646532-83-4Relevant articles and documents
Design, synthesis, and in vitro evaluation of aza-peptide aldehydes and ketones as novel and selective protease inhibitors
Border, Sarah E.,Caffrey, Conor R.,Corrigan, Thomas S.,Do?an Ekici, ?zlem,Fajtova, Pavla,Hadad, Christopher M.,Kasper, Kayla Q.,Lotti Diaz, Leilani M.,McElroy, Craig A.,Ratigan, Steven C.,Salvesen, Guy S.,Sojka, Daniel
, p. 1387 - 1402 (2020/07/13)
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 si
Aza-peptide epoxides: A new class of inhibitors selective for clan CD cysteine proteases
Asgian, Juliana L.,James, Karen Ellis,Li, Zhao Zhao,Carter, Wendy,Barrett, Alan J.,Mikolajczyk, Jowita,Salvesen, Guy S.,Powers, James C.
, p. 4958 - 4960 (2007/10/03)
Aza-peptide epoxides, a new class of irreversible protease inhibitors, are specific for the clan CD cysteine proteases. The inhibitors have second-order rate constants up to 105 M-1 s-1, with the most potent epoxides having the S,S stereochemistry. The aza-Asn derivatives are effective legumain inhibitors, while the aza-Asp epoxides were specific for caspases. The inhibitors have little or no inhibition with other proteases such as chymotrypsin, papain, or cathepsin B.
