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http://hdl.handle.net/1843/56274| Type: | Artigo de Periódico |
| Title: | Synthesis and evaluation of benzothiazole-triazole and benzothiadiazole-triazole scaffolds as potential molecular probes for amyloid-β aggregation |
| Authors: | Christine Dyrager Rafael Pinto Vieira Sofie Nyström K. Peter R. Nilsson Tim Storr |
| Abstract: | Small-molecule ligands that bind to misfolded protein aggregates are essential tools for the study and detection of pathological hallmarks in neurodegenerative disorders, such as Alzheimer's disease (AD). In the present study, three compounds (one benzothiazole-triazole, L1, and two benzothiadiazole-triazoles, L2 and L3) were synthesized via a modular approach (azide–alkyne cycloaddition) and evaluated as potential ligands for amyloid-β (Aβ) aggregates. The binding to amyloid-like fibrils, generated from recombinant Aβ1–42, were studied and the binding specificity to amyloid deposits was evaluated in brain sections from transgenic mice with AD pathology. All three derivatives showed significant reduced emission in the presence of recombinant Aβ1–42 amyloid fibrils. In addition, the observed binding to Aβ deposits in tissue sections suggests that the benzothiazole-triazole and benzothiadiazole-triazole structures are promising molecular scaffolds that can be modified for binding to specific protein aggregates. |
| Subject: | Fungicidas Doença de Alzheimer Doenças neurodegenerativas |
| language: | eng |
| metadata.dc.publisher.country: | Brasil |
| Publisher: | Universidade Federal de Minas Gerais |
| Publisher Initials: | UFMG |
| metadata.dc.publisher.department: | ICB - DEPARTAMENTO DE BIOQUÍMICA E IMUNOLOGIA |
| Rights: | Acesso Restrito |
| metadata.dc.identifier.doi: | https://doi.org/10.1039/C6NJ01703G |
| URI: | http://hdl.handle.net/1843/56274 |
| Issue Date: | 2017 |
| metadata.dc.url.externa: | https://pubs.rsc.org/en/content/articlelanding/2017/NJ/C6NJ01703G |
| metadata.dc.relation.ispartof: | New Journal of Chemistry |
| Appears in Collections: | Artigo de Periódico |
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