The synthesis of lysylfluoromethanes and their properties as inhibitors of trypsin, plasmin and cathepsin B.

@article{Angliker1987TheSO,
  title={The synthesis of lysylfluoromethanes and their properties as inhibitors of trypsin, plasmin and cathepsin B.},
  author={Herbert Angliker and P O Wikstrom and P Rauber and Elwood R. Shaw},
  journal={The Biochemical journal},
  year={1987},
  volume={241 3},
  pages={871-5}
}
The synthesis of two lysylfluoromethanes is described by an extension of the synthesis method of Rauber, Angliker, Walker & Shaw [(1986) Biochem. J. 239, 633-640]. Ala-Phe-Lys-CH2F was found to be an active-centre-directed inhibitor of plasmin and trypsin, as is the corresponding chloromethane. However, the rate of covalent-bond formation is about an order of magnitude lower at 25 degrees C for the fluoro derivative. It was, in addition, an extremely effective inactivator of cathepsin B at pH 5… CONTINUE READING