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Issue 3, 2016
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Lipodisks integrated with weak affinity chromatography enable fragment screening of integral membrane proteins

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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.

Graphical abstract: Lipodisks integrated with weak affinity chromatography enable fragment screening of integral membrane proteins

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Publication details

The article was received on 12 Oct 2015, accepted on 03 Dec 2015 and first published on 07 Dec 2015


Article type: Paper
DOI: 10.1039/C5AN02105G
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Citation: Analyst, 2016,141, 981-988

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    Lipodisks integrated with weak affinity chromatography enable fragment screening of integral membrane proteins

    M. Duong-Thi, M. Bergström, K. Edwards, J. Eriksson, S. Ohlson, J. To Yiu Ying, J. Torres and V. Agmo Hernández, Analyst, 2016, 141, 981
    DOI: 10.1039/C5AN02105G

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