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- Duong-Thi, Minh-DaoLinnéuniversitetet,Institutionen för kemi och biomedicin (KOB),Nanyang Technol University, Singapore (author)
Lipodisks integrated with weak affinity chromatography enable fragment screening of integral membrane proteins
- Article/chapterEnglish2016
Publisher, publication year, extent ...
- 2016
- Royal Society of Chemistry (RSC),2016
- printrdacarrier
Numbers
- LIBRIS-ID:oai:DiVA.org:lnu-50634
- https://urn.kb.se/resolve?urn=urn:nbn:se:lnu:diva-50634URI
- https://doi.org/10.1039/c5an02105gDOI
Supplementary language notes
- Language:English
- Summary in:English
Part of subdatabase
- SwePubSwePub
Classification
Notes
- 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.
Subject headings and genre
- NATURVETENSKAP Kemi Analytisk kemi hsv//swe
- NATURAL SCIENCES Chemical Sciences Analytical Chemistry hsv//eng
- Analytisk kemi
- Analytical Chemistry
Added entries (persons, corporate bodies, meetings, titles ...)
- Bergström, MariaLinnéuniversitetet,Institutionen för kemi och biomedicin (KOB)(Swepub:lnu)nbema (author)
- Edwards, KatarinaUppsala University (author)
- Eriksson, JonnyUppsala University (author)
- Ohlson, StenLinnéuniversitetet,Institutionen för kemi och biomedicin (KOB)(Swepub:lnu)nohst (author)
- To Yiu Ying, JanetNanyang Technol University, Singapore (author)
- Torres, JaumeNanyang Technol University, Singapore (author)
- Agmo Hernández, VíctorUppsala University (author)
- LinnéuniversitetetInstitutionen för kemi och biomedicin (KOB) (creator_code:org_t)
Related titles
- In:The Analyst: Royal Society of Chemistry (RSC)141:3, s. 981-9880003-26541364-5528
Internet link
- https://dr.ntu.edu.sg/bitstream/10356/80267/2/Supporting%20information_Lipodisks%20Integrated%20with%20Weak%20Affinity%20Chromatography%20Enable%20Fragment%20Screening%20of%20Integral%20Membrane%20Proteins.pdf
- https://urn.kb.se/resolve?urn=urn:nbn:se:lnu:diva-50634
- https://doi.org/10.1039/c5an02105g
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