Please use this identifier to cite or link to this item: http://hdl.handle.net/10397/34502
Title: Grassypeptolides as natural inhibitors of dipeptidyl ppeptidase 8 and T-cell activation
Authors: Kwan, JC
Liu, Y
Ratnayake, R
Hatano, R
Kuribara, A
Morimoto, C
Ohnuma, K
Paul, VJ
Ye, T 
Luesch, H
Keywords: Dipeptidyl peptidases
Grassypeptolides
Immunochemistry
Natural products
Protease inhibition
Issue Date: 2014
Publisher: John Wiley and Sons
Source: ChemBioChem, 2014, v. 15, no. 6, p. 799-804 How to cite?
Journal: ChemBioChem
Abstract: Natural products made by marine cyanobacteria are often highly modified peptides and depsipeptides that have the potential to act as inhibitors for proteases. In the interests of finding new protease inhibition activity and selectivity, grassypeptolide A (1) was screened against a panel of proteases and found to inhibit DPP8 selectively over DPP4. Grassypeptolides were also found to inhibit IL-2 production and proliferation in activated T-cells, consistent with a putative role of DPP8 in the immune system. These effects were also observed in Jurkat cells, and DPP activity in Jurkat cell cytosol was shown to be inhibited by grassypeptolides. In silico docking suggests two possible binding modes of grassypeptolides—at the active site of DPP8 and at one of the entrances to the internal cavity. Collectively these results suggest that grassypeptolides might be useful tool compounds in the study of DPP8 function.
URI: http://hdl.handle.net/10397/34502
ISSN: 1439-4227 (print)
1439-7633 (online)
DOI: 10.1002/cbic.201300762
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