Learn More
The discovery that drugs targeting a single G protein-coupled receptor (GPCR) can differentially modulate distinct subsets of the receptor signaling repertoire has created a challenge for drug discovery at these important therapeutic targets. Here, we demonstrate that a single label-free assay based on cellular impedance provides a real-time integration of(More)
G protein-coupled receptors (GPCRs) are the largest superfamily of receptors encoded by the human genome, and represent the largest class of current drug targets. Over the last decade and a half, it has become widely accepted that most, if not all, GPCRs possess spatially distinct allosteric sites that can be targeted by exogenous substances to modulate the(More)
The  2 adrenergic receptor ( 2 AR) increases intracellular Ca 2+ in a variety of cell types. By combining pharmacological and genetic manipulations, we reveal a novel mechanism through which the β 2 AR promotes Ca 2+ mobilization (pEC 50 = 7.32 ± 0.10) in non-excitable human embryonic kidney (HEK)-293S cells. Down-regulation of Gs with sustained cholera(More)
  • 1