Tyrosine Phosphatase-1B inhibitors discovered

Small molecule drugs could potentially be used in Type-2 diabetes treatment

Structural Bioinformatics Inc. (SBI; San Diego) has discovered a number of selective Protein Tyrosine Phosphatase-1B (PTP-1B) inhibitory lead molecules. The company plans to optimize the leads for testing as a therapy in animal models for Type-2 diabetes and obesity.

Type-2 diabetes affects some 16 million people in the United States, with 800,000 new patients diagnosed each. Current treatments include injectable insulin, oral hypoglycemics, and glitazones, but safety precautions and concerns about side effects, including weight gain and liver failure, remain.

SBI scientists have shown that PTP-1B is critically implicated in insulin receptor regulation and re-sensitization, and have validated the the molecule as a novel drug discovery target through molecular biology and animal pharmacological studies. Orally active PTP-1B enzyme inhibitors may offer advantages over glitazones as a mechanism-based Type-2 diabetes treatment.

Structural Bioinformatics is focused on computational proteomics, the large-scale generation and use of protein structure and protein structural information. The company has developed technologies to generate 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 pharmaceutical companies.

For more information: Jerry Dodd, Vice President of Corporate Development, Structural Bioinformatics Inc., 10929 Technology Place, San Diego, CA 92127. Tel: 858-675-2400. Fax 858-618-1041. Email: jdodd@strubix.com.

Edited by Jim Pomager
Assistant Editor, Drug Discovery Online