Pharmacopeia Drug Discovery, Inc.

Douglas Auld

John J Baldwin

Robert A Horlick

Maria Webb

Robert Swanson

Barbara Strohl

Jiuquao Zhao

Xiao Ge Chen

A method for determining the level of kinase activity or phosphatase activity in a sample without the use of antibodies or radioactive labels is disclosed. The method employs a fluorescently-labeled phosphorylatable reporter peptide that is capable of being cleaved by a protease only when the peptide is in an unphosphorylated state. A change in fluorescence characteristics is an indication that the peptide is cleaved and, therefore, in an unphosphorylated state. Thus, the level of protease cleavage, as measured by the fluorescence change, provides a direct measure of phosphatase activity whereas the level of kinase activity is inversely proportion to the level of protease cleavage. The method is particularly well suited to high throughput screening, for example, for screening compounds which modulate kinase or phosphatase activity.

Methods for measuring phosphatase activity

Methods for identifying modulators of receptor activity using orthologues of human receptors are described. Additionally, a method for identifying an animal model useful in the screening of potential therapeutic agents is provided. The genes for bradykinin Breceptors from five mammalian species, vervet monkey, rhesus macaque, tree shrew, dog and pig, as well as the genes for CXCR2 receptors from chimpanzee, gorilla, orangutan, rhesus, vervet and baboon have been cloned and characterized and are described herein.

Orthologues of human receptors and methods of use

Methods for measuring kinase activity

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Cranbury, NJ, United States of America

Douglas Auld