Celera Genomics And Syrrx Publish X-Ray Crystal Structure Of A Human Histone Deacetylase
Promising Target For Cancer Treatments Visualized at the Atomic Level
SOUTH SAN FRANCISCO, CA - July 14, 2004
Celera Genomics Group (NYSE:CRA), an Applera Corporation business, today announced publication in the journal Structure of the first three-dimensional x-ray crystal structure of a member of the class I histone deacetylases, human histone deacetylase 8 (HDAC8). HDAC enzymes can lead to the proliferation of cancer cells. Celera Genomics is investigating HDAC inhibitors in preclinical trials as potential treatments for cancer.
Researchers from Celera Genomics and Syrrx, Inc. determined the structure of human histone deacetylase 8 (HDAC8) bound to an experimental HDAC inhibitor synthesized by Celera Genomics, as well as the structures of other HDAC inhibitors currently under preclinical and clinical evaluation by other parties. The HDAC8 structure was determined using Syrrx's Nanovolume Crystallization® technology to crystallize disease-associated proteins. Celera Genomics and Syrrx are independently using the structure to design novel small-molecule HDAC inhibitors that may have advantages over current HDAC inhibitors undergoing evaluation.
“This structure provides new insights into how the HDAC’s function and a framework for identifying novel HDAC inhibitors,” said Robert Booth, Ph.D., Chief Scientific Officer of Celera Genomics. “Celera’s scientists have identified several novel inhibitors that exhibit in vivo efficacy in xenograft models of cancer, including one that reduced tumor volume by approximately 89% relative to untreated controls in a 17 day preclinical study.”
Histone deacetylation is carried out by a set of related HDAC enzymes and causes changes in DNA structures that can lead to the proliferation of cancer cells. Previously published studies indicate that inhibition of the HDAC enzymes can modulate cell growth rates, and in some cases, specifically induce the death of tumor cells. These data have fueled the design of small-molecule inhibitors of HDAC that are currently undergoing testing as potential treatments for major human diseases, including cancer.
About Celera Genomics and Applera Corporation
Applera Corporation consists of two operating groups. The Celera Genomics Group, located in Rockville, MD, and South San Francisco, CA, is engaged principally in integrating advanced technologies to discover and develop new therapeutics. Celera intends to leverage its proteomic, bioinformatic, and genomic capabilities to identify and validate drug targets, and to discover and develop new therapeutics. Its Celera Discovery SystemTM online platform, marketed exclusively by Applied Biosystems, is an integrated source of information based on the human genome and other biological and medical sources. The Applied Biosystems Group (NYSE: ABI) serves the life science industry and research community by developing and marketing instrument-based systems, consumables, software, and services. Applied Biosystems is headquartered in Foster City, CA, and reported sales of $1.7 billion during fiscal 2003. Celera Diagnostics, a 50/50 joint venture between Applied Biosystems and Celera Genomics, is focused on discovery, development, and commercialization of novel diagnostic products. Information about Applera Corporation, including reports and other information filed by the company with the Securities and Exchange Commission, is available at www.applera.com, or by telephoning 800.762.6923. Information about Celera Genomics is available at www.celera.com. All information in this press release is as of the date of the release, and Applera does not undertake any duty to update this information, including any forward-looking statements, unless required by law.
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