Karl Heinz Klempnauer
Yusenko M, Jakobs A, Klempnauer K. A novel cell-based screening assay for small-molecule MYB inhibitors identifies podophyllotoxins teniposide and etoposide as inhibitors of MYB activity. Sci Rep. 2018;8:13159 pubmed publisher
..Teniposide and etoposide therefore act like double-edged swords that might be particularly effective to inhibit tumor cells with deregulated MYB. ..
Uttarkar S, Dukare S, Bopp B, Goblirsch M, Jose J, Klempnauer K. Naphthol AS-E Phosphate Inhibits the Activity of the Transcription Factor Myb by Blocking the Interaction with the KIX Domain of the Coactivator p300. Mol Cancer Ther. 2015;14:1276-85 pubmed publisher
Ohnheiser J, Ferlemann E, Haas A, MÃ¼ller J, Werwein E, Fehler O, et al
. Programmed cell death 4 protein (Pdcd4) and homeodomain-interacting protein kinase 2 (Hipk2) antagonistically control translation of Hipk2 mRNA. Biochim Biophys Acta. 2015;1853:1564-73 pubmed publisher
..Furthermore, the effect of Hipk2 on the translation of Hipk1 RNA suggests that Hipk2 and Pdcd4 can act in similar manner to control the translation of other mRNAs. ..
Dukare S, Klempnauer K. A conserved patch of hydrophobic amino acids modulates Myb activity by mediating protein-protein interactions. Biochim Biophys Acta. 2016;1859:914-21 pubmed publisher
Uttarkar S, Piontek T, Dukare S, Schomburg C, Schlenke P, Berdel W, et al
. Small-Molecule Disruption of the Myb/p300 Cooperation Targets Acute Myeloid Leukemia Cells. Mol Cancer Ther. 2016;15:2905-2915 pubmed
..Mol Cancer Ther; 15(12); 2905-15. Â©2016 AACR. ..
Jakobs A, Steinmann S, Henrich S, Schmidt T, Klempnauer K. Helenalin Acetate, a Natural Sesquiterpene Lactone with Anti-inflammatory and Anti-cancer Activity, Disrupts the Cooperation of CCAAT Box/Enhancer-binding Protein ? (C/EBP?) and Co-activator p300. J Biol Chem. 2016;291:26098-26108 pubmed
..Its selectivity for the LAP* isoform also makes helenalin acetate an interesting tool to dissect the functions of the LAP* and LAP isoforms. ..
Uttarkar S, Frampton J, Klempnauer K. Targeting the transcription factor Myb by small-molecule inhibitors. Exp Hematol. 2017;47:31-35 pubmed publisher
..Characterization of these compounds suggests disruption of the protein-protein-interaction of Myb and the coactivator p300 as a suitable strategy to inhibit Myb. ..
Falkenberg K, Jakobs A, Matern J, Dörner W, Uttarkar S, Trentmann A, et al
. Withaferin A, a natural compound with anti-tumor activity, is a potent inhibitor of transcription factor C/EBP?. Biochim Biophys Acta Mol Cell Res. 2017;1864:1349-1358 pubmed publisher
..The finding that WFA is a potent inhibitor of C/EBP? suggests that inhibition of C/EBP? might contribute to the biological activities of WFA. ..
Fehler O, Singh P, Haas A, Ulrich D, MÃ¼ller J, Ohnheiser J, et al
. An evolutionarily conserved interaction of tumor suppressor protein Pdcd4 with the poly(A)-binding protein contributes to translation suppression by Pdcd4. Nucleic Acids Res. 2014;42:11107-18 pubmed publisher
..Overall, our work identifies PABP as a novel functionally relevant Pdcd4 interaction partner that contributes to the regulation of translation by Pdcd4. ..