Abdallah Alfayomy
Abdallah Alfayomy
Tel. ++49 345 55 25188
e-mail: Abdallah_alfayomy(at)pharmazie.uni-halle.de
Design and synthesis of novel PROTACs for different protein kinases
Targeted protein degradation in cells by chemical compounds is seen as one of the emerging techniques to establish alternatives to classical small molecule-based inhibition. Chemically induced protein degradation can serve as a biological tool and also offers new opportunities for drug discovery. One series of compounds that has been established for protein degradation are the so-called PROTACs. These compounds are heterobifunctional molecules consisting of three parts: an E3 ligase ligand, a binder for the target protein of interest (POI) and a linker that connects them. The E3 ligase ligand of PROTACs hijacks the ubiquitin-proteasome system, and brings the E3 ligase into spatial proximity to the target protein to degrade it. In the current project we are focusssing on the development and biological characterization of different type of protein degraders for some protein kinases.
Publications:
A. M. Alfayomy, R. Ashry, A. Kansy, F. Erdmann, M. Schmidt, O. H. Krämer, W. Sippl. Design, synthesis, and biological characterization of proteolysis targeting chimera (PROTACs) for the Ataxia telangiectasia and RAD3-related (ATR) kinase. Eur J Med Chem. 2024 Jan 29;267:116167. doi:10.1016/j.ejmech.2024.116167.