Screening for Non-Pore-Binding Modulators of EAG K+ Channels

In this report, we present two independent screening campaigns in which we wanted to identify small molecules that bind to either the intracellular cytoplasmic amino terminal Per-Arnt-Sim (PAS) domain from the human EAG-related gene (ERG) channel or the amino or carboxy terminal globular domains from the mouse EAG1 channel, affecting their interaction. We report that in both cases, compounds were identified that showed weak, nonspecific binding. We suggest alternative routes should be pursued in future efforts to identify specific, high-affinity binders to these cytoplasmic domains.

Source: Journal of Biomolecular Screening - July 19, 2016 Category: Molecular Biology Authors: Fernandes, A. S., Morais-Cabral, J. H., Harley, C. A. Tags: Technical Note Source Type: research