrophilic face of MP has produced analogues, including [Lys5, Lys8,Aib10]MP, that differentially regulate mast cell secretion and/or cytotoxicity. Finally, the identification of cell penetrant variants of MP chimerae has enabled the effective intracellular delivery of non-permeable biomolecules and presents an opportunity to target novel intracellular therapeutic loci.
Keywords: Mastoparan, G protein-coupled receptors, chimerism, secretion, cytotoxicity, analogues, α-aminoisobutyric acid, signal transduction and transportan
Current Protein & Peptide Science
Title: Biological Applications of the Receptor Mimetic Peptide Mastoparan
Volume: 7 Issue: 6
Author(s): Sarah Jones and John Howl
Affiliation:
Keywords: Mastoparan, G protein-coupled receptors, chimerism, secretion, cytotoxicity, analogues, α-aminoisobutyric acid, signal transduction and transportan
Abstract: The receptor mimetic and mast cell degranulating peptide mastoparan (MP) translocates cell membranes as an amphipathic α-helix, a feature that is undoubtedly a major determinant of bioactivity through the activation of heterotrimeric G proteins. Chimeric combinations of MP with G protein-coupled receptor (GPCR) ligands has produced peptides that exhibit biological activities distinct from their composite components. Thus, chimeric peptides such as galparan and M391 differentially modulate GTPase activity, display altered binding affinities for appropriate GPCRs and possess disparate secretory properties. MP and MP-containing chimerae also bind and modulate the activities of various other intracellular protein targets and are valuable tools to manipulate and study enzymatic activity, calcium homeostasis and apoptotic signalling pathways. In addition, charge delocalisation within the hydrophilic face of MP has produced analogues, including [Lys5, Lys8,Aib10]MP, that differentially regulate mast cell secretion and/or cytotoxicity. Finally, the identification of cell penetrant variants of MP chimerae has enabled the effective intracellular delivery of non-permeable biomolecules and presents an opportunity to target novel intracellular therapeutic loci.
Export Options
About this article
Cite this article as:
Jones Sarah and Howl John, Biological Applications of the Receptor Mimetic Peptide Mastoparan, Current Protein & Peptide Science 2006; 7 (6) . https://dx.doi.org/10.2174/138920306779025585
DOI https://dx.doi.org/10.2174/138920306779025585 |
Print ISSN 1389-2037 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5550 |
Call for Papers in Thematic Issues
Advancements in Proteomic and Peptidomic Approaches in Cancer Immunotherapy: Unveiling the Immune Microenvironment
The scope of this thematic issue centers on the integration of proteomic and peptidomic technologies into the field of cancer immunotherapy, with a particular emphasis on exploring the tumor immune microenvironment. This issue aims to gather contributions that illustrate the application of these advanced methodologies in unveiling the complex interplay ...read more
Artificial Intelligence for Protein Research
Protein research, essential for understanding biological processes and creating therapeutics, faces challenges due to the intricate nature of protein structures and functions. Traditional methods are limited in exploring the vast protein sequence space efficiently. Artificial intelligence (AI) and machine learning (ML) offer promising solutions by improving predictions and speeding up ...read more
Nutrition and Metabolism in Musculoskeletal Diseases
The musculoskeletal system consists mainly of cartilage, bone, muscles, tendons, connective tissue and ligaments. Balanced metabolism is of vital importance for the homeostasis of the musculoskeletal system. A series of musculoskeletal diseases (for example, sarcopenia, osteoporosis) are resulted from the dysregulated metabolism of the musculoskeletal system. Furthermore, metabolic diseases (such ...read more
Protein Folding, Aggregation and Liquid-Liquid Phase Separation
Protein folding, misfolding and aggregation remain one of the main problems of interdisciplinary science not only because many questions are still open, but also because they are important from the point of view of practical application. Protein aggregation and formation of fibrillar structures, for example, is a hallmark of a ...read more
Related Journals
- 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
Related Articles
-
The Acute Phase Protein α1-Acid Glycoprotein: A Model for Altered Glycosylation During Diseases
Current Protein & Peptide Science <i>Uncaria tomentosa</i> (Willd. ex Schult.): Focus on Nutraceutical Aspects
Current Bioactive Compounds The Applications of Biomarkers in Early Clinical Drug Development to Improve Decision-Making Processes
Current Clinical Pharmacology Redox Homeostasis, Bioactive Agents and Transduction Therapy
Current Signal Transduction Therapy Microenvironmental Interactions in Chronic Lymphocytic Leukemia: Hints for Pathogenesis and Identification of Targets for Rational Therapy
Current Pharmaceutical Design Bruton Kinase Inhibitors in Chronic Lymphocytic Leukemia
Anti-Cancer Agents in Medicinal Chemistry A Novel Method for Screening of Anti-Cancer Drugs: Availability of Screening in Acidic Medium
Recent Patents on Biomedical Engineering (Discontinued) 1,3,4-Oxadiazole Derivatives as Potential Biological Agents
Mini-Reviews in Medicinal Chemistry Phosphoproteomics as a Promising Tool for Broadening the Analysis of Clinical Samples and for the Fight Against Cancer Disease
Current Pharmaceutical Analysis Glycerophospholipid Synthesis as a Novel Drug Target Against Cancer
Current Molecular Pharmacology Lipid-Based Drug Delivery Systems for Cancer Treatment
Current Drug Targets Targeting the p53-Family in Cancer and Chemosensitivity: Triple Threat
Current Drug Targets Flavonoid-Based Cancer Therapy: An Updated Review
Anti-Cancer Agents in Medicinal Chemistry Investigating ABCB1-Mediated Drug-Drug Interactions: Considerations for In vitro and In vivo Assay Design
Current Drug Metabolism Synergy Against Fungal Pathogens: Working Together is Better Than Working Alone
Current Medicinal Chemistry Role of Oxidative Stress in Hepatitis C Virus Induced Hepatocellular Carcinoma
Current Cancer Drug Targets Drug Repurposing for the Treatment of Staphylococcal Infections
Current Pharmaceutical Design Melatonin a Promising Candidate for DNA Double-Stranded Breaks Reduction in Patients Undergoing Abdomen-Pelvis Computed Tomography Examinations
Anti-Cancer Agents in Medicinal Chemistry Synthesis of a Tyr-Tyr Dipeptide Library and Evaluation Against Tumor Cells
Medicinal Chemistry Malignant Mesothelioma: Biology, Diagnosis and Therapeutic Approaches
Current Molecular Pharmacology