1300689-97-7Relevant academic research and scientific papers
Peptido sulfonyl fluorides as new powerful proteasome inhibitors
Brouwer, Arwin J.,Jonker, Anika,Werkhoven, Paul,Kuo, Ethan,Li, Nan,Gallastegui, Nerea,Kemmink, Johan,Florea, Bogdan I.,Groll, Michael,Overkleeft, Herman S.,Liskamp, Rob M. J.
, p. 10995 - 11003 (2013/02/25)
A new class of potent proteasome inhibitors is described, of which the members contain an amino acid inspired sulfonyl fluoride as the electrophilic trap. In total, 24 peptido sulfonyl fluoride inhibitors have been designed and synthesized, which were inspired by the backbone sequences of the proteasome inhibitors bortezomib, epoxomicin, and Cbz-Leu3-aldehyde. Nine of them were very potent proteasome inhibitors, the best of which had an IC 50 of 7 nM. A number of the peptido sulfonyl fluoride inhibitors were found to be highly selective for the β5 proteasome subunit.
Synthesis and biological evaluation of novel irreversible serine protease inhibitors using amino acid based sulfonyl fluorides as an electrophilic trap
Brouwer, Arwin J.,Ceylan, Tarik,Jonker, Anika M.,Linden, Tima Van Der,Liskamp, Rob M.J.
, p. 2397 - 2406 (2011/05/12)
We have designed and synthesized novel irreversible serine protease inhibitors containing aliphatic sulfonyl fluorides as an electrophilic trap. These substituted taurine sulfonyl fluorides derived from taurine or protected amino acids were conveniently s
