Jan. 16 /PRNewswire/ -- Rigel Pharmaceuticals, Inc. (Nasdaq: RIGL - news) today announced that a new study published in the current issue of Nature Genetics (volume 27, no.1, January 2001) demonstrates the utility of the company's combinatorial biology technology in rapidly and efficiently identifying novel, functional drug targets in important disease signaling pathways. Functionally-validated targets are being used to develop a new generation of drugs that can treat diseases like cancer and hepatitis at the genetic level.
The study reports, for the first time, that technology developed by Rigel and licensed from the laboratory of Garry P. Nolan, Ph.D., at Stanford University enables the expression of peptide libraries inside mammalian cells, giving rise to a new way to approach functional genomics. Historically, researchers have experienced tremendous technical difficulty achieving intracellular expression of large numbers of functionally active peptides and proteins, which inhibited their ability to precisely identify targets inside a cell that could reverse a disease process. With the advent of Rigel's technology, researchers now have a simple yet powerful, broadly-applicable method to decipher the complex signaling pathways inside a cell.
``The ability to rapidly and precisely identify functional drug targets and understand how they impact complex signaling pathways is considered a key challenge in drug discovery in the post-genomic era,'' said Donald Payan, M.D., Rigel's executive vice president and chief scientific officer, and an author on the Nature Genetics study. ``Our combinatorial biology technology, which offers the first demonstration of a practical way to get at large-scale functional genomics in mammalian systems, provides a functional means to identify potential drug-target candidates as well as a biological understanding of human cellular disease mechanisms. Moreover, our proprietary technology is broadly applicable to a wide range of biological questions and their related disease states, making Rigel an attractive partner to pharmaceutical companies that need to fill their drug pipelines.''
A patent covering the technology described in this study was issued to Rigel by the U.S. Patent and Trademark Office (USPTO) in November, 2000. The USPTO's new guidelines regarding patenting of genes states the Patent Office's aim to prevent companies from patenting genes before having a clear defined use for them. Rigel believes the technology covered in this patent is consistent with the stated aim of the guidelines because it first identifies the use or function of a gene that is disease relevant and then identifies the gene.
The Nature Genetics study and accompanying editorial reports Rigel's success in applying its combinatorial biology technology to the emerging clinical problem of resistance to the anti-cancer drug, Taxol, to demonstrate proof-of-principle of this novel approach to functional genomics. The researchers used retroviruses to deliver a different peptide (a short segment of a larger protein) inside each of millions of mammalian tumor cells to see which tumor cells could survive when treated with the cancer-killing agent. Using Rigel's proprietary functional assays that are designed to identify the peptides that change the cell's biological outcome in the desired way (i.e., those tumor cells that survive in the presence of Taxol), the researchers identified seven peptides that allowed for increased Taxol resistance, one of which consistently had the highest survival rate and was linked to upregulation of the gene ABCB1 (also known as MDR1 for multiple drug resistance). Rigel's combinatorial biology technology also allows for the isolation and recovery of the target to which the peptide bound, and enables researchers to determine the mechanism by which the peptide exerts its effect.... |
