Christiane Göllner
Christiane Göllner
Tel. ++49 345 55 25169
e-mail: christiane.goellner(at)pharmazie.uni-halle.de
Neo synthesis of glycolipid inhibitors of Myt1 kinase and structure-activity relationships of novell kinase inhibitors as suggestive extension to conventional chemotherapy and to overcome resistance
The enzyme Myt1 kinase is an impotant regulator of cdc2/cyclin B kinase activity. The inhibitory phosphorylation of cdc2 is important for the timing of entry into mitosis. Various studies have shown that premature activation of cdc2 leads to mitotic catastrophe and cell death. Inhibition of Myt1 kinase is predicted to cause premature activation of cdc2. Therefore inhibitors of Myt1 kinase can kill rapidly proliferating cells and interfere cell cycle checkpoints. Such inhibitors could be a suggestive extension to conventional chemotherapy and to overcome resistance.
As result of a systematic search for potential anti-cancer agents from plants and marine organisms two bioactive glycoglycerolipids were isolated from a marine alga extract. The compounds show in a bioassay a higher activity against the enzyme Myt1 kinase than staurosporin as positive control.
Aim of our research is the neo-synthesis of these natural products, the systematical variation
of molecule domains and structure-activity relationships.
Publications
C. Göllner, C. Philipp, B. Dobner, W. Sippl and M. Schmidt
First total synthesis of 1,2-dipalmitoyl-3-(N-palmitoyl-6-deoxy-6-amino-a-D-glucosyl)glycerol – a glycoglycerolipid of a marine alga with a high inhibitor activity against human Myt1-kinase
Carbohydr Res. 2009, 344(13), 1628-1631
Poster Abstracts
C. Göllner, C. Philipp, B. Dobner, W. Sippl, M. Schmidt.
New glycoglycerolipid-derivatives as potential lead structures for Myt1 kinase inhibitors
Jahrestagung der Deutschen Pharmazeutischen Gesellschaft.
Jena, 29.09. - 01.10. 2009.
C. Philipp, C. Göllner, H.H. Rüttinger, W. Sippl, M. Pietzsch, M. Schmidt.
Generation of Myt1 kinase and development of Myt1 kinase bioassays
Jahrestagung der Deutschen Pharmazeutischen Gesellschaft.
Jena, 29.09. - 01.10. 2009.
C. Göllner, C. Philipp, B. Dobner, W. Sippl, M. Schmidt
Neosynthese marinerGlycoglycerolipideund neuartiger Derivate als potentielle Inhibitoren der Myt1 Kinase
DPhG Jahrestagung Bonn,
06.10-08.10. 2008
C. Philipp, C. Göllner, W. Sippl, M. Schmidt
Entwicklung und Vergleich biochemischer Assays zur Bestimmung der Aktivität potentieller Myt1 Kinaseinhibitoren
DPhG Jahrestagung Bonn,
06.10-08.10. 2008