Rigel Pharmaceuticals, Inc. Describes Role Of UHRF1, A Ubiquitin Ligase, In Tumor Growth

SOUTH SAN FRANCISCO, Calif., Nov. 28 /PRNewswire-FirstCall/ -- Rigel Pharmaceuticals, Inc. today announced that findings from its study identifying the role of a E3 ubiquitin ligase known as UHRF1 in the regulation of cellular proliferation and cellular repair was published in Molecular Biology of the Cell, the journal of the American Society for Cell Biology. The Rigel study shows the potential of this protein as an attractive oncology target.

Early cellular events associated with tumorigenesis often include loss of cell cycle checkpoints or alteration in growth signaling pathways. Identification of novel genes involved in cellular proliferation may lead to new classes of cancer therapeutics. Scientists at Rigel, in collaboration with Johnson & Johnson Pharmaceutical Research and Development, isolated UHRF1 from a functional genomics screen designed to identify genes that interfere with proliferation. They found that UHRF1 expression is elevated in proliferating cells and primary tumors. The scientists further found that interference with UHRF1 ubiquitin ligase function rendered cells sensitive to the effects of chemotherapeutics, identifying a role for UHRF1 ligase activity in cellular survival.

“We are particularly interested in the selective inhibition of ubiquitin ligases, since it could lead to pharmaceutical product candidates with higher specificity and lower toxicity for cancer patients,” said Donald G. Payan, M.D., executive vice president and chief scientific officer of Rigel. “The targeting of intracellular protein degradation pathways has become an especially attractive therapeutic strategy due to the success of proteasome inhibitors in the treatment of multiple myeloma.”

This study is part of a five-year collaboration between Rigel and Johnson & Johnson that began in December 1998. The purpose of the collaboration was to identify and validate novel drug targets that regulate the cell cycle, which controls cancer progression. Over the course of this collaboration, Johnson & Johnson accepted eight targets that Rigel researchers discovered and validated. Johnson & Johnson is currently moving these targets forward to discover and develop drug candidates, which inhibit tumor cell growth or sensitize tumor cells to chemotherapeutic agents.

About Rigel

Rigel is a clinical-stage drug development company that discovers and develops novel, small-molecule drugs for the treatment of inflammatory diseases, cancer and viral diseases. Our goal is to move one new product candidate for a significant indication into the clinic each year. We have achieved this goal since 2002. Our pioneering research focuses on intracellular signaling pathways and related targets that are critical to disease mechanisms. Rigel’s productivity has resulted in strategic collaborations with large pharmaceutical partners to develop and market our product candidates. We have product development programs in allergy/asthma, rheumatoid arthritis and cancer.

This press release contains “forward-looking” statements, including statements related to Rigel’s plans to pursue clinical development of product candidates and the timing thereof and the potential efficacy of product candidates. Any statements contained in this press release that are not statements of historical fact may be deemed to be forward-looking statements. Words such as “plans,” “intends,” “expects” and similar expressions are intended to identify these forward-looking statements. There are a number of important factors that could cause Rigel’s results to differ materially from those indicated by these forward-looking statements, including risks associated with the timing and success of pre-clinical studies and clinical trials, as well as other risks detailed from time to time in Rigel’s SEC reports, including its Quarterly Report on Form 10-Q for the quarter ended September 30, 2005. Rigel does not undertake any obligation to update forward- looking statements.

Contact: Raul Rodriguez Phone: 650-624-1302 Email: invrel@rigel.com Media Contact: Jennifer Pendergrass, WeissComm Partners, Inc. Phone: 415-946-1070 Email: jennifer@weisscommpartners.com

Photo: NewsCom: http://www.newscom.com/cgi-bin/prnh/20030226/RIGLLOGOAP Archive: http://photoarchive.ap.orgPRN Photo Desk photodesk@prnewswire.comRigel Pharmaceuticals, Inc.

CONTACT: Raul Rodriguez of Rigel Pharmaceuticals, Inc., +1-650-624-1302,or invrel@rigel.com; or Jennifer Pendergrass of WeissComm Partners, Inc.,+1-415-946-1070, or jennifer@weisscommpartners.com, for RigelPharmaceuticals, Inc.

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