Publication number: 20100021921
Abstract: The present invention relates to isolated polypeptides which comprise a functional kinase domain comprising the amino acid sequence of the native human Abl kinase domain or an essentially similar sequence thereof in which at least one amino acid selected from Met244, Leu248, Gly250, Glu252, Tyr253, Val256, Glu258, Phe311, Ile313, Phe317, Met318, Met351, Glu355, Glu359, Ile360, His361, Leu370, Asp381, Phe382, His396, Ser417, Glu459 and Phe486 is replaced by another amino acid, said mutated functional kinase domain being resistant to inhibition of its tyrosine kinase activity by N-[4-methyl-3-(4-pyridin-3-yl-pyrimidin-2-ylamino)-phenyl]-4-(4-methyl-piperazin-1-ylmethyl)-benzamide or a salt thereof, to the use of such polypeptides to screen for compounds which inhibit the tyrosine kinase activity of such polypeptides, to nucleic acid molecules encoding such polypeptides, to recombinant vectors and host cells comprising such nucleic acid molecules and to the use of such nucleic acid molecules in the production of
Type:
Application
Filed:
August 21, 2009
Publication date:
January 28, 2010
Inventors:
Christophe Barthe, Susan Branford, Amie Corbin, Brian Jay Druker, Justus Duyster, Andreas Hochhaus, Timothy Hughes, Sebastian Kreil, Thibaut Leguay, Francois-Xavier Mahon, Gerald Marit, Martin Muller, Christian Peschel, Claude Preudhomme, Catherine Roche Lestienne, Zbigniew Rudzki
Publication number: 20090117641
Abstract: The present invention relates to isolated polypeptides which comprise a functional kinase domain comprising the amino acid sequence of the native human Abl kinase domain or an essentially similar sequence thereof in which at least one amino acid selected from Met244, Leu248, Gly250, Glu252, Tyr253, Val256, Glu258, Phe311, Ile313, Phe317, Met318, Met351, Glu355, Glu359, Ile360, His361, Leu370, Asp381, Phe382, His396, Ser417, Glu459 and Phe486 is replaced by another amino acid, said mutated functional kinase domain being resistant to inhibition of its tyrosine kinase activity by N-[4-methyl-3-(4-pyridin-3-yl-pyrimidin-2-ylamino)-phenyl]-4-(4-methyl-piperazin-1-ylmethyl)-benzamide or a salt thereof, to the use of such polypeptides to screen for compounds which inhibit the tyrosine kinase activity of such polypeptides, to nucleic acid molecules encoding such polypeptides, to recombinant vectors and host cells comprising such nucleic acid molecules and to the use of such nucleic acid molecules in the production of
Type:
Application
Filed:
June 30, 2008
Publication date:
May 7, 2009
Inventors:
Christophe Barthe, Susan Bradford, Amie Corbin, Brian Jay Druker, Justus Duyster, Andreas Hochhaus, Timothy Hughes, Sebastian Kreil, Thibaut Leguay, Francios-Xavier Mahon, Gerald Marit, Martin Muller, Christian Peschel, Claude Preudhomme, Catherine Roche Lestienne, Zbigniew Rudzki
Publication number: 20050202519
Abstract: The present invention relates to isolated polypeptides which comprise a functional kinase domain comprising the amino acid sequence of the native human Abl kinase domain or an essentially similar sequence thereof in which at least one amino acid selected from Met244, Leu248, Gly250, Glu252, Tyr253, Val256, Glu258, Phe311, Ile313, Phe317, Met318, Met351, Glu355, Glu359, Ile360, His361, Leu370, Asp381, Phe382, His396, Ser417, Glu459 and Phe486 is replaced by another amino acid, said mutated functional kinase domain being resistant to inhibition of its tyrosine kinase activity by N-[4-methyl-3-(4-pyridin-3-yl-pyrimidin-2-ylamino)-phenyl]-4-(4-methyl-piperazin-1-ylmethyl)-benzamide or a salt thereof, to the use of such polypeptides to screen for compounds which inhibit the tyrosine kinase activity of such polypeptides, to nucleic acid molecules encoding such polypeptides, to recombinant vectors and host cells comprising such nucleic acid molecules and to the use of such nucleic acid molecules in the production of
Type:
Application
Filed:
October 4, 2002
Publication date:
September 15, 2005
Inventors:
Christophe Barthe, Susan Branford, Amie Corbin, Brian Druker, Justus Duyster, Andreas Hochhaus, Timothy Hughes, Sebastian Kreil, Thibaut Leguay, Francois-Xavier Mahon, Gerald Marit, Martin Muller, Chriatian Peschel, Claude Preudhomme, Catherine Roche Lestienne, Zbigniew Rudzki