Description:

The Department of Pharmacology invites you to a guest speaker lecture presented by Andrew M. Schumacher, Ph.D., Senior Investigator at the Genomics Institute of the Novartis Research Foundation.

Below is an overview as decribed by Dr. Schumacher:

Transient receptor potential A1 (TRPA1) is a nonselective cation channel that plays an important role in nociception, or the sensing of noxious stimuli. TRPA1 activation in sensory neurons results in the secretion of proinflammatory peptides involved in pain transmission. TRPA1 may therefore be a key nociceptor in both acute and neuropathic pain resulting from disease or injury. Consistent with these data, TRPA1 knockout mice show a reduced pain response, suggesting a therapeutic approach. High throughput screening and medicinal chemistry optimization generated selective antagonists of TRPA1 with drug-like properties. These show robust activity in rodent models of inflammatory pain and topical models of ocular pain. Highlights from the widely used approach will include screening and optimization of novel chemical scaffolds for pharmacologic properties as well as function. The approach also reveals how target validation guides selection of potential therapeutic indications.