4.7 Article

Total synthesis of grassystatin A, a probe for cathepsin E function

Journal

BIOORGANIC & MEDICINAL CHEMISTRY
Volume 20, Issue 15, Pages 4774-4780

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2012.05.077

Keywords

Total synthesis; Grassystatin A; Cathepsin E inhibitor; Antigen processing and presentation

Funding

  1. National Natural Science Foundation of China [81172975]
  2. University of Florida College of Pharmacy

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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 IC50 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. (C) 2012 Elsevier Ltd. All rights reserved.

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