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dc.contributor.authorDuong-Thi, Minh-Daoen
dc.contributor.authorBergström, Mariaen
dc.contributor.authorEdwards, Katarinaen
dc.contributor.authorEriksson, Jonnyen
dc.contributor.authorOhlson, Stenen
dc.contributor.authorTo Yiu Ying, Janeten
dc.contributor.authorTorres, Jaumeen
dc.contributor.authorAgmo Hernández, Víctoren
dc.identifier.citationDuong-Thi, M. D., Bergström, M., Edwards, K., Eriksson, J., Ohlson, S., To Yiu Ying, J., et al. (2016). Lipodisks integrated with weak affinity chromatography enable fragment screening of integral membrane proteins. Analyst, 141(3), 981-988.en
dc.description.abstractMembrane proteins constitute the largest class of drug targets but they present many challenges in drug discovery. Importantly, the discovery of potential drug candidates is hampered by the limited availability of efficient methods for screening drug-protein interactions. In this work we present a novel strategy for rapid identification of molecules capable of binding to a selected membrane protein. An integral membrane protein (human aquaporin-1) was incorporated into planar lipid bilayer disks (lipodisks), which were subsequently covalently coupled to porous derivatized silica and packed into HPLC columns. The obtained affinity columns were used in a typical protocol for fragment screening by weak affinity chromatography (WAC), in which one hit was identified out of a 200 compound collection. The lipodisk-based strategy, which ensures a stable and native-like lipid environment for the protein, is expected to work also with other membrane proteins and screening procedures.en
dc.description.sponsorshipNRF (Natl Research Foundation, S’pore)en
dc.format.extent22 p.en
dc.relation.ispartofseriesThe Analysten
dc.subjectBiological Sciencesen
dc.titleLipodisks integrated with weak affinity chromatography enable fragment screening of integral membrane proteinsen
dc.typeJournal Articleen
dc.contributor.schoolSchool of Biological Sciencesen
dc.description.versionAccepted versionen
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