SAN DIEGO--(BW HealthWire)--Nov. 6, 2000--Privately-held Structural Bioinformatics Inc. (SBI) Monday announced the award of a USD $100,000 Phase I Small Business Innovation Research (SBIR) grant from the National Cancer Institute, a division of the National Institutes of Health in Bethesda, Md., to develop non-peptide small molecules for cancer treatment.
The grant entitled ``Structure-based Design of Novel Bcl-2 Antagonists'' will enable SBI scientists to apply the company's proprietary protein modeling and dynamic pharmacophore-based searching of existing and virtual combinatorial libraries to rapidly identify and synthesize small-molecule inhibitors of this essential protein-protein interaction.
Bcl-2 is a critical regulator of programmed cell death (apoptosis). A systematic survey of a variety of human cancer specimens revealed that this proto-oncogene is over-expressed in many tumors. Over expression of this protein promotes cell survival of cancerous cells by enhancing the cells' ability to proliferate, metastasize and resist chemotherapy. A recent phase II clinical success from blocking expression of this gene through an antisense compound has validated its importance. However, no small-molecule inhibitor of Bcl-2 is currently in clinical development. SBI's computational approach has identified initial small-molecule inhibitors, which it expects to structurally refine to drug candidates under SBIR funding.
``NCI funding acknowledges the importance of this target and SBI's past successes in designing small molecules to disrupt much larger binding surfaces,'' said Jerry Dodd, SBI's vice president of Corporate Development.
Structural Bioinformatics is a world leader in computational proteomics -- the large-scale generation and use of protein structure and protein structural information. 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 (CombiLib(TM) modules) or present in our clients' in-house compound collections. |
