TY - JOUR AU - Coman, Anca G.; Paraschivescu, Codruta C.; Hadade, Niculina D.; Juncu, Andrei; Vlaicu, Ovidiu; Popescu, Costin-Ioan; Matache, Mihaela TI - New Acyloxymethyl Ketones: Useful Probes for Cysteine Protease Profiling SN - 0039-7881 SN - 1437-210X PY - 2016 JO - Synthesis JF - Synthesis LA - EN VL - 48 IS - 22 SP - 3917 EP - 3923 ET - 2016/07/29 DA - 2016/10/27 KW - acyloxymethyl ketones KW - activity-based probes KW - peptidyl-AOMKs KW - 2,6-dimethylbenzoates KW - solid-phase peptide synthesis AB - Peptidyl-acyloxymethyl ketones (AOMKs) belong to a class of selective, irreversible inhibitors (activity-based probes) widely used as chemical tools of investigating proteins, for example, in activity-based protein profiling. The synthesis of the AOMKs has always been challenging and current methodologies involve both solution and solid-phase synthesis. Herein, the synthesis of a new scaffold useful for the preparation of peptidyl-AOMKs is reported and it is demonstrated that the new synthetic probes bearing a 4-functionalized 2,6-dimethylbenzoate efficiently inhibit cysteine proteases like cathepsin B. PB - © Georg Thieme Verlag DO - 10.1055/s-0035-1562781 UR - http://www.thieme-connect.com/products/ejournals/abstract/10.1055/s-0035-1562781 ER -