1252973-63-9Relevant academic research and scientific papers
Optimization of a series of dipeptides with a P3 threonine residue as non-covalent inhibitors of the chymotrypsin-like activity of the human 20S proteasome
Blackburn, Christopher,Barrett, Cynthia,Blank, Jonathan L.,Bruzzese, Frank J.,Bump, Nancy,Dick, Lawrence R.,Fleming, Paul,Garcia, Khristofer,Hales, Paul,Hu, Zhigen,Jones, Matthew,Liu, Jane X.,Sappal, Darshan S.,Sintchak, Michael D.,Tsu, Christopher,Gigstad, Kenneth M.
scheme or table, p. 6581 - 6586 (2011/02/23)
Starting from a tripeptide screening hit, a series of dipeptide inhibitors of the proteasome with Thr as the P3 residue has been optimized with the aid of crystal structures in complex with the β-5/6 active site of y20S. Derivative 25, (β5 IC50
