Zobrazeno 1 - 10
of 15
pro vyhledávání: '"Stefan Rubner"'
Autor:
Nagarajan Elumalai, Angela Berg, Stefan Rubner, Linda Blechschmidt, Chen Song, Kalaiselvi Natarajan, Jörg Matysik, Thorsten Berg
Publikováno v:
Scientific Reports, Vol 7, Iss 1, Pp 1-9 (2017)
Abstract The transcription factor STAT5b is a target for tumour therapy. We recently reported catechol bisphosphate and derivatives such as Stafib-1 as the first selective inhibitors of the STAT5b SH2 domain. Here, we demonstrate STAT5b binding of ca
Externí odkaz:
https://doaj.org/article/7eb0fb05f08d4517a3fb77233ccd9bc2
Autor:
Nora Raulien, Kathleen Friedrich, Sarah Strobel, Stefan Rubner, Sven Baumann, Martin von Bergen, Antje Körner, Martin Krueger, Manuela Rossol, Ulf Wagner
Publikováno v:
Frontiers in Immunology, Vol 8 (2017)
Monocytes enter sites of microbial or sterile inflammation as the first line of defense of the immune system and initiate pro-inflammatory effector mechanisms. We show that activation with bacterial lipopolysaccharide (LPS) induces them to undergo a
Externí odkaz:
https://doaj.org/article/71cf90a8636b43909de2f52342d55cb5
Autor:
Florian Nietzold, Stefan Rubner, Beata Labuzek, Przemysław Golik, Ewa Surmiak, Xabier del Corte, Radoslaw Kitel, Christoph Protzel, Regina Reppich‐Sacher, Jan Stichel, Katarzyna Magiera‐Mularz, Tad A. Holak, Thorsten Berg
Publikováno v:
ChemBioChem. 24
Nutlin-3a is a reversible inhibitor of the p53/MDM2 interaction. We have synthesized the derivative Nutlin-3a-aa bearing an additional exocyclic methylene group in the piperazinone moiety. Nutlin-3a-aa is more active than Nutlin-3a against purified w
Autor:
Jens Meiler, Julian Gräb, Martin Gräber, Stefan Rubner, Angela Berg, Linda Blechschmidt, Darwin Y. Fu, Barbara Klüver, Thorsten Berg
Publikováno v:
ACS Chemical Biology. 14:796-805
STAT family proteins are important mediators of cell signaling and represent therapeutic targets for the treatment of human diseases. Most STAT inhibitors target the protein-protein interaction domain, the SH2 domain, but specificity for a single STA
Publikováno v:
Angewandte Chemie. 130:17289-17293
Hydrophobic tagging (HT) of bioactive compounds can induce target degradation via the proteasomal pathway. The first application of hydrophobic tagging to an existing inhibitor of protein-protein interactions is now presented. We developed Poloxin-2H
Publikováno v:
Chemistry - A European Journal. 24:13762-13766
Strain-promoted azide-alkyne cycloadditions (SPAAC) have proven extremely useful for labeling of biomolecules, but typically produce isomeric mixtures. This is not appropriate for the formation of bioactive molecules in living cells. Here, the first
Publikováno v:
Chemical communications (Cambridge, England). 55(95)
We present the first application of hydrophobic tagging to a non-covalent inhibitor of protein–protein interactions. Nutlin-3a-HT, created by fusing the hydrophobic tag HyT13 to the MDM2–p53 interaction inhibitor Nutlin-3a, prevented cellular acc
Publikováno v:
Chemistry (Weinheim an Der Bergstrasse, Germany)
We present a new approach for the identification of inhibitors of phosphorylation‐dependent protein–protein interaction domains, in which phenolic fragments are adapted by in silico O‐phosphorylation before docking‐based screening. From a dat
Publikováno v:
Organicbiomolecular chemistry. 17(12)
We report the hydrophobically-tagged Plk1 PBD inhibitor Poloxin-2HT+, which selectively degrades the tumor target Plk1 and induces apoptosis in human tumor cells with higher potency than the hydrophobically-tagged inhibitor Poloxin-2HT. Our data prov
Autor:
Manuela Rossol, Martin von Bergen, Antje Körner, Ulf Wagner, Stefan Rubner, Sarah Strobel, Nora Raulien, Sven Baumann, Martin Krueger, Kathleen Friedrich
Publikováno v:
Frontiers in Immunology, Vol 8 (2017)
Frontiers in Immunology
Frontiers in Immunology
Monocytes enter sites of microbial or sterile inflammation as the first line of defense of the immune system and initiate pro-inflammatory effector mechanisms. We show that activation with bacterial lipopolysaccharide (LPS) induces them to undergo a