Fluorescent probes for use in protein kinase inhibitor...

Organic compounds -- part of the class 532-570 series – Organic compounds – Nitrogen attached directly or indirectly to the purine ring...

Reexamination Certificate

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Details

C544S230000, C514S275000, C252S301160

Reexamination Certificate

active

07125996

ABSTRACT:
The invention provides methods relating to a novel screening assay format that can be applied to broad members of the protein kinase gene family. The assay uses a series of labeled, active site probes described herein that can be displaced by an inhibitor agent. The Kdfor the inhibitor compound is derived based on the Kdof the probe for the kinase and the dose response of the inhibitor agent. The invention also provides active site probes suitable for use with the screening method.

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patent: WO 03/031606 (2003-04-01), None
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A. Janoshazi, et al. “Rapid in Vitro Conformational Changes of the Catalytic Site of PKCalpha Assessed by FIM-1 Fluorescence” Biochemistry 1999, 38, 13316-13327 XP 002317136.
H. Vankayalapati, et al. “Targeting Aurora2 Kinase in Oncogenesis: A Structural Bioinformatics Approach to Target Validation and Rational Drug Design” Molecular Cancer Therapeutics 2003, 2, 283-294 XP002317137.

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