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Title: Lipodisks integrated with weak affinity chromatography enable fragment screening of integral membrane proteins
Authors: Duong-Thi, Minh-Dao
Bergström, Maria
Edwards, Katarina
Eriksson, Jonny
Ohlson, Sten
To Yiu Ying, Janet
Torres, Jaume
Agmo Hernández, Víctor
Keywords: Biological Sciences
Issue Date: 2016
Source: Duong-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.
Series/Report no.: The Analyst
Abstract: Membrane 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.
ISSN: 0003-2654
DOI: 10.1039/C5AN02105G
Schools: School of Biological Sciences 
Fulltext Permission: open
Fulltext Availability: With Fulltext
Appears in Collections:SBS Journal Articles

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