SAN DIEGO--(BW HealthWire)--Nov. 8, 2000--Privately-held Structural Bioinformatics Inc. (SBI) announced today that it has discovered a number of selective Protein Tyrosine Phosphatase-1B inhibitory lead molecules.
The PTP-1B enzyme inhibitory leads will now be optimized for testing as a novel therapy in appropriate animal models for Type-2 diabetes and obesity. Currently, Type-2 diabetes affects an estimated 16 million people with 800,000 newly diagnosed patients added yearly in the United States. During the last decade, the numbers of Type-2 diabetes cases, hospitalizations, and deaths have been increasing. Moreover, evidence shows that Type-2 diabetes is increasing in severity, especially in westernized societies. Thus far, treatment of Type-2 diabetes has been based on injectable insulin, oral hypoglycemics, and the more recently introduced glitazones. However, safety precautions and concerns about certain side effects observed for some members of this family, including weight gain and liver failure, remain.
PTP-1B has been shown to be critically implicated in insulin receptor regulation and re-sensitization, and has been clearly validated as a novel drug discovery target through molecular biology and animal pharmacological studies. Orally active PTP-1B enzyme inhibitors may offer a significant advancement and advantage over the glitazones as a mechanism-based Type-2 diabetes treatment.
Recently, Structural Bioinformatics announced the selection of a kinase inhibitor discovered by SBI, in its collaboration with Yamanouchi, for advancement into preclinical development. Previously, SBI announced the discovery of HER-2 antagonist lead compounds as potential therapeutics for the treatment of breast, prostate, and colon cancers, and IL-5 antagonists for potential treatment of asthma. Other discovery projects underway include Bcl-2 inhibitors and protein kinase inhibitors. In each of these cases, SBI scientists have successfully applied the Company's proprietary DynaPharm(TM) and CombiLib(TM) technologies to computationally predict and synthesize putative small-molecule inhibitors, in multiple chemical scaffolds, within 90 to 120 days, with hit rates in biological assays ranging from 2% to 24%.
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 technologies to generate highly refined three-dimensional structural models of proteins from primary genetic information and commercializes these technologies through its structural database products and through drug discovery collaborations with leading pharmaceutical companies. SBI has offices in San Diego and Horsholm, Denmark. |
