Drug Discovery

Most drugs bind to active sites on proteins involved in critical metabolic pathways. When drugs bind to a specific site on a target protein they either prevent (antagonist effect) or facilitate (agonist effect) the protein's cellular function. The binding of the drug to its target depends on the Structure-Activity-Relationship (SAR). Hence it is crucial for successful drug discovery to precisely characterize the drug target site.

Contrary to previous dogma, it is now known that a single gene frequently codes for multiple versions of the same protein through multiple intermediary mRNAs. Hence a variety of target sites for the drug are possible. Although present technologies may identify the blueprint for an active site (e.g. presence of an exon), they do not accurately predict the SAR relationship of all possible variants. With our proprietary technologies we are able to accurately characterize the multiple mRNAs, and thereby confidently predict the 3-D structure of the target site variants, as well as their SARs.

Drug discovery is a 'Research process that identifies molecules with desired biological effects in animal models, and thus have promise as new therapeutic drugs in humans'. Drug discovery starts with the solution of two fundamental issues: 

• Identification of pathway proteins that are associated with the disease process.
• Selection of the target protein.

Our approach includes:

• Determination of key proteins in the disease pathway.
• Determination of structural variations of disease pathway proteins in test animals and/or humans.
• Determination of structural variations of drug specific non-target proteins in test animal and/or humans.
• Finalizing lead protein target(s).