ACADIA Pharmaceuticals Inc., a biopharmaceutical company utilizing innovative technology to fuel drug discovery and clinical development of novel treatments for central nervous system (CNS) disorders, has reported on the development of assay technologies for a major class of drug targets, tyrosine kinase linked receptors (RTKs). This important gene family has been demonstrated to play a significant role in the development of many disease states, including CNS disorders and cancer.

In a poster presentation at the Molecular Pharmacology Gordon Conference in Ciocco, Italy, recently, ACADIA highlighted a novel application of BRET (Bioluminescence Resonance Energy Transfer) technology used to measure the interaction of RTKs with several signalling proteins. This assay technology allowed ACADIA scientists to define the biology of mutant forms of the epidermal growth factor receptor that have been associated with lung cancer. ACADIA scientists have found that these mutations induce constitutive signalling through several proteins. Iressa and Tarceva, two drugs used to treat cancer, block this constitutive signalling with potencies that are dependent on the signalling protein and the specific mutation.

In an abstract at the ASCO (American Society of Clinical Oncology) Annual Meeting 2005 in Orlando, Florida, May 13-17, ACADIA described the application of its proprietary assay technology known as R-SAT (Receptor Selection and Amplification Technology) to the development of high throughput assays for the majority of known RTKs. While R-SAT has the capability of identifying activators and inhibitors of RTKs, a key feature of the assay technology is its ability to identify compounds that block constitutive signalling of RTKs, explains a release from the company.

"In addition to focusing on G-protein coupled receptors and nuclear receptors, we have now expanded our technology platform to include RTKs. This will allow us to further strengthen our drug discovery capabilities and systematically search for novel small molecule therapeutics for these targets," said Mark R. Brann, president and chief scientific officer of ACADIA.