Novel Class of Compounds Produced to Regulate Gene Expression

Strategic Insights -

Genelabs Technologies, Inc., a biopharmaceutical company, and DuPont Pharmaceuticals have renewed their research and license agreement for an additional year to discover and develop drugs that control the expression of certain disease-associated genes. The purpose of the agreement is to develop new therapeutic interventions for diseases such as cancer and autoimmune disorders. The collaboration utilizes an integrated platform of drug discovery technologies, including structure-biased combinatorial chemistry and high-throughput screening with proprietary assays. These assays identify small molecules that bind to DNA in a sequence-specific manner, designed to bind to regulatory regions that control gene expression.

Key Takeaways:

  • The renewed agreement between Genelabs and DuPont Pharmaceuticals aims to develop new therapeutic interventions for diseases such as cancer and autoimmune disorders.
  • The collaboration utilizes an integrated platform of drug discovery technologies, including structure-biased combinatorial chemistry and high-throughput screening with proprietary assays.
  • Small molecules have been designed to bind specifically to regulatory regions that control the expression of genes involved in diseases.
  • The technologies are designed to facilitate the discovery of novel DNA-binding chemistries and the characterization of these molecules.
  • The resulting drugs are expected to be capable of up-regulating or down-regulating, as appropriate, the expression levels of target genes.
  • The collaboration has identified drug binding sites in the promoters of the genes selected for the collaboration to date, and potential drug leads are being screened for multiple therapeutic gene targets.
  • The companies have made excellent progress in the collaboration, with molecules from several sources being screened for their DNA-binding characteristics.
  • Genelabs transcription regulation scientists have used site-directed mutagenesis in reporter gene systems to determine the regulatory protein binding sites that are critical to gene expression in several target genes.
  • The company is developing its own chemistry capabilities, and the collaboration is expected to lead to the discovery of an entirely new field of drugs.
  • The translating technologies are designed to offer access to a new field of pharmaceuticals, small molecule DNA-binding drugs targeted to specific disease-associated genes.

Statistics:

  • The milestones in the agreement can provide up to $20 million for each gene target during the course of the drug development process.
  • The total value of the agreement could exceed $200 million and will depend on the number of lead compounds and/or drugs discovered.
  • The company has identified drug binding sites in the promoters of the genes selected for the collaboration to date, which is a significant achievement.
  • High-throughput screening with proprietary assays has identified potential drug leads for multiple therapeutic gene targets.
  • The company is developing its own chemistry capabilities, which will enhance its ability to create novel DNA-binding chemistries.

Sources:

  • Genelabs Technologies, Inc. (Nasdaq: GNLB)
  • DuPont Pharmaceuticals
  • Isis Pharmaceuticals, Inc.
  • Tripos, Inc.
  • PR Newswire
  • http://www.genelabs.com
  • http://www.prnewswire.com