Lead Inventor:
Virginia Cornish, Ph.D.
Screening of molecules as drug candidates based on protein binding:
Drugs exert their therapeutic effect by binding to a particular protein and regulating its activity. Thus it is important to identify whether a molecule, as a drug candidate, is able to bind on a protein target. Methods to identify molecules' binding to proteins are of great use in drug discovery and screening.
Protein binding as indicator of candidtae drug molecules :
Method for identifying a molecule as being able to bind a protein target in a cell, involves (a) covalently binding the molecule to trimethoprim (TMP) to form a screening molecule, (b) introducing the screening molecule into the cell which (A) expresses (i) a first fusion protein comprising a binding domain capable of binding TMP, and (ii) a second fusion protein comprising the protein target, and (B) comprises a reporter gene, where one of the fusion proteins comprises a DNA-binding domain and the other fusion protein comprises a transcription activation domain and where expression of the reporter gene is conditioned on the proximity of the DNA-binding domain to the transcription activation domain, and (c) determining whether the screening molecule binds to the first fusion protein and to the second fusion protein by determining whether the cell expresses the reporter gene, where expression of the reporter gene indicates that the molecule binds the protein target and wherein lack of expression of the reporter gene indicates that the molecule does not bind the protein target.
Applications:
• To identifying molecule as being able to bind protein target in cell
• Drug discovery and screening
• Discovery of functional genomics
Advantages:
• Fast identification of a molecule as being able to bind a protein target
• Easy to establish
Patent Status: Patent Pending (US20090162858A1) ~ see link below.
Licensing Status: Available for Licensing and Sponsored Research Support