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Vertex receives patent for drug discovery targeting kinase gene family.

Vertex Pharmaceuticals, Inc. (Cambridge, MA; 617-577-6614) announced that it has been granted United States Patent 6,162,613 from the United States Patent and Trademark Office, for method of designing novel chemical inhibitors of protein kinases. The method involves using mutagenesis techniques to create hybrid kinases that act as surrogate targets for drug design and compound screening. This method, which combines the disciplines of cell biology, structural genomics, computational chemistry and medicinal chemistry, may accelerate the design and development

of new drug candidates by reducing lead discovery and optimization timelines.

"This invention provides versatile intellectual property around a family of targets of high interest to Vertex, and also protects, we believe, a unique and advantageous method of drug discovery," said Vicki L. Sato, Ph.D, President of Vertex. "The kinase gene family contains numerous promising targets for small molecule drug design, and we are excited about the potential for this new process to help drive productivity in our kinase inhibitor research program."

Kinases are enzymes that play a key role in transmitting signals between and within cells, and drive a wide variety of important cellular functions and responses. Kinases exert their effect by phosphorylating other proteins, which then become activated and perform a specific function. There are more than 500 known kinases in the kinase protein family. Kinases are implicated in most major diseases, including cancer, autoimmune and inflammatory disease, cardiovascular disease, metabolic disease and neurological disease, and are widely considered to be ideal targets for intervention with small molecule drugs.

In May 2000, Vertex entered into a collaboration with Novartis which will provide Vertex with up to $800 million in pre-commercial payments for the discovery, development, and commercialization of up to eight kinase inhibitors. Vertex is also independently and with other partners developing drugs for selected kinase targets, including p38 MAP kinase inhibitors for the treatment of inflammation with Kissei Pharmaceutical Co., Ltd. of Japan.

United States Patent 6,162,613, titled "Methods for designing inhibitors of serine/threonine and tyrosine kinases," describes a method for creating novel, potent chemical classes of inhibitors for a given kinase target. This method involves the creation of a hybrid kinase by making one or more genetic substitutions in the ATP-binding site of a well-characterized kinase, in order to mimic the atomic-level topography of a kinase of interest. The design of inhibitors directed at the hybrid kinase can effectively create proprietary compound classes that potently inhibit the kinase of interest, and the activity of the novel compounds can be confirmed without the need for directly screening compounds against the wild-type kinase of interest. Three- dimensional structural determination of the hybrid kinase, either alone or in complex with inhibitors, can be used as a further basis for design of novel compound classes.

In addition to potentially accelerating drug discovery, the technology underlying this invention provides researchers with a compound screening platform whereby hybrid kinases can be used as surrogate targets for any protein kinase targets that may be the subject of drug design efforts. The technological approach described in this patent provides for both structural analysis of enzyme-inibitor complexes and automated in vitro screening using mutant kinases.

The inventors of the patent are Drs. Michael S. Su, Edward Fox, Keith P. Wilson and Ursula Germann, all of Vertex.

Vertex is pioneering the field of chemogenomics, which represents a union of medicinal chemistry and molecular biology. Medicinal chemistry is dedicated to identifying compounds that are useful in the treatment of disease. Genomics seeks to determine the identity and function of all genes in an organism. By taking advantage of drug discovery approaches and technologies that can describe the interactions a drug must have with a given target molecule, the aim of the field of chemogenomics is to describe many or all possible drugs for a drug target or group of drug targets.

As part of its drug discovery efforts to date in the kinase protein family, Vertex has determined the three-dimensional atomic structure of numerous novel kinases and kinase/inhibitor co-complexes. Vertex has also identified the physiological role of specific kinases using gene-targeting approaches. Using medicinal, computational, and combinatorial chemistry, Vertex has generated lead classes of kinase inhibitors, and has patents issued or filed related to certain classes of kinase inhibitors, and methods for discovering kinase inhibitors using Vertex's proprietary technologies.
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Title Annotation:Vertex Pharmaceuticals Inc.
Comment:Vertex receives patent for drug discovery targeting kinase gene family.(Vertex Pharmaceuticals Inc.)
Publication:BIOTECH Patent News
Article Type:Brief Article
Geographic Code:1USA
Date:Jan 1, 2001
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