Sökning: WFRF:(Snijder Arjan 1971) > Drug Discovery at t...
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000 | 02608naa a2200349 4500 | |
001 | oai:research.chalmers.se:f5c257aa-0e97-4150-9974-2a8454885a2d | |
003 | SwePub | |
008 | 171007s2015 | |||||||||||000 ||eng| | |
024 | 7 | a https://research.chalmers.se/publication/2173922 URI |
024 | 7 | a https://doi.org/10.1021/acs.analchem.5b007402 DOI |
040 | a (SwePub)cth | |
041 | a engb eng | |
042 | 9 SwePub | |
072 | 7 | a art2 swepub-publicationtype |
072 | 7 | a ref2 swepub-contenttype |
100 | 1 | a Gunnarsson, Anders,d 1981u AstraZeneca AB4 aut0 (Swepub:cth)kb01guan |
245 | 1 0 | a 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 | 1 | b 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 | 7 | a NATURVETENSKAPx Kemix Analytisk kemi0 (SwePub)104012 hsv//swe |
650 | 7 | a NATURAL SCIENCESx Chemical Sciencesx Analytical Chemistry0 (SwePub)104012 hsv//eng |
700 | 1 | a Snijder, Arjan,d 1971u AstraZeneca AB4 aut |
700 | 1 | a Hicks, J.u AstraZeneca AB4 aut |
700 | 1 | a Gunnarsson, J.u AstraZeneca AB4 aut |
700 | 1 | a Höök, Fredrik,d 1966u Chalmers tekniska högskola,Chalmers University of Technology4 aut0 (Swepub:cth)fredrikh |
700 | 1 | a Geschwindner, S.u AstraZeneca AB4 aut |
710 | 2 | a AstraZeneca ABb Chalmers tekniska högskola4 org |
773 | 0 | t Analytical Chemistryd : American Chemical Society (ACS)g 87:8, s. 4100-4103q 87:8<4100-4103x 0003-2700x 1520-6882 |
856 | 4 | u http://dx.doi.org/10.1021/acs.analchem.5b00740y FULLTEXT |
856 | 4 8 | u https://research.chalmers.se/publication/217392 |
856 | 4 8 | u https://doi.org/10.1021/acs.analchem.5b00740 |
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