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Keryx patents gene-based drug discovery involving kinase targeted compounds.

Keryx Biopharmaceuticals, Inc. (Jerusalem, Israel; 972 2541 2700) announced that the United States Patent and Trademark Office has granted patent 6,174,993, a critical patent related to drug discovery for an important family of kinases implicated in diseases such as cancer, diabetes, obesity, and autoimmune disorders. The new patent is owned jointly by Children's Hospital of Boston (Boston, MA) and The Hebrew University of Jerusalem (Jerusalem, Israel), and licensed exclusively to Keryx.

Kinases are essential for the body's intracellular signaling and other vital functions. The patent describes the recent discovery of a small area within a certain class of kinases that is highly specific to each% kinase. Details of this region are critical for the design of compounds that specifically target the kinase and form an essential part of Keryx's KinAce bioinformatics technology platform that utilizes sequence based genomics data for drug discovery.

Kinases, which play a key role in cell signaling, have emerged as one of the most promising classes of drug discovery targets for pharmaceutical and biotechnology companies. The technology of this patent , the first of several related to our core KinAce platform, provides a direct pathway from gene sequence data to potential drug candidates-an approach that we believe represents a new and extraordinarily efficient paradigm for drug discovery," said Morris Laster, MD, Chairman and Chief Executive Officer of Keryx "With the pending completion. of the draft of the human genome, the number of kinase targets is likely to increase."

"At Keryx, we have applied the technology of this patent and several pending applications to identify a number of promising early leads in hormone resistant prostate cancer, diabetes, obesity, fibrotic disorders, and autoimmune diseases," added Benjamin Corn, MD, President of Keryx . "In addition, the ability of our KinAce platform to rapidly generate specific kinase modulators provides a new and powerful tool for investigating kinase functional genomics."

Kinases are proteins that play a key role in the way cells communicate-a process known as signal transduction. If this communication is compromised, various disease states may result. Kinases regulate a variety of essential cellular events-such as the ability of cells to enter and/or complete mitosis (division), cellular proliferation, cellular differentiation, the control of fat metabolism, immune responses, inflammatory response and the control of glycogen metabolism. Therefore, compounds that have the ability to up and/or down regulate the activity of kinases have enormous potential for the treatment of many major diseases, such as cancer, obesity, autoimmune disorders, and diabetes. However, as kinases share very similar structures, identifying compounds that target specific kinases without interfering with the activity of others is a key challenge to kinase-based drug discovery.

The patent, which focuses on one of the most important classes of kinases called serine threonine kinases, is based on the discovery that short sequences (six to ten amino acids in length) derived from a specific region of serine threonine kinases sequences can be used to selectively modulate the activity of a kinase. The regions are distinct for each kinase, providing a basis for the discovery of highly specific modulators.

In addition to advancing its KinAce drug discovery technology, Keryx is developing KRX-101 (sulodexide), an in-licensed product that is in late stage clinical development for diabetic nephropathy. The company recently announced that it has secured a United States patent for the use of KRX-101 in the treatment of diabetic retinopathy, an eye-related complication of diabetes.

Keryx is building a pipeline of drug candidates that target protein kinases by applying its proprietary bioinformatics technology to genomics data. Kinases, which play a key role in the way cells communicate, are implicated in a wide range of diseases.
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Comment:Keryx patents gene-based drug discovery involving kinase targeted compounds.
Publication:BIOTECH Patent News
Geographic Code:7ISRA
Date:Feb 1, 2001
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