dc.contributor.author
Henning, Lisa Maria
dc.contributor.author
Bhatia, Sumati
dc.contributor.author
Bertazzon, Miriam
dc.contributor.author
Marczynke, Michaela
dc.contributor.author
Seitz, Oliver
dc.contributor.author
Volkmer, Rudolf
dc.contributor.author
Haag, Rainer
dc.contributor.author
Freund, Christian
dc.date.accessioned
2018-06-08T04:18:05Z
dc.date.available
2015-06-04T07:47:24.211Z
dc.identifier.uri
https://refubium.fu-berlin.de/handle/fub188/16998
dc.identifier.uri
http://dx.doi.org/10.17169/refubium-21178
dc.description.abstract
The coupling of peptides to polyglycerol carriers represents an important
route towards the multivalent display of protein ligands. In particular, the
inhibition of low affinity intracellular protein–protein interactions can be
addressed by this design. We have applied this strategy to develop binding
partners for FBP21, a protein which is important for the splicing of pre-mRNA
in the nucleus of eukaryotic cells. Firstly, by using phage display the
optimized sequence WPPPPRVPR was derived which binds with KDs of 80 μM and 150
µM to the individual WW domains and with a KD of 150 μM to the tandem-WW1–WW2
construct. Secondly, this sequence was coupled to a hyperbranched polyglycerol
(hPG) that allowed for the multivalent display on the surface of the dendritic
polymer. This novel multifunctional hPG-peptide conjugate displayed a KD of
17.6 µM which demonstrates that the new carrier provides a venue for the
future inhibition of proline-rich sequence recognition by FBP21 during
assembly of the spliceosome.
de
dc.rights.uri
http://creativecommons.org/licenses/by/2.0/
dc.subject
isothermal titration calorimetry
dc.subject
multivalent polymers
dc.subject
polyglycerol peptide conjugates
dc.subject
proline-rich sequence recognition
dc.subject.ddc
500 Naturwissenschaften und Mathematik::540 Chemie
dc.title
Exploring monovalent and multivalent peptides for the inhibition of FBP21-tWW
dc.type
Wissenschaftlicher Artikel
dcterms.bibliographicCitation
Beilstein J. Org. Chem. - 11 (2015), S. 701–706
dcterms.bibliographicCitation.doi
10.3762/bjoc.11.80
dcterms.bibliographicCitation.url
http://www.beilstein-journals.org/bjoc/single/articleFullText.htm?publicId=1860-5397-11-80
refubium.affiliation
Biologie, Chemie, Pharmazie
de
refubium.mycore.fudocsId
FUDOCS_document_000000022541
refubium.note.author
Der Artikel wurde in einer Open-Access-Zeitschrift publiziert.
refubium.resourceType.isindependentpub
no
refubium.mycore.derivateId
FUDOCS_derivate_000000004988
dcterms.accessRights.openaire
open access