One particular advantage of the F2H® platform is that only those molecules will emerge as possible drug candidates which are taken up into cells and which show little or no cytotoxicity. In addition, due to the standardized binding platform used, it is possible to conduct comparative protein-protein-interaction (PPI) studies.
To date, more than 50 protein-protein-interactions have been successfully reconstructed with the F2H® system. "For example, by tracing the binding of p53 to Mdm2 or Mdm4, known inhibitors of these interactions could be verified and new inhibitors identified" states Dr. Kourosh Zolghadr, Head of R&D at ChromoTek. ChromoTek's academic partner, Prof. Sir David Lane, calls the F2H® approach a missing link between biochemistry and cell biology. In collaboration with his lab, the F2H® assay was successfully applied for comprehensive (stapled) peptide profiling for activation of p53 (recently published in ACS Chem. Biol. 8 (3): 506-512 (2013)).
ChromoTek not only offers p53:Mdm2 and/or p53:Mdm4 compound screening and profiling services but, owing to the flexibility and versatility of this new technology, develops customized F2H® PPI assays to conduct compound screening services for biotech/pharma partners aiming to increase the efficiency of their drug discovery and validation programs with real time cellular data.