Targeting the deubiquitinase USP7 for degradation with PROTACs

• DOI: 10.1039/d2cc02094g
• Publication Date: 2022-07-13T06:41:06Z
• Authors: Arunima Murgai; Izidor Sosič; Martina Gobec; Patricia Lemnitzer; Matic Proj; Sophie Wittenburg; Rabea Voget; Michael Gütschow; Jan Krönke; Christian Steinebach
• Keywords: deubikvitinacijski encimi, terapevtski pristop; 0301 basic medicine; Apoptosis; 3. Good health; Ubiquitin-Specific Peptidase 7; 03 medical and health sciences; Rak (medicina); Neoplasms; Humans; Intercellular Signaling Peptides and Proteins; Terapevtska uporaba.; Farmakologija.; info:eu-repo/classification/udc/615

A novel class of USP7 PROTACs were designed and synthesized. CST967, a CRBN-based degrader, showed potent and selective depletion of USP7 leading to apoptosis in multiple cancer lines.