Highly Efficient and Selective Inhibitors Targeting BET Bromodomains
Herausforderung
BET proteins are important because they regulate both normal transcription processes as well as the transcription of oncogenes such as c-myc and Bcl-2 in various types of cancer. An efficient and selective inhibition of the BET proteins is therefore of great importance for cancer therapies. Various compounds, including benzenesulfonamide derivates are known to possess this property. However, there is a great desire for further, more selective inhibitors.
Lösung
The use of sulfoximine, sulfondiimide and sulfonimidamide derivatives allows to generate novel molecules with a stereogenic sulfur atom. The utilization of this chirality provides new, highly effective and selective BET inhibitors.
Vorteile
Novel BET inhibitors bearing a stereocenter
Chirality is the key to high efficacy and selectivity
Status
International patent application pending and German patent application pending
Proof of concept and ongoing research
RWTH Aachen University is looking for partners for patent exploitation.
Weitere Informationen
Chiral Analogues of PFI-1 as BET Inhibitors and Their Functional Role in Myeloid Maligncies B. Altenburg, M. Frings, J.-H. Schöbel, J. Goßen, K. Pannen, K. Vanderliek, G. Rossetti, S. Koschmieder, N. Chatain, C. Bolm, ACS Med. Chem. Lett.2020, here.
