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WFRF:(Snijder Arjan 1971)
 

Sökning: WFRF:(Snijder Arjan 1971) > Drug Discovery at t...

LIBRIS Formathandbok  (Information om MARC21)
FältnamnIndikatorerMetadata
00002608naa a2200349 4500
001oai:research.chalmers.se:f5c257aa-0e97-4150-9974-2a8454885a2d
003SwePub
008171007s2015 | |||||||||||000 ||eng|
024a https://research.chalmers.se/publication/2173922 URI
024a https://doi.org/10.1021/acs.analchem.5b007402 DOI
040 a (SwePub)cth
041 a engb eng
042 9 SwePub
072 7a art2 swepub-publicationtype
072 7a ref2 swepub-contenttype
100a Gunnarsson, Anders,d 1981u AstraZeneca AB4 aut0 (Swepub:cth)kb01guan
2451 0a Drug Discovery at the Single Molecule Level: Inhibition-in-Solution Assay of Membrane-Reconstituted beta-Secretase Using Single-Molecule Imaging
264 c 2015-04-10
264 1b American Chemical Society (ACS),c 2015
520 a 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
650 7a NATURVETENSKAPx Kemix Analytisk kemi0 (SwePub)104012 hsv//swe
650 7a NATURAL SCIENCESx Chemical Sciencesx Analytical Chemistry0 (SwePub)104012 hsv//eng
700a Snijder, Arjan,d 1971u AstraZeneca AB4 aut
700a Hicks, J.u AstraZeneca AB4 aut
700a Gunnarsson, J.u AstraZeneca AB4 aut
700a Höök, Fredrik,d 1966u Chalmers tekniska högskola,Chalmers University of Technology4 aut0 (Swepub:cth)fredrikh
700a Geschwindner, S.u AstraZeneca AB4 aut
710a AstraZeneca ABb Chalmers tekniska högskola4 org
773t Analytical Chemistryd : American Chemical Society (ACS)g 87:8, s. 4100-4103q 87:8<4100-4103x 0003-2700x 1520-6882
856u http://dx.doi.org/10.1021/acs.analchem.5b00740y FULLTEXT
8564 8u https://research.chalmers.se/publication/217392
8564 8u https://doi.org/10.1021/acs.analchem.5b00740

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