- GPCR Structure and Function
- Synthetic Neurobiology
- Drug Discovery
GPCR structure and function
G-protein coupled receptors (GPCRs) represent one of the most evolutionarily diverse superfamilies of the human genome. My lab studies all aspects of GPCR structure and function ranging from the atomic-level analysis of ligand-receptor interactions to in vivo studies. Currently we are focused on members of the serotonin (5-hydroxytryptamine; 5-HT) and opioid receptor families and their accessory proteins.
We invented the chemogenetic technology dubbed: DREADD (Designer Receptors Exclusively Activated by Designer Drug) which is currently used by 100’s of labs around the world (see Vardy et al, Neuron 2015 for recent paper).
We are actively engaged in drug discovery efforts via the shared resources of the National Institute of Mental Health’s Psychoactive Drug Screening Program. Our goals are to discover and develop novel small molecule probes for in vitro and in vivo validation of molecular targets for therapeutic drug discovery. We have particular strengths with GPCR and ion-channels and have expanded our capabilities to enable screening of the entire GPCR-ome in massively parallel screening campaigns (see Keiser et al, Nature 2009; Huang et al, Nature in press and Kroeze et al, Nature Structural Biology 2015 for recent papers).