2. Academic Validation
  3. A MedChem toolbox for cereblon-directed PROTACs

A MedChem toolbox for cereblon-directed PROTACs

  • Medchemcomm. 2019 May 28;10(6):1037-1041. doi: 10.1039/c9md00185a.
Christian Steinebach 1,  Izidor Sosič 2,  Stefanie Lindner 3,  Aleša Bricelj 2,  Franziska Kohl 1,  Yuen Lam Dora Ng 3,  Marius Monschke 4,  Karl G Wagner 4,  Jan Krönke 3,  Michael Gütschow 1
Affiliations

Affiliations

  • 1 Pharmaceutical Institute , Pharmaceutical Chemistry I , University of Bonn , An der Immenburg 4 , 53121 Bonn , Germany . Email: guetschow@uni-bonn.de.
  • 2 Faculty of Pharmacy , University of Ljubljana , 1000 Ljubljana , Slovenia.
  • 3 Department of Internal Medicine III , University Hospital Ulm , Albert-Einstein-Allee 23 , 89081 Ulm , Germany.
  • 4 Pharmaceutical Institute , Pharmaceutical Technology , University of Bonn , Gerhard-Domagk-Straße 3 , 53121 Bonn , Germany.
PMID: 31304001 DOI: 10.1039/c9md00185a
Abstract

A modular chemistry toolbox was developed for cereblon-directed PROTACs. A variety of linkers was attached to a CRBN ligand via the 4-amino position of pomalidomide. We used linkers of different constitution to modulate physicochemical properties. We equipped one terminus of the linker with a set of functional groups, e.g. protected amines, protected carboxylic acids, alkynes, chloroalkanes, and protected alcohols, all of which are considered to be attractive for PROTAC design. We also highlight different opportunities for the expansion of the medicinal chemists' PROTAC toolbox towards heterobifunctional molecules, e.g. with biotin, fluorescent, hydrophobic and peptide tags.

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