Marc will outline the development, optimization and validation of a range of voltage-gated Ca2+ channel assays on the Patchliner automated patch clamp platform that were subsequently used in an 8 year drug discovery collaboration between Metrion Biosciences and a german pharma company.
The project was successful in identifying several lead series of selective,state-dependent inhibitors of Cav2.2 N-type channels for use as novel, non-opioid analgesic.This required the creation of biophysical screening assays to identify the potency of small molecules against the resting and inactivated state of the human neuronal Ca2+ channels Cav2.1(P/Q type), Cav2.2 and Cav3.2 (T-type), some of which are notoriously difficult in terms of expression levels and current rundown.