Synthetic inhibitors of human tissue kallikrein

  • Immunopharmacology. 1996 May;32(1-3):117-8. doi: 10.1016/0162-3109(95)00069-0.
D M Evans  1 ,  D M Jones ,  G R Pitt ,  D Ashworth ,  F De Clerck ,  F Verheyen ,  M Szelke
Affiliations
  • 1. Ferring Research Institute, University of Southampton Research Centre, UK.
PMID: 8796285 DOI: 10.1016/0162-3109(95)00069-0
Abstract

We have developed a series of novel, potent low molecular weight (4-600 Da) inhibitors of TK which were stable to cleavage by the enzyme and showed a high degree of selectivity for TK over several Other serine proteases. Compound 7 (CH-2856) was found to reduce eosinophilia in a model of allergic inflammation. The effects observed in vivo provide further evidence for the involvement of TK and kinins in the pathophysiology of allergic diseases such as asthma.

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