SAN DIEGO, CA - (May 13, 1999) - Privately-held Structural Bioinformatics Inc. (SBI) today announced the award of a USD $100,000 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, to develop non-peptide small-molecule inhibitors targeting a bacterial metalloproteinase. The grant will enable SBI scientists to apply the Company's proprietary protein modeling and dynamic pharmacophore-based searching of existing and virtual combinatorial libraries to identify and synthesize putative small-molecule inhibitors rapidly.

"We are very pleased to receive this second SBIR grant to apply our lead-finding technology to yet another therapeutic area," remarked Dr. Edward Maggio, Ph.D., President and Chief Executive Officer of Structural Bioinformatics Inc. "Our first SBIR grant announced last month is for the discovery and development of HER2 antagonists as potential therapeutics for the treatment of breast, prostate, and colon cancers. By means of the SBIR program and various corporate collaborations with pharmaceutical companies, we hope to continue to establish the Company as the leader in rapid small-molecule lead discovery."

The goal of this Phase I SBIR grant is to identify a number of non-peptide small-molecule inhibitors which target the protease. SBI will use its patented and proprietary algorithms first to model the dynamic surface of the target protein and then to extract 3-D-pharmacophore structural information. The pharmacophore information will then be used to computationally prescreen large-scale small-molecule compound libraries (both commercial and in-house generated virtual combinatorial libraries) for likely drug activity. SBI's computational prescreening technology (DynaPharm^TM technology) results in a typical hit rate ranging from 5 to 20% for finding drug-like leads. DynaPharm^TM-based screening permits an astounding reduction in the number of compounds to be actually synthesized and tested by a factor of 100X to 1000X compared to traditional drug discovery efforts. In previous projects, SBI has successfully applied this technology to six clinically important targets on behalf of three corporate pharmaceutical collaborators over the course of the last 18 months. In each case, multiple chemical series of antagonists were generated for each target in the viral protease, protein kinase, hormone and apoptosis areas.

About SBI:

Structural Bioinformatics Inc. accelerates small-molecule drug development by closing the gap from gene sequence to lead discovery and is a world leader in computer-based protein analysis. The Company has developed advanced algorithms that are used to calculate the dynamic 3-D structure of proteins from sequence information using comparative modeling augmented with energy-based methods. In turn, the 3-D information is used to design and select small molecules from various chemical subclasses that will act as inhibitors or antagonists to the protein. SBI enables pharmaceutical companies to make sense of the enormous amount of genetic data emerging from sequencing of the human genome and to translate the data into structural information and, eventually, drug candidates.