Literature DB >> 8796285

Synthetic inhibitors of human tissue kallikrein.

D M Evans1, D M Jones, G R Pitt, D Ashworth, F De Clerck, F Verheyen, M Szelke.   

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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Year:  1996        PMID: 8796285     DOI: 10.1016/0162-3109(95)00069-0

Source DB:  PubMed          Journal:  Immunopharmacology        ISSN: 0162-3109


  7 in total

Review 1.  Unleashing the therapeutic potential of human kallikrein-related serine proteases.

Authors:  Ioannis Prassas; Azza Eissa; Gennadiy Poda; Eleftherios P Diamandis
Journal:  Nat Rev Drug Discov       Date:  2015-02-20       Impact factor: 84.694

2.  A synthetic tissue kallikrein inhibitor suppresses cancer cell invasiveness.

Authors:  W C Wolf; D M Evans; L Chao; J Chao
Journal:  Am J Pathol       Date:  2001-11       Impact factor: 4.307

3.  Involvement of tissue kallikrein but not plasma kallikrein in the development of symptoms mediated by endogenous kinins in acute pancreatitis in rats.

Authors:  Thomas Griesbacher; Irmgard Rainer; Beate Tiran; D Michael Evans
Journal:  Br J Pharmacol       Date:  2002-11       Impact factor: 8.739

4.  Neutrophils and the kallikrein-kinin system in proteinase-activated receptor 4-mediated inflammation in rodents.

Authors:  Steeve Houle; Martin D Papez; Mara Ferazzini; Morley D Hollenberg; Nathalie Vergnolle
Journal:  Br J Pharmacol       Date:  2005-11       Impact factor: 8.739

5.  Kallikrein inhibitors limit kinin B(2) antagonist-induced progression of oedematous to haemorrhagic pancreatitis in rats.

Authors:  T Griesbacher; I Rainer; B Tiran; B A Peskar
Journal:  Br J Pharmacol       Date:  2008-08-11       Impact factor: 8.739

Review 6.  Natural and synthetic inhibitors of kallikrein-related peptidases (KLKs).

Authors:  Peter Goettig; Viktor Magdolen; Hans Brandstetter
Journal:  Biochimie       Date:  2010-07-06       Impact factor: 4.079

Review 7.  Hyperresponsiveness in the human nasal airway: new targets for the treatment of allergic airway disease.

Authors:  P J Turner; J C Foreman
Journal:  Mediators Inflamm       Date:  1999       Impact factor: 4.711

  7 in total

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