Differential membrane binding of α/β-peptide foldamers: implications for cellular delivery and mitochondrial targeting
نویسندگان
چکیده
The intrinsic pathway of apoptosis is regulated by the Bcl-2 family proteins. Inhibition anti-apoptotic members represents a strategy to induce apoptotic cell death in cancer cells. We have measured membrane binding properties series peptides, including modified α/β-peptides, designed exhibit enhanced permeability allow entry and improved access for engagement members. peptide cargo based on pro-apoptotic protein Bim, which interacts with all proteins initiate apoptosis. α/β-peptides contained cyclic β-amino acid residues increase their stability permeability. Dual polarisation interferometry was used study each two different model systems mimic either plasma or outer mitochondrial membrane. impact structure also investigated, results demonstrated that peptides had increased affinity significantly altered bilayer. showed presence an RRR motif ability bind insert into mimic, provide insights role selective targeting peptides.
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ژورنال
عنوان ژورنال: Australian Journal of Chemistry
سال: 2023
ISSN: ['0004-9425', '1445-0038']
DOI: https://doi.org/10.1071/ch23063