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10.1002/cbic.201300762

http://scihub22266oqcxt.onion/10.1002/cbic.201300762
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C4050061!4050061!24591193
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suck abstract from ncbi


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pmid24591193      Chembiochem 2014 ; 15 (6): 799-804
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  • Grassypeptolides As Natural Inhibitors of Dipeptidyl Peptidase 8 and T-Cell Activation #MMPMID24591193
  • Kwan JC; Liu Y; Ratnayake R; Hatano R; Kuribara A; Morimoto C; Ohnuma K; Paul VJ; Ye T; Luesch H
  • Chembiochem 2014[Apr]; 15 (6): 799-804 PMID24591193show ga
  • 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 interest of finding novel protease inhibition activity and selectivity grassypeptolide A (1) was screened against a panel of proteases and found to selectively inhibit DPP8 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 ? both at the active site of DPP8 and at one of the entrances to the internal cavity. Collectively these results suggest that grassypeptolides may be useful tool compounds in the study of DPP8 function.
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