889359-41-5Relevant academic research and scientific papers
Development of activity-based probes for trypsin-family serine proteases
Pan, Zhengying,Jeffery, Douglas A.,Chehade, Kareem,Beltman, Jerlyn,Clark, James M.,Grothaus, Paul,Bogyo, Matthew,Baruch, Amos
, p. 2882 - 2885 (2006)
A series of diphenylphosphonate-based probes were developed for the trypsin-like serine proteases. These probes selectively target serine proteases rather than general serine hydrolases that are targets for fluorophosphonate-based probes. This increased s
Phosphonate inhibitors of West Nile virus NS2B/NS3 protease
Skoreński, Marcin,Milewska, Aleksandra,Pyr?, Krzysztof,Sieńczyk, Marcin,Oleksyszyn, Józef
, p. 8 - 14 (2018/11/01)
West Nile virus (WNV) is a member of the flavivirus genus belonging to the Flaviviridae family. The viral serine protease NS2B/NS3 has been considered an attractive target for the development of anti-WNV agents. Although several NS2B/NS3 protease inhibitors have been described so far, most of them are reversible inhibitors. Herein, we present a series of α-aminoalkylphosphonate diphenyl esters and their peptidyl derivatives as potent inhibitors of the NS2B/NS3 protease. The most potent inhibitor identified was Cbz-Lys-Arg-(4-GuPhe)P(OPh)2 displaying Ki and k2/Ki values of 0.4 μM and 28 265 M?1s?1, respectively, with no significant inhibition of trypsin, cathepsin G, and HAT protease.
