Sökning: id:"swepub:oai:gup.ub.gu.se/218001" >
8-Triazolylpurines:...
8-Triazolylpurines: Towards Fluorescent Inhibitors of the MDM2/p53 Interaction
-
- Pettersson, Mariell, 1984 (författare)
- Gothenburg University,Göteborgs universitet,Institutionen för kemi och molekylärbiologi,Department of Chemistry and Molecular Biology,University of Gothenburg
-
- Bliman, David (författare)
- Gothenburg University,Göteborgs universitet,Institutionen för kemi och molekylärbiologi,Department of Chemistry and Molecular Biology,University of Gothenburg
-
- Jacobsson, Jimmy (författare)
- Gothenburg University,Göteborgs universitet,Institutionen för kemi och molekylärbiologi,Department of Chemistry and Molecular Biology,University of Gothenburg,St. Jude Children Research Hospital
-
visa fler...
-
- Nilsson, Jesper, 1984 (författare)
- Chalmers tekniska högskola,Chalmers University of Technology
-
Min, J. (författare)
-
- Iconaru, L. (författare)
- St. Jude Children Research Hospital
-
- Guy, R. K. (författare)
- St. Jude Children Research Hospital
-
- Kriwacki, R. W. (författare)
- St. Jude Children Research Hospital
-
- Andreasson, Joakim, 1973 (författare)
- Chalmers tekniska högskola,Chalmers University of Technology
-
- Grøtli, Morten, 1966 (författare)
- Gothenburg University,Göteborgs universitet,Institutionen för kemi och molekylärbiologi,Department of Chemistry and Molecular Biology,University of Gothenburg
-
visa färre...
-
(creator_code:org_t)
- 2015-05-05
- 2015
- Engelska.
-
Ingår i: PLoS ONE. - : Public Library of Science (PLoS). - 1932-6203. ; 10:5
- Relaterad länk:
-
https://gup.ub.gu.se... (primary) (free)
-
visa fler...
-
https://journals.plo...
-
http://publications.... (primary) (free)
-
https://gup.ub.gu.se...
-
https://doi.org/10.1...
-
https://research.cha...
-
visa färre...
Abstract
Ämnesord
Stäng
- Small molecule nonpeptidic mimics of alpha-helices are widely recognised as protein-protein interaction (PPIs) inhibitors. Protein-protein interactions mediate virtually all important regulatory pathways in a cell, and the ability to control and modulate PPIs is therefore of great significance to basic biology, where controlled disruption of protein networks is key to understanding network connectivity and function. We have designed and synthesised two series of 2,6,9-substituted 8-triazolylpurines as alpha-helix mimetics. The first series was designed based on low energy conformations but did not display any biological activity in a biochemical fluorescence polarisation assay targeting MDM2/p53. Although solution NMR conformation studies demonstrated that such molecules could mimic the topography of an alpha-helix, docking studies indicated that the same compounds were not optimal as inhibitors for the MDM2/p53 interaction. A new series of 8-triazolylpurines was designed based on a combination of docking studies and analysis of recently published inhibitors. The best compound displayed low micromolar inhibitory activity towards MDM2/p53 in a biochemical fluorescence polarisation assay. In order to evaluate the applicability of these compounds as biologically active and intrinsically fluorescent probes, their absorption/emission properties were measured. The compounds display fluorescent properties with quantum yields up to 50%.
Ämnesord
- NATURVETENSKAP -- Kemi (hsv//swe)
- NATURAL SCIENCES -- Chemical Sciences (hsv//eng)
Publikations- och innehållstyp
- ref (ämneskategori)
- art (ämneskategori)
Hitta via bibliotek
-
PLoS ONE
(Sök värdpublikationen i LIBRIS)
Till lärosätets databas
- Av författaren/redakt...
-
Pettersson, Mari ...
-
Bliman, David
-
Jacobsson, Jimmy
-
Nilsson, Jesper, ...
-
Min, J.
-
Iconaru, L.
-
visa fler...
-
Guy, R. K.
-
Kriwacki, R. W.
-
Andreasson, Joak ...
-
Grøtli, Morten, ...
-
visa färre...
- Om ämnet
-
- NATURVETENSKAP
-
NATURVETENSKAP
-
och Kemi
- Artiklar i publikationen
-
PLoS ONE
- Av lärosätet
-
Göteborgs universitet
-
Chalmers tekniska högskola