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| 001 | 136651 | ||
| 005 | 20240321220118.0 | ||
| 024 | 7 | _ | |a 10.1074/jbc.M112.357665 |2 doi |
| 024 | 7 | _ | |a pmid:22891248 |2 pmid |
| 024 | 7 | _ | |a pmc:PMC3464581 |2 pmc |
| 024 | 7 | _ | |a 0021-9258 |2 ISSN |
| 024 | 7 | _ | |a 1067-8816 |2 ISSN |
| 024 | 7 | _ | |a 1083-351X |2 ISSN |
| 024 | 7 | _ | |a altmetric:887460 |2 altmetric |
| 037 | _ | _ | |a DZNE-2020-02973 |
| 041 | _ | _ | |a English |
| 082 | _ | _ | |a 540 |
| 100 | 1 | _ | |a Kroth, Heiko |0 P:(DE-HGF)0 |b 0 |
| 245 | _ | _ | |a Discovery and structure activity relationship of small molecule inhibitors of toxic β-amyloid-42 fibril formation. |
| 260 | _ | _ | |a Bethesda, Md. |c 2012 |b Soc.60645 |
| 264 | _ | 1 | |3 online |2 Crossref |b American Society for Biochemistry & Molecular Biology (ASBMB) |c 2012-08-13 |
| 264 | _ | 1 | |3 print |2 Crossref |b American Society for Biochemistry & Molecular Biology (ASBMB) |c 2012-10-05 |
| 336 | 7 | _ | |a article |2 DRIVER |
| 336 | 7 | _ | |a Output Types/Journal article |2 DataCite |
| 336 | 7 | _ | |a Journal Article |b journal |m journal |0 PUB:(DE-HGF)16 |s 1585575296_26569 |2 PUB:(DE-HGF) |
| 336 | 7 | _ | |a ARTICLE |2 BibTeX |
| 336 | 7 | _ | |a JOURNAL_ARTICLE |2 ORCID |
| 336 | 7 | _ | |a Journal Article |0 0 |2 EndNote |
| 520 | _ | _ | |a Increasing evidence implicates Aβ peptides self-assembly and fibril formation as crucial events in the pathogenesis of Alzheimer disease. Thus, inhibiting Aβ aggregation, among others, has emerged as a potential therapeutic intervention for this disorder. Herein, we employed 3-aminopyrazole as a key fragment in our design of non-dye compounds capable of interacting with Aβ42 via a donor-acceptor-donor hydrogen bond pattern complementary to that of the β-sheet conformation of Aβ42. The initial design of the compounds was based on connecting two 3-aminopyrazole moieties via a linker to identify suitable scaffold molecules. Additional aryl substitutions on the two 3-aminopyrazole moieties were also explored to enhance π-π stacking/hydrophobic interactions with amino acids of Aβ42. The efficacy of these compounds on inhibiting Aβ fibril formation and toxicity in vitro was assessed using a combination of biophysical techniques and viability assays. Using structure activity relationship data from the in vitro assays, we identified compounds capable of preventing pathological self-assembly of Aβ42 leading to decreased cell toxicity. |
| 536 | _ | _ | |a 342 - Disease Mechanisms and Model Systems (POF3-342) |0 G:(DE-HGF)POF3-342 |c POF3-342 |f POF III |x 0 |
| 588 | _ | _ | |a Dataset connected to CrossRef, PubMed, |
| 650 | _ | 7 | |a 3-aminopyrazole |2 NLM Chemicals |
| 650 | _ | 7 | |a Amyloid beta-Peptides |2 NLM Chemicals |
| 650 | _ | 7 | |a Cytotoxins |2 NLM Chemicals |
| 650 | _ | 7 | |a Peptide Fragments |2 NLM Chemicals |
| 650 | _ | 7 | |a Pyrazoles |2 NLM Chemicals |
| 650 | _ | 7 | |a amyloid beta-protein (1-42) |2 NLM Chemicals |
| 650 | _ | 2 | |a Amyloid beta-Peptides: antagonists & inhibitors |2 MeSH |
| 650 | _ | 2 | |a Amyloid beta-Peptides: chemistry |2 MeSH |
| 650 | _ | 2 | |a Cell Line, Tumor |2 MeSH |
| 650 | _ | 2 | |a Cytotoxins: antagonists & inhibitors |2 MeSH |
| 650 | _ | 2 | |a Cytotoxins: chemistry |2 MeSH |
| 650 | _ | 2 | |a Humans |2 MeSH |
| 650 | _ | 2 | |a Hydrogen Bonding |2 MeSH |
| 650 | _ | 2 | |a Hydrophobic and Hydrophilic Interactions |2 MeSH |
| 650 | _ | 2 | |a Peptide Fragments: antagonists & inhibitors |2 MeSH |
| 650 | _ | 2 | |a Peptide Fragments: chemistry |2 MeSH |
| 650 | _ | 2 | |a Protein Structure, Secondary |2 MeSH |
| 650 | _ | 2 | |a Pyrazoles: chemistry |2 MeSH |
| 650 | _ | 2 | |a Structure-Activity Relationship |2 MeSH |
| 700 | 1 | _ | |a Ansaloni, Annalisa |0 P:(DE-HGF)0 |b 1 |
| 700 | 1 | _ | |a Varisco, Yvan |0 P:(DE-HGF)0 |b 2 |
| 700 | 1 | _ | |a Jan, Asad |0 P:(DE-HGF)0 |b 3 |
| 700 | 1 | _ | |a Sreenivasachary, Nampally |0 P:(DE-HGF)0 |b 4 |
| 700 | 1 | _ | |a Rezaei-Ghaleh, Nasrollah |0 P:(DE-HGF)0 |b 5 |
| 700 | 1 | _ | |a Giriens, Valérie |0 P:(DE-HGF)0 |b 6 |
| 700 | 1 | _ | |a Lohmann, Sophie |0 P:(DE-HGF)0 |b 7 |
| 700 | 1 | _ | |a López-Deber, María Pilar |0 P:(DE-HGF)0 |b 8 |
| 700 | 1 | _ | |a Adolfsson, Oskar |0 P:(DE-HGF)0 |b 9 |
| 700 | 1 | _ | |a Pihlgren, Maria |0 P:(DE-HGF)0 |b 10 |
| 700 | 1 | _ | |a Paganetti, Paolo |0 P:(DE-HGF)0 |b 11 |
| 700 | 1 | _ | |a Froestl, Wolfgang |0 P:(DE-HGF)0 |b 12 |
| 700 | 1 | _ | |a Nagel-Steger, Luitgard |0 P:(DE-HGF)0 |b 13 |
| 700 | 1 | _ | |a Willbold, Dieter |0 P:(DE-HGF)0 |b 14 |
| 700 | 1 | _ | |a Schrader, Thomas |0 P:(DE-HGF)0 |b 15 |
| 700 | 1 | _ | |a Zweckstetter, Markus |0 P:(DE-2719)2810591 |b 16 |u dzne |
| 700 | 1 | _ | |a Pfeifer, Andrea |0 P:(DE-HGF)0 |b 17 |
| 700 | 1 | _ | |a Lashuel, Hilal A |0 P:(DE-HGF)0 |b 18 |
| 700 | 1 | _ | |a Muhs, Andreas |0 P:(DE-HGF)0 |b 19 |e Corresponding author |
| 773 | 1 | 8 | |a 10.1074/jbc.m112.357665 |b : American Society for Biochemistry & Molecular Biology (ASBMB), 2012-08-13 |n 41 |p 34786-34800 |3 journal-article |2 Crossref |t Journal of Biological Chemistry |v 287 |y 2012 |x 0021-9258 |
| 773 | _ | _ | |a 10.1074/jbc.M112.357665 |g Vol. 287, no. 41, p. 34786 - 34800 |0 PERI:(DE-600)1474604-9 |n 41 |q 287:41<34786 - 34800 |p 34786-34800 |t The journal of biological chemistry |v 287 |y 2012 |x 0021-9258 |
| 856 | 7 | _ | |2 Pubmed Central |u http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3464581 |
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| 910 | 1 | _ | |a Deutsches Zentrum für Neurodegenerative Erkrankungen |0 I:(DE-588)1065079516 |k DZNE |b 16 |6 P:(DE-2719)2810591 |
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