title: Total synthesis of grassystatin A, a probe for cathepsin E function.
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.
authors: School of Pharmacy, Fudan University, Shanghai 201203, China.
authors: Siming
authors: S
authors: Yang
authors: Wei
authors: W
authors: Zhang
authors: Ning
authors: N
authors: Ding
authors: Jeannette
authors: J
authors: Lo
authors: Yanxia
authors: Y
authors: Liu
authors: Michael J
authors: MJ
authors: Clare-Salzler
authors: Hendrik
authors: H
authors: Luesch
authors: Yingxia
authors: Y
authors: Li
mesh_terms: D000818:Animals; D020059:Cathepsin E / Q000037:antagonists & inhibitors* / Q000378:metabolism; D004305:Dose-Response Relationship, Drug; D005260:Female; D008297:Male; D051379:Mice; D008822:Mice, Transgenic; D015394:Molecular Structure; D010455:Peptides / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D011480:Protease Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D010455:Peptides; D011480:Protease Inhibitors; C576631:grassystatin A; D020059:Cathepsin E