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.
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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 |
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