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Multivariate design...
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Larsson, AndreasUmeå universitet,Kemiska institutionen
(author)
Multivariate design, synthesis, and biological evaluation of peptide inhibitors of FimC/FimH protein-protein interactions in uropathogenic Escherichia coli
- Article/chapterEnglish2005
Publisher, publication year, extent ...
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2005-02-01
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American Chemical Society (ACS),2005
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printrdacarrier
Numbers
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LIBRIS-ID:oai:DiVA.org:umu-13553
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https://urn.kb.se/resolve?urn=urn:nbn:se:umu:diva-13553URI
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https://doi.org/10.1021/jm040818lDOI
Supplementary language notes
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Language:English
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Summary in:English
Part of subdatabase
Classification
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Subject category:ref swepub-contenttype
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Subject category:art swepub-publicationtype
Notes
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A peptide library targeting protein-protein interactions crucial for pilus assembly in Gram negative bacteria has been designed using statistical molecular design. A nonamer peptide scaffold was used, with seven positions being varied. The selection was performed in the building block space, and previously known structure-activity data were included in the design procedure. This resulted in a heavily reduced library consisting of 32 peptides which was prepared by solid-phase synthesis. The ability of the peptides to inhibit the protein-protein interaction between the periplasmic chaperone FimC and the pilus adhesin FimH was then determined in an ELISA. Novel peptides with the capability to inhibit the FimC/FimH protein(-)protein interaction to the same extent as the native FimC peptides were discovered. Multivariate QSAR studies of the response in the ELISA gave valuable information on the properties of amino acids which were preferred at the seven positions in the nonamer scaffold. This information can be used in attempts to develop optimized peptides and peptidomimetics that inhibit pilus assembly in pathogenic bacteria.
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Added entries (persons, corporate bodies, meetings, titles ...)
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Johansson, Susanne M. C.Umeå universitet,Kemiska institutionen
(author)
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Pinkner, Jerome S.
(author)
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Hultgren, Scott J.
(author)
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Almqvist, FredrikUmeå universitet,Kemiska institutionen(Swepub:umu)fral0001
(author)
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Kihlberg, JanUmeå universitet,Kemiska institutionen(Swepub:umu)jaki0001
(author)
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Linusson, AnnaUmeå universitet,Kemiska institutionen(Swepub:umu)analin99
(author)
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Umeå universitetKemiska institutionen
(creator_code:org_t)
Related titles
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In:Journal of Medicinal Chemistry: American Chemical Society (ACS)48:4, s. 935-9450022-26231520-4804
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