6 research outputs found
Immobilized bivalent inhibitors as tools for the affinity-based isolation of human mast cell tryptases
No full textPrimed-site probing of papain-like cysteine proteases
No full textPfizer JM, Assfalg-Machleidt I, Machleidt W, Moroder L, Schaschke N. Primed-site probing of papain-like cysteine proteases. INTERNATIONAL JOURNAL OF PEPTIDE RESEARCH AND THERAPEUTICS. 2007;13(1-2):93-104
Molecular modeling: A search for a calpain inhibitor as a new treatment for cataractogenesis
No full textStudies of 17 analoges of 3 (SJA6017) in an in silico calpain model are reconciled to measured IC(50) values against ovine calpain. The studies validate the potential of the "model" and criteria established for inhibition as a tool to select structures for synthesis to test as calpain inhibitors. Using this screening methodology of virtual libraries led us to synthesize several inhibitors including macrocycle 33, which in vitro sheep eye lens culture experiments showed to substantially slow opacification.Blair G Stuart, James M. Coxon, James D. Morton, Andrew D. Abell, D. Quentin McDonald, Steven G. Aitken, Matthew A. Jones and Roy Bickerstaff
