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
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
-
Structure, Substrate Complexation and Reaction Mechanism of Bacterial Asparaginases
Current Chemical Biology Editorial (Hot Topic Potential Value and Limitation of Dual Inhibitors of PI3K and mTOR in the Treatment of Cancer)
Current Cancer Drug Targets Microtubule Targeting Agents: A Benchmark in Cancer Therapy
Current Drug Therapy Novel Purine Nucleoside Analogues for Hematological Malignancies
Recent Patents on Anti-Cancer Drug Discovery MicroRNAs in Cancer Stem Cells: New Regulators of Stemness
Current Pharmaceutical Design Targeting the PI3K/Akt/mTOR Axis by Apigenin for Cancer Prevention
Anti-Cancer Agents in Medicinal Chemistry Effects of Oxymatrine from Ku Shen on Cancer Cells
Anti-Cancer Agents in Medicinal Chemistry Efficient Purification of rhG-CSF and its PEGylated Forms and Evaluation for In Vitro Activities
Protein & Peptide Letters Luteolin, a Flavonoid with Potential for Cancer Prevention and Therapy
Current Cancer Drug Targets Cannabinoid Type 2 Receptor as a Target for Chronic - Pain
Mini-Reviews in Medicinal Chemistry The Aging of the Adaptive Immune System
Current Immunology Reviews (Discontinued) Myeloid and Lymphoid Neoplasms with Eosinophilia and Abnormalities of PDGFRA, PDGFRB or FGFR1
Current Cancer Therapy Reviews The Use of the Zebrafish Model to Aid in Drug Discovery and Target Validation
Current Topics in Medicinal Chemistry IAPs as a Target for Anticancer Therapy
Current Cancer Drug Targets Novel Inhibitors of Inosine Monophosphate Dehydrogenase in Patent Literature of the Last Decade
Recent Patents on Anti-Cancer Drug Discovery Apoptosis-related BCL2-family Members: Key Players in Chemotherapy
Anti-Cancer Agents in Medicinal Chemistry New N’-Arylidene-2-[(4-Nitrophenyl)Piperazın-1-yl]Acetohydrazide Derivatives: Synthesis and Anticancer Activity Investigation
Letters in Drug Design & Discovery Natural Antioxidants: Therapeutic Prospects for Cancer and Neurological Diseases
Mini-Reviews in Medicinal Chemistry Cell-in-cell phenomenon: A New Paradigm in Life Sciences.
Current Molecular Medicine Theranostic Systems and Strategies for Monitoring Nanomedicine-Mediated Drug Targeting
Current Pharmaceutical Biotechnology