Publication


Featured researches published by Haruki Hasegawa.


Analytical Biochemistry | 2003

Development of a high-throughput fluoroimmunoassay for Syk kinase and Syk kinase inhibitors

Noriyuki Yamamoto; Haruki Hasegawa; Hitomi Seki; Karl Ziegelbauer; Takahiro Yasuda

Syk is a tyrosine kinase which is indispensable in immunoglobulin Fc receptor- and B cell receptor-mediated signal transduction in various immune cells. This pathway is important in the pathophysiology of allergy. In this study we established a quantitative nonradioactive kinase assay to identify inhibitors of Syk. We used recombinant GST-tagged Syk purified from baculovirus-infected insect cells. As a substrate, biotinylated peptide corresponding to the activation loop domain of Syk, whose tyrosine residues are autophosphorylated upon activation, was employed to screen both ATP- and substrate-competitive inhibitors. After the kinase reaction in solution phase, substrate was trapped on a streptavidin-coated plate, followed by detection of the phosphorylated tyrosine with europium-labeled anti-phosphotyrosine antibody. The kinase reaction in solution phase greatly enhanced phosphorylation of substrate compared to that of plate-coated substrate. High signal-to-background ratio and low data scattering were obtained in the optimized high-throughput screening (HTS) format. Further, several kinase inhibitors showed concentration-dependent inhibition of recombinant Syk kinase activity with almost the same efficacy for immunoprecipitated Syk from a human cell line. These data suggest that this assay is useful to screen Syk kinase inhibitors in HTS.


Archive | 2004

Beta-amino acid compounds as integrin antagonists

Markus Albers; Thomas Lehmann; Thomas Rölle; Gerhard Müller; Gerhard Hessler; Masaomi Tajimi; Karl Ziegelbauer; Hiromi Okigami; Haruki Hasegawa


Archive | 2001

Piperidyl carboxylic acids as integrin antagonists

Rüdiger Fischer; Thomas Lehmann; Gerhard Müller; Gerhard Hessler; Masaomi Tajimi; Karl Ziegelbauer; Hiromi Okigami; Haruki Hasegawa; Hiroshi Komura; Manami Mizoguchi


Archive | 2001

Cyclic carboxylic acids as integrin antagonists

Thomas Lehmann; Rüdiger Fischer; Markus Albers; Thomas Rölle; Gerhard Müller; Gerhard Hessler; Masaomi Tajimi; Karl Ziegelbauer; Hiromi Okigami; Kevin Bacon; Haruki Hasegawa


Archive | 2002

Succinic acid derivatives

Thomas Rölle; Thomas Lehmann; Markus Albers; Gerhard Müller; Gerhard Hessler; Rüdiger Fischer; Masaomi Tajimi; Karl Ziegelbauer; Kevin Bacon; Haruki Hasegawa; Hiromi Okigami


Archive | 1999

New beta-aminoacid amide derivatives, are integrin antagonists useful for treating inflammatory, autoimmune or immunological disorders e.g. asthma, diabetes or rheumatoid arthritis

Markus Albers; Thomas Lehmann; Thomas Dr. Roelle; Gerhard Mueller; Gerhard Hesler; Masaomi Tajimi; Karl Ziegelbauer; Hiromi Okigami; Haruki Hasegawa


Archive | 2001

Beta-amino acid derivatives as integrin receptor antagonists

Thomas Rölle; Thomas Lehmann; Markus Albers; Gerhard Hessler; Gerhard Müller; Rüdiger Fischer; Masaomi Tajimi; Karl Ziegelbauer; Kevin B. Bacon; Haruki Hasegawa; Hiromi Okigami


Archive | 2002

Para-amino benzoic acids as integrin antagonists

Thomas Lehmann; Markus Albers; Thomas Rölle; Gerhard Hessler; Masaomi Tajimi; Karl Ziegelbauer; Hiromi Okigami; Kevin Bacon; Haruki Hasegawa


Archive | 2006

DERIVADOS DEL ACIDO SUCCINICO.

Thomas Dr. Roelle; Thomas Lehmann; Markus Albers; Gerhard Mueller; Gerhard Hessler; Ruediger Fischer; Masaomi Tajimi; Karl Ziegelbauer; Kevin Bacon; Haruki Hasegawa; Hiromi Okigami


Archive | 2002

Bernsteinsäurederivate Succinic acid derivatives

Thomas Dr. Roelle; Thomas Lehmann; Markus Albers; Gerhard Mueller; Gerhard Hessler; Ruediger Fischer; Masaomi Tajimi; Karl Ziegelbauer; Kevin Bacon; Haruki Hasegawa; Hiromi Okigami

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