Design, synthesis, and in vitro evaluation of aza-peptide aldehydes and ketones as novel and selective protease inhibitors

• Main Authors: Thomas S. Corrigan (Author), Leilani M. Lotti Diaz (Author), Sarah E. Border (Author), Steven C. Ratigan (Author), Kayla Q. Kasper (Author), Daniel Sojka (Author), Pavla Fajtova (Author), Conor R. Caffrey (Author), Guy S. Salvesen (Author), Craig A. McElroy (Author), Christopher M. Hadad (Author), Özlem Doğan Ekici (Author)
• Format: Book
• Published: Taylor & Francis Group, 2020-01-01T00:00:00Z.
• Subjects: article
• Online Access: Connect to this object online.

Aza-peptide aldehydes and ketones are a new class of reversible protease inhibitors that are specific for the proteasome and clan CD cysteine proteases. We designed and synthesised aza-Leu derivatives that were specific for the chymotrypsin-like active site of the proteasome, aza-Asp derivatives tha...