869494-32-6Relevant academic research and scientific papers
Efficient Entropy-Driven Inhibition of Dipeptidyl Peptidase III by Hydroxyethylene Transition-State Peptidomimetics
Breinbauer, Rolf,Gruber, Karl,Ivkovic, Jakov,Jha, Shalinee,Kumar, Prashant,Lembacher-Fadum, Christian,Macheroux, Peter,Puschnig, Johannes,Reithofer, Viktoria
, p. 14108 - 14120 (2021)
Dipeptidyl peptidase III (DPP3) is a ubiquitously expressed Zn-dependent protease, which plays an important role in regulating endogenous peptide hormones, such as enkephalins or angiotensins. In previous biophysical studies, it could be shown that substr
Design and synthesis of peptidomimetic severe acute respiratory syndrome chymotrypsin-like protease inhibitors
Ghosh, Arun K.,Xi, Kai,Ratia, Kiira,Santarsiero, Bernard D.,Fu, Wentao,Harcourt, Brian H.,Rota, Paul A.,Baker, Susan C.,Johnson, Michael E.,Mesecar, Andrew D.
, p. 6767 - 6771 (2007/10/03)
Design, synthesis, and biological evaluation of peptidomimetic severe acute respiratory syndrome chymotrypsin-like protease (SARS-3CLpro) inhibitors for severe acute respiratory syndrome coronavirus (SARS-CoV) are described. These inhibitors exhibited antiviral activity against SARS-CoV in infected cells in the micromolar range. An X-ray crystal structure of our lead inhibitor (4) bound to SARS-3CLpro provided important drug-design templates for the design of small-molecule inhibitors.
