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Drug Discovery at t...
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Gunnarsson, Anders,1981AstraZeneca AB
(författare)
Drug Discovery at the Single Molecule Level: Inhibition-in-Solution Assay of Membrane-Reconstituted beta-Secretase Using Single-Molecule Imaging
- Artikel/kapitelEngelska2015
Förlag, utgivningsår, omfång ...
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2015-04-10
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American Chemical Society (ACS),2015
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LIBRIS-ID:oai:research.chalmers.se:f5c257aa-0e97-4150-9974-2a8454885a2d
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https://research.chalmers.se/publication/217392URI
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https://doi.org/10.1021/acs.analchem.5b00740DOI
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Språk:engelska
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Sammanfattning på:engelska
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Ämneskategori:art swepub-publicationtype
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Ämneskategori:ref swepub-contenttype
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Inhibition-in-solution assays (ISA) employing surface-based biosensors such as surface plasmon resonance (SPR) are an effective screening approach in drug discovery. However, analysis of potent binders remains a significant hurdle due to limited sensitivity and accompanied depletion of the inhibiting compounds due to high protein concentrations needed for detectable binding signals. To overcome this limitation, we explored a microscopy-based single-molecule ISA compatible with liposome-reconstituted membrane proteins. Using a set of validated small molecule inhibitors against beta-secretase 1 (BACE1), the assay was benchmarked with respect to sensitivity and dynamic range against SPR. We demonstrate that the dynamic range of measurable affinities is greatly extended by more than 2 orders of magnitude as compared to SPR, thus facilitating measurements of highly potent (K-d
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Biuppslag (personer, institutioner, konferenser, titlar ...)
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Snijder, Arjan,1971AstraZeneca AB
(författare)
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Hicks, J.AstraZeneca AB
(författare)
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Gunnarsson, J.AstraZeneca AB
(författare)
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Höök, Fredrik,1966Chalmers tekniska högskola,Chalmers University of Technology(Swepub:cth)fredrikh
(författare)
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Geschwindner, S.AstraZeneca AB
(författare)
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AstraZeneca ABChalmers tekniska högskola
(creator_code:org_t)
Sammanhörande titlar
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Ingår i:Analytical Chemistry: American Chemical Society (ACS)87:8, s. 4100-41030003-27001520-6882
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