New Acyloxymethyl Ketones: Useful Probes for Cysteine Protease Profiling.

Autor: Coman, Anca G., Paraschivescu, Codruta C., Hadade, Niculina D., Juncu, Andrei, Vlaicu, Ovidiu, Popescu, Costin-Ioan, Matache, Mihaela
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Zdroj: Synthesis; 2016, Vol. 48 Issue 22, p3917-3923, 7p
Abstrakt: 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. [ABSTRACT FROM AUTHOR]
Databáze: Complementary Index