Oxyanion-mediated inhibition of serine proteases.

@article{Presnell1998OxyanionmediatedIO,
  title={Oxyanion-mediated inhibition of serine proteases.},
  author={S R Presnell and Girish Sunil Patil and Cameron Mura and Kevin M. Jude and John M. Conley and Jay A. Bertrand and C M Kam and James C. Powers and Loren Dean Williams},
  journal={Biochemistry},
  year={1998},
  volume={37 48},
  pages={17068-81}
}
Novel aryl derivatives of benzamidine were synthesized and tested for their inhibitory potency against bovine trypsin, rat skin tryptase, human recombinant granzyme A, human thrombin, and human plasma kallikrein. All compounds show competitive inhibition against these proteases with Ki values in the micromolar range. X-ray structures were determined to 1.8 A resolution for trypsin complexed with two of the para-substituted benzamidine derivatives, 1-(4-amidinophenyl)-3-(4-chlorophenyl)urea… CONTINUE READING