[Thrombin induced tumour growth - pharmacological control].
The central enzyme of blood coagulation, the serine proteinase thrombin, is capable to modify the growth of tumour cells by interaction with protease activated receptors 1 and 4 of the tumour cells. Thrombin is permanently available in tumour micro environment; meizothrombin is generated from prothrombin at a tumour specific activation complex and can influence tumour cell growth via PAR-1 and 7-transdomain protein receptor signalling pathway, too. PEG-coupled direct thrombin inhibitors that possess special pharmacokinetic characteristics and that have been designed for long lasting efficacy in extracellular space, control serine proteinase activity in tumour micro environment and therefore they own a high potential anti-tumour efficacy. In xenographic tumour models this new substance class has shown a significant carcinostatic effect.
Nowak
G
G
AG Pharmakologische Hämostaseologie, Medizinische Fakultät, Friedrich-Schiller-Universität Jena, Drackendorfer Str. 1, 07747 Jena.
Lopez
M
M
Zieger
M
M
D000595:Amino Acid Sequence; D002455:Cell Division / Q000187:drug effects*; D006629:Hirudins / Q000494:pharmacology; D006801:Humans; D008958:Models, Molecular; D008969:Molecular Sequence Data; D009369:Neoplasms / Q000473:pathology*; D011487:Protein Conformation; D044463:Receptor, PAR-1 / Q000502:physiology; D018179:Receptors, Thrombin / Q000737:chemistry / Q000502:physiology*; D015398:Signal Transduction; D013917:Thrombin / Q000009:adverse effects*
D006629:Hirudins; D044463:Receptor, PAR-1; D018179:Receptors, Thrombin; D013917:Thrombin