660847-45-0Relevant articles and documents
Optimization of subsite binding to the β5 subunit of the human 20S proteasome using vinyl sulfones and 2-keto-1,3,4-oxadiazoles: Syntheses and cellular properties of potent, selective proteasome inhibitors
Rydzewski, Robert M.,Burrill, Leland,Mendonca, Rohan,Palmer, James T.,Rice, Mark,Tahilramani, Ram,Bass, Kathryn E.,Leung, Ling,Gjerstad, Erik,Janc, James W.,Pan, Lin
, p. 2953 - 2968 (2007/10/03)
Beginning with the peptide sequence Cbz-Ile-Glu(OtBu)-Ala-Leu found in PSI (3), a series of vinyl sulfones (VS) were synthesized for evaluation as inhibitors of the chymotrypsin-like activity of the 20S proteasome. Variations at the key P3 position confir