Rationally designed peptides inhibit the formation of α-synuclein fibrils and oligomers.

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Tác giả: Mohammed Al-Azzani, Tariq T Ali, Gerhard H Braus, Luisa Maria Gatzemeier, Michael Hoppert, Dora Kaloyanova, Madiha Merghani, Piotr Neumann, Tiago F Outeiro, Blagovesta Popova

Ngôn ngữ: eng

Ký hiệu phân loại:

Thông tin xuất bản: France : European journal of medicinal chemistry , 2025

Mô tả vật lý:

Bộ sưu tập: NCBI

ID: 739040

Parkinson's Disease (PD) is characterized by the pathological aggregation of α-synuclein (αSyn) into oligomers and amyloid fibrils, making αSyn aggregation a key target for drug development. Peptides have gained recent attention as potential agents to inhibit aggregation. Two previously identified peptide inhibitors, discovered through large-scale yeast screening, were used as templates for in silico mutagenesis aimed at designing novel peptides with improved efficacy in inhibiting αSyn aggregation and cytotoxicity. The newly designed peptides underwent in silico docking analysis, and the most promising candidates were tested in vitro and in cellular models. Peptides T02 and T05 emerged as the most effective inhibitors, with T02 binding αSyn monomers and T05 targeting lower-order oligomers. Both peptides reduce αSyn fibril and oligomer formation in vitro and significantly suppress αSyn aggregation and cytotoxicity in yeast and human H4 cells. These novel peptides represent antagonists of αSyn aggregation with promising potential for therapeutic intervention for PD.
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