Search Results - "Graeber, Martin"
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Serendipitous alkylation of a Plk1 ligand uncovers a new binding channel
Published in Nature chemical biology (17-07-2011)“…Polo-like kinase 1 (Plk1) regulates multiple processes that are important for cell proliferation, and it is a promising anticancer drug target. Efforts to…”
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The STAT5b Linker Domain Mediates the Selectivity of Catechol Bisphosphates for STAT5b over STAT5a
Published in ACS chemical biology (19-04-2019)“…STAT family proteins are important mediators of cell signaling and represent therapeutic targets for the treatment of human diseases. Most STAT inhibitors…”
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Direct monitoring of protein–protein inhibition using nano electrospray ionization mass spectrometry
Published in Chemical science (Cambridge) (2014)“…Dissociation of the TNF-alpha trimer caused by the small-molecule inhibitor SPD304 was monitored using native ESI-MS and ion mobility spectrometry (IMS). Upon…”
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A High-Throughput Fluorescence Polarization-Based Assay for the SH2 Domain of STAT4
Published in Methods and protocols (23-11-2022)“…The signal transducer and activation of transcription (STAT) proteins are a family of Src homology 2 (SH2) domain-containing transcription factors. The family…”
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Development of high-throughput assays based on fluorescence polarization for inhibitors of the polo-box domains of polo-like kinases 2 and 3
Published in Analytical biochemistry (15-12-2009)“…The serine/threonine kinases Plk1, Plk2, and Plk3 harbor a protein–protein interaction domain dubbed polo-box domain (PBD). Recently, the inhibition of the PBD…”
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Oral Disinfectants Inhibit Protein-Protein Interactions Mediated by the Anti-Apoptotic Protein Bcl-x sub(L) and Induce Apoptosis in Human Oral Tumor Cells
Published in Angewandte Chemie International Edition (01-04-2013)“…Chlorhexidine and alexidine have long been used as oral disinfectants by humans. Both compounds inhibit protein-protein interactions mediated by the…”
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Synthesis and biochemical evaluation of highly enantiomerically pure (R,R)- and (S,S)-alexidine
Published in Bioorganic & medicinal chemistry (01-12-2013)“…Alexidine is in everyday human use as oral disinfectant and contact lens disinfectant. It is used as a mixture of stereoisomers. Since all of alexidine’s known…”
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Selective Targeting of Disease-Relevant Protein Binding Domains by O-Phosphorylated Natural Product Derivatives
Published in ACS chemical biology (21-10-2011)“…Phosphorylation-dependent protein binding domains are crucially important for intracellular signaling pathways and thus highly relevant targets in chemical…”
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The Natural Product Betulinic Acid Inhibits C/EBP Family Transcription Factors
Published in Chembiochem : a European journal of chemical biology (23-01-2012)“…Nature does it: Small‐molecule inhibitors of transcription factors are highly sought after, but only a limited number are known to date. Here, we report the…”
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Phosphopeptides with improved cellular uptake properties as ligands for the polo-box domain of polo-like kinase 1
Published in Bioorganic & medicinal chemistry letters (15-08-2011)“…Human polo-like kinase 1 (Plk1) is involved in cell proliferation and overexpressed in a broad variety of different cancer types. Due to its crucial role in…”
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