%0 Journal Article
%T Kinetic Study of Human Full-Length Wild-Type JAK2 and V617F Mutant Proteins
%A Dirk Erdmann
%A Bertrand Allard
%A Jacqueline Bohn
%A Alain De Pover
%A Andreas Floersheimer
%A Patrizia Fontana
%A Marc Gerspacher
%A Jean Christophe Hau
%A Francesco Hofmann
%A Thomas Radimerski
%A Roman Wille
%A Catherine ZimmermannPatrick Ch¨¨ne
%J The Open Enzyme Inhibition Journal
%D 2008
%I 
%R 10.2174/1874940200801010080]
%X The Janus kinase 2 (JAK2) is a drug target in particular because a missense mutation in this gene (V617F) has been identified in various human diseases. We report here the first kinetic study of the human full-length wild type and V617F JAK2 proteins and of their isolated kinase domain. The kinetic parameters of both full-length proteins are similar revealing that the mutation does not affect JAK2 catalytic activity suggesting that it has a more complex role in the regulation of JAK2 activity. Our study also shows that the domains located outside the kinase domain have little influence on JAK2 catalytical activity.
%U http://www.benthamscience.com/open/toeij/articles/V001/80TOEIJ.htm