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Screening of small ...
Screening of small molecules using the inhibition of oligomer formation in α-synuclein aggregation as a selection parameter
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- Staats, Roxine (författare)
- University of Cambridge
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- Michaels, Thomas C.T. (författare)
- University of Cambridge,Harvard University
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- Flagmeier, Patrick (författare)
- University of Cambridge
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- Chia, Sean (författare)
- University of Cambridge
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- Horne, Robert I. (författare)
- University of Cambridge
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- Habchi, Johnny (författare)
- University of Cambridge
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- Linse, Sara (författare)
- Lund University,Lunds universitet,NanoLund: Centre for Nanoscience,Annan verksamhet, LTH,Lunds Tekniska Högskola,Biokemi och Strukturbiologi,Centrum för Molekylär Proteinvetenskap,Kemiska institutionen,Institutioner vid LTH,Other operations, LTH,Faculty of Engineering, LTH,Biochemistry and Structural Biology,Center for Molecular Protein Science,Department of Chemistry,Departments at LTH,Faculty of Engineering, LTH
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- Knowles, Tuomas P.J. (författare)
- University of Cambridge
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- Dobson, Christopher M. (författare)
- University of Cambridge
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- Vendruscolo, Michele (författare)
- University of Cambridge
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(creator_code:org_t)
- 2020-12-18
- 2020
- Engelska.
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Ingår i: Communications Chemistry. - : Springer Science and Business Media LLC. - 2399-3669. ; 3:1
- Relaterad länk:
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http://dx.doi.org/10... (free)
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https://www.nature.c...
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https://lup.lub.lu.s...
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https://doi.org/10.1...
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Abstract
Ämnesord
Stäng
- The aggregation of α-synuclein is a central event in Parkinsons’s disease and related synucleinopathies. Since pharmacologically targeting this process, however, has not yet resulted in approved disease-modifying treatments, there is an unmet need of developing novel methods of drug discovery. In this context, the use of chemical kinetics has recently enabled accurate quantifications of the microscopic steps leading to the proliferation of protein misfolded oligomers. As these species are highly neurotoxic, effective therapeutic strategies may be aimed at reducing their numbers. Here, we exploit this quantitative approach to develop a screening strategy that uses the reactive flux toward α-synuclein oligomers as a selection parameter. Using this approach, we evaluate the efficacy of a library of flavone derivatives, identifying apigenin as a compound that simultaneously delays and reduces the formation of α-synuclein oligomers. These results demonstrate a compound selection strategy based on the inhibition of the formation of α-synuclein oligomers, which may be key in identifying small molecules in drug discovery pipelines for diseases associated with α-synuclein aggregation.
Ämnesord
- MEDICIN OCH HÄLSOVETENSKAP -- Medicinska och farmaceutiska grundvetenskaper -- Neurovetenskaper (hsv//swe)
- MEDICAL AND HEALTH SCIENCES -- Basic Medicine -- Neurosciences (hsv//eng)
- NATURVETENSKAP -- Biologi -- Biokemi och molekylärbiologi (hsv//swe)
- NATURAL SCIENCES -- Biological Sciences -- Biochemistry and Molecular Biology (hsv//eng)
Publikations- och innehållstyp
- art (ämneskategori)
- ref (ämneskategori)
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Till lärosätets databas
- Av författaren/redakt...
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Staats, Roxine
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Michaels, Thomas ...
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Flagmeier, Patri ...
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Chia, Sean
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Horne, Robert I.
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Habchi, Johnny
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visa fler...
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Linse, Sara
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Knowles, Tuomas ...
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Dobson, Christop ...
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Vendruscolo, Mic ...
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visa färre...
- Om ämnet
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- MEDICIN OCH HÄLSOVETENSKAP
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MEDICIN OCH HÄLS ...
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och Medicinska och f ...
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och Neurovetenskaper
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- NATURVETENSKAP
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NATURVETENSKAP
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och Biologi
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och Biokemi och mole ...
- Artiklar i publikationen
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Communications C ...
- Av lärosätet
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Lunds universitet