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000136651 0247_ $$2doi$$a10.1074/jbc.M112.357665
000136651 0247_ $$2pmid$$apmid:22891248
000136651 0247_ $$2pmc$$apmc:PMC3464581
000136651 0247_ $$2ISSN$$a0021-9258
000136651 0247_ $$2ISSN$$a1067-8816
000136651 0247_ $$2ISSN$$a1083-351X
000136651 0247_ $$2altmetric$$aaltmetric:887460
000136651 037__ $$aDZNE-2020-02973
000136651 041__ $$aEnglish
000136651 082__ $$a540
000136651 1001_ $$0P:(DE-HGF)0$$aKroth, Heiko$$b0
000136651 245__ $$aDiscovery and structure activity relationship of small molecule inhibitors of toxic β-amyloid-42 fibril formation.
000136651 260__ $$aBethesda, Md.$$bSoc.60645$$c2012
000136651 264_1 $$2Crossref$$3online$$bAmerican Society for Biochemistry & Molecular Biology (ASBMB)$$c2012-08-13
000136651 264_1 $$2Crossref$$3print$$bAmerican Society for Biochemistry & Molecular Biology (ASBMB)$$c2012-10-05
000136651 3367_ $$2DRIVER$$aarticle
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000136651 3367_ $$0PUB:(DE-HGF)16$$2PUB:(DE-HGF)$$aJournal Article$$bjournal$$mjournal$$s1585575296_26569
000136651 3367_ $$2BibTeX$$aARTICLE
000136651 3367_ $$2ORCID$$aJOURNAL_ARTICLE
000136651 3367_ $$00$$2EndNote$$aJournal Article
000136651 520__ $$aIncreasing 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.
000136651 536__ $$0G:(DE-HGF)POF3-342$$a342 - Disease Mechanisms and Model Systems (POF3-342)$$cPOF3-342$$fPOF III$$x0
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000136651 650_7 $$2NLM Chemicals$$a3-aminopyrazole
000136651 650_7 $$2NLM Chemicals$$aAmyloid beta-Peptides
000136651 650_7 $$2NLM Chemicals$$aCytotoxins
000136651 650_7 $$2NLM Chemicals$$aPeptide Fragments
000136651 650_7 $$2NLM Chemicals$$aPyrazoles
000136651 650_7 $$2NLM Chemicals$$aamyloid beta-protein (1-42)
000136651 650_2 $$2MeSH$$aAmyloid beta-Peptides: antagonists & inhibitors
000136651 650_2 $$2MeSH$$aAmyloid beta-Peptides: chemistry
000136651 650_2 $$2MeSH$$aCell Line, Tumor
000136651 650_2 $$2MeSH$$aCytotoxins: antagonists & inhibitors
000136651 650_2 $$2MeSH$$aCytotoxins: chemistry
000136651 650_2 $$2MeSH$$aHumans
000136651 650_2 $$2MeSH$$aHydrogen Bonding
000136651 650_2 $$2MeSH$$aHydrophobic and Hydrophilic Interactions
000136651 650_2 $$2MeSH$$aPeptide Fragments: antagonists & inhibitors
000136651 650_2 $$2MeSH$$aPeptide Fragments: chemistry
000136651 650_2 $$2MeSH$$aProtein Structure, Secondary
000136651 650_2 $$2MeSH$$aPyrazoles: chemistry
000136651 650_2 $$2MeSH$$aStructure-Activity Relationship
000136651 7001_ $$0P:(DE-HGF)0$$aAnsaloni, Annalisa$$b1
000136651 7001_ $$0P:(DE-HGF)0$$aVarisco, Yvan$$b2
000136651 7001_ $$0P:(DE-HGF)0$$aJan, Asad$$b3
000136651 7001_ $$0P:(DE-HGF)0$$aSreenivasachary, Nampally$$b4
000136651 7001_ $$0P:(DE-HGF)0$$aRezaei-Ghaleh, Nasrollah$$b5
000136651 7001_ $$0P:(DE-HGF)0$$aGiriens, Valérie$$b6
000136651 7001_ $$0P:(DE-HGF)0$$aLohmann, Sophie$$b7
000136651 7001_ $$0P:(DE-HGF)0$$aLópez-Deber, María Pilar$$b8
000136651 7001_ $$0P:(DE-HGF)0$$aAdolfsson, Oskar$$b9
000136651 7001_ $$0P:(DE-HGF)0$$aPihlgren, Maria$$b10
000136651 7001_ $$0P:(DE-HGF)0$$aPaganetti, Paolo$$b11
000136651 7001_ $$0P:(DE-HGF)0$$aFroestl, Wolfgang$$b12
000136651 7001_ $$0P:(DE-HGF)0$$aNagel-Steger, Luitgard$$b13
000136651 7001_ $$0P:(DE-HGF)0$$aWillbold, Dieter$$b14
000136651 7001_ $$0P:(DE-HGF)0$$aSchrader, Thomas$$b15
000136651 7001_ $$0P:(DE-2719)2810591$$aZweckstetter, Markus$$b16$$udzne
000136651 7001_ $$0P:(DE-HGF)0$$aPfeifer, Andrea$$b17
000136651 7001_ $$0P:(DE-HGF)0$$aLashuel, Hilal A$$b18
000136651 7001_ $$0P:(DE-HGF)0$$aMuhs, Andreas$$b19$$eCorresponding author
000136651 77318 $$2Crossref$$3journal-article$$a10.1074/jbc.m112.357665$$b : American Society for Biochemistry & Molecular Biology (ASBMB), 2012-08-13$$n41$$p34786-34800$$tJournal of Biological Chemistry$$v287$$x0021-9258$$y2012
000136651 773__ $$0PERI:(DE-600)1474604-9$$a10.1074/jbc.M112.357665$$gVol. 287, no. 41, p. 34786 - 34800$$n41$$p34786-34800$$q287:41<34786 - 34800$$tThe journal of biological chemistry$$v287$$x0021-9258$$y2012
000136651 8567_ $$2Pubmed Central$$uhttp://www.ncbi.nlm.nih.gov/pmc/articles/PMC3464581
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000136651 9101_ $$0I:(DE-588)1065079516$$6P:(DE-2719)2810591$$aDeutsches Zentrum für Neurodegenerative Erkrankungen$$b16$$kDZNE
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000136651 9141_ $$y2012
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