40290-56-0Relevant articles and documents
Tripeptide analogues of MG132 as protease inhibitors
Pehere, Ashok D.,Nguyen, Steven,Garlick, Sarah K.,Wilson, Danny W.,Hudson, Irene,Sykes, Matthew J.,Morton, James D.,Abell, Andrew D.
supporting information, p. 436 - 441 (2019/01/04)
The 26S proteasome and calpain are linked to a number of important human diseases. Here, we report a series of analogues of the prototypical tripeptide aldehyde inhibitor MG132 that show a unique combination of high activity and selectivity for calpains over proteasome. Tripeptide aldehydes (1–3) with an aromatic P3 substituent show enhanced activity and selectivity against ovine calpain 2 relative to chymotrypsin-like activity of proteasome. Docking studies reveal the key contacts between inhibitors and calpain to confirm the importance of the S3 pocket with respect to selectivity between calpains 1 and 2 and the proteasome.
Chiral Ligands Containing Heteroatoms. 11. Optically Active 2-Hydroxymethyl Piperazines as Catalyst in the Enantioselective Addition of Diethylzinc to Benzaldehyde
Falorni, Massimo,Satta, Michele,Conti, Sandra,Giacomelli, Giampaolo
, p. 2389 - 2398 (2007/10/02)
Starting from enantiomerically pure serine, a series of (2R,5S) and (2S,5S)-2-hydroxymethyl-5-alkyl piperazines 1-5 were prepared in good yields without any racemization.The use of these compounds as chiral catalysts for the enantioselective addition of d