Trifluoromethyl ketones and methyl fluorophosphonates as inhibitors of group IV and VI phospholipases A(2): structure-function studies with vesicle, micelle, and membrane assays.

@article{Ghomashchi1999TrifluoromethylKA,
  title={Trifluoromethyl ketones and methyl fluorophosphonates as inhibitors of group IV and VI phospholipases A(2): structure-function studies with vesicle, micelle, and membrane assays.},
  author={Farideh Ghomashchi and Richard Loo and Jes{\"u}s Balsinde and Fulvia B{\'a}rtoli and Rafael Apitz-Castro and J. Derrell Clark and Edward A. Dennis and Michael H Gelb},
  journal={Biochimica et biophysica acta},
  year={1999},
  volume={1420 1-2},
  pages={45-56}
}
A series of fatty alkyl trifluoromethyl ketones and methyl fluorophosphonates have been prepared and tested as inhibitors and inactivators of human groups IV and VI phospholipases A(2) (cPLA(2) and iPLA(2)). Compounds were analyzed with phospholipid vesicle-, detergent-phospholipid mixed-micelle-, and natural membrane-based assays, and, with few exceptions, the relative inhibitor potencies measured with the three assays were similar. Ph(CH(2))(4)COCF(3) and Ph(CH(2))(4)PO(OMe)F emerged as a… CONTINUE READING
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