Chemical Genomics for Identifying Drug Candidates

Chemical genomics can help identify a diversity of targets in large gene families, according to Acadia Pharmaceuticals (San Diego, CA, USA). By using this new approach, the company's discovery efforts to date have resulted in the identification of novel small molecule ligands for more than 60 receptor targets.

Acadia has focused on two gene families that are particularly rich in drug targets, the G-protein coupled receptors (GPCRs) and nuclear receptors. Together, these two important gene families are believed to be the targets of more than half of the known drugs. Acadia has established functional assays for more than 250 targets out of the nearly 500 GPCRs and nuclear receptors within its proprietary chemical-genomics platform. The company says its broad drug discovery pipeline addresses large unmet medical needs and major commercial markets, including psychosis.

Acadia has identified ligands for several unexploited targets, including small molecule agonists for HNF4-alpha and PAR2. HNF4-alpha is an orphan nuclear receptor that when mutated causes a form of diabetes. PAR2 is a GPCR that is activated by the protease trypsin and has been linked to inflammatory disease and neuropathic pain.

"These exciting discoveries position Acadia to launch the first small molecule drug discovery efforts aiming at innovative therapies that exploit HNF-alpha and PAR2 modulation,” said Mark R. Brann, Ph.D., president and chief scientific officer of Acadia. Dr. Brann described the company's accomplishments at the Chemical Genomics Session of the 28th National Medicinal Chemistry Symposium in San Diego (CA, USA).




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