Sugen Incorporated

Yissum Research Development Company of the Hebrew University of Jerusalem Ltd.

Other

Jianming Tsai

Klaus Peter Hirth

Peng Cho Tang

Aviv Gazit

Laura Kay Shawver

Elaina Mann

Hui Chen

Alexander Levitzki

Harald App

The present invention concerns compounds and their use to inhibit the activity of a receptor tyrosine kinase. The invention is preferably used to treat cell proliferative disorders such as cancers characterized by over-activity or inappropriate activity HER2 or EGFR.

Method and compositions for inhibiting cell proliferative disorders

Methods and compositions for inhibiting cell proliferative disorders

The present invention concerns compounds and their use to inhibit the activity of a receptor tyrosine kinase. The invention is preferably used to treat cell proliferative disorders such as cancers charcterized by over-activity or inappropriate activity HER2 or EGFR.

The invention is directed to rapid and quantitative assay systems for screening test compounds for their ability to modulate tyrosine kinase or phosphatase activities involved in signal transduction by determining the tyrosine phosphorylation state of a protein substrate using an anti-phosphotyrosine antibody and an antibody specific for the protein substrate. These assays may be practiced in a whole cell or cell-free system. The assays can be used to identify test compounds for use in therapeutic applications to disease processes in which tyrosine kinase or phosphatase activity in a signal transduction pathway contributes to a pathological process.

Screening assays for compounds

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Jianming Tsai