![]() Our technical consultants would be happy to discuss your structural design needs with you at any time. ![]() To transform this first-generation compound into a lead compound, diversification of staple type and position combined with fine-tuning core hydrophobicity and positive net charge is likely to increase. The resultant stapled peptides are then able to compete efficiently for binding to protein targets involved in protein-protein interactions that are mediated by -helices. Stapling is carried out by covalently linking the. A major limitation of the stapled peptide is its predominant endocytic uptake resulting in high peptide amounts being trapped in endosomes. Stapling is a key technique for stabilising peptides in an -helical structure. A stapled peptide is a short peptide, typically in an alpha-helical conformation, that is constrained by a synthetic brace (staple). CPC Scientific has extensively developed stapled peptide structures and is the company of choice to manufacture your stapled peptide requirements. Peptide stapling is a strategy for constraining short peptides typically in an alpha-helical conformation. As a rapidly emerging class of next-generation drugs, stapled peptides are expected to combine the synthetic manipulability and cell-penetrating ability of small molecules with the three-dimensionality and versatile target recognition ability of biologics. Because stapled peptides are locked into a stabilized α-helical structure (the most common element of protein secondary structures), they can easily penetrate cells. Small molecules only work on proteins with a specific feature on their surfaces and most protein biologics do not penetrate into cells. Stapled peptides show an ability to inhibit intracellular PPIs that previously have been intractable with traditional small molecule or biologics. The idea of peptide stapling was introduced to overcome the limitations of two broad classes of therapeutic agents (small molecules and protein biologics) in targeting intracellular protein-protein interactions. design a stapled peptide, SP9, which blocks. Hydrocarbon stapled peptides are peptides locked into their bioactive alpha-helical conformation through site-specific introduction of a chemical brace, an all-hydrocarbon staple. Excessive secretion of mucus is the major cause of airway obstruction in respiratory diseases.
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