Public Relations Contact:
 
Alicia Althoff
Marketing Communications Coordinator
alicia@strubix.com

Structural Bioinformatics, Inc.
10929 Technology Place
San Diego CA 92127
Telephone: (858) 675-2400 ext. 119
Facsimile: (858) 618-1041
 
http://www.strubix.com/

 
STRUCTURAL BIOINFORMATICS INC. ANNOUNCES DISCOVERY OF
SMALL-MOLECULE INTERLEUKIN-5 RECEPTOR ANTAGONIST LEADS
FOR TREATMENT OF EOSINOPHILIA-INDUCED ALLERGIC DISEASES
 

 SAN DIEGO, CA - (January 17, 2000) - Privately-held Structural Bioinformatics, Inc. (SBI) announced today that it has discovered a number of interleukin-5 (IL-5) receptor antagonist molecules through a Phase I Small Business Innovation Research (SBIR) grant from the National Institute of Allergy and Infectious Diseases, a division of the National Institutes of Health in Bethesda, MD. The IL-5 receptor antagonist leads will now be optimized for testing as a novel therapy for allergic diseases including asthma. Currently, asthma affects an estimated 10 to 15 million people and claims the lives of more than 4,000 people per year in the United States. During the last decade, the numbers of asthma cases, hospitalizations, and deaths have been increasing. Moreover, evidence shows that asthma is increasing in severity, especially in westernized societies. Thus far, treatment of asthma has been based on corticosteroids (inhaled and systemic), leukotriene antagonists and bronchodilators. However, prolonged use of these drugs leads to the development of tachyphylaxis and other serious side effects, including death. The IL-5 receptor is implicated in eosinophilia which, in turn, is historically ascribed to allergic diseases including dermatitis, eczema, rhinitis, conjunctivitis and extrinsic asthma. Orally active IL-5 receptor antagonists may offer a significant advancement as a mechanism-based asthma treatment.

Another SBIR grant to Structural Bioinformatics has led to the discovery of HER2 antagonists as potential therapeutics for the treatment of breast, prostate, and colon cancers. A third grant is focused on the discovery of inhibitors of a bacterial metalloproteinase. In each of these cases, SBI scientists have successfully applied the Company's proprietary DynaPharmTM and CombiLibTM technologies to predict computationally and synthesize putative small-molecule inhibitors, in multiple chemical scaffolds, within 90 to 120 days, with hit rates in biological assays ranging from 4% to 17%.

Structural Bioinformatics is a world leader in computational proteomics--the large-scale generation and use of protein structure and protein structural properties. The Company has developed advanced and proprietary computational technologies to generate highly refined three-dimensional structural models of proteins from primary gene sequence data that compare well with crystal structures, and to perform primary drug-discovery screening in silico on millions of compounds present in SBI's scaffold-specific virtual combinatorial libraries (CombiLibTM modules) or our clients' in-house compound collections. SBI offers two subscription database products. The first, SBdBaseTM, which is composed of thousands of structural models of proteins from more than 150 distinct families, promises to accelerate lead discovery and optimization and to enable rational experimental design broadly across multiple disciplines within the pharmaceutical and life sciences. The second, SVdBaseTM, is actually a growing series of database modules each containing structural models generated from genetic variations in a single, medically important gene, such as HIV reverse transcriptase or protease, which provide pharmacogenomic insights early-on in the drug discovery and optimization process, and facilitate the selection of optimal clinical candidates prior to initiation of clinical trials. SBI's partner in generating HIV SVdBases is Quest Diagnostics, Inc. SBI also employs its technologies in collaborative R&D programs. Current partners include BioChem Pharma Inc., Yamanouchi Pharmaceutical Co., Ltd. and DuPont Pharmaceuticals Company.