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The Importance of Correct Protein Concentration for Kinetics and Affinity Determination in Structure-function Analysis
Published on: March 17, 2010
Total synthesis of grassystatin A, a probe for cathepsin E function
Siming Yang1, Wei Zhang, Ning Ding
1School of Pharmacy, Fudan University, Shanghai 201203, China.
Bioorganic & Medicinal Chemistry
|July 4, 2012
Abstract:
The linear depsipeptide grassystatin A, a valuable probe for the study of cathepsin E function, has been synthesized by a [4+6] strategy. It exhibited specific inhibitory activity against cathepsin E with an IC(50) value of 0.8 nM. Our studies indicated that inhibition of cathepsin E did not have an impact on ovalbumin antigen processing and peptide presentation, unique from studies of other aspartic protease inhibitors.
