Bryan Roth

Bryan Roth

Professor

Department of Pharmacology

Michael Hooker Distinguished Professor of Protein Therapeutics and Translational Proteomics

Division of Medicinal Chemistry and Natural Products, School of Pharmacy

Director, NIMH Psychoactive
Drug Screening Program

M.D., Medicine
St. Louis University School of Medicine

Ph.D. Biochemistry
St. Louis School of Medicine, St. Louis, MO

Biosketch [.pdf]

NIMH Psychoactive Drug Screening Program
Ki Database
Roth Lab Website

Contact Information  ->>

Research Interests

  • GPCR Structure and Function
  • Drug Discovery

Research Synopsis

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.

Drug Discovery

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 are gradually expanding our capabilities to, eventually, screen the receptorome (the entire complement of receptors in the genome) and kinome (the entire complement of kinases in the genome) in massively parallel screening campaigns (see figure).

Publications

pubmed

Click above for PubMed publications.

  • Keiser, M., Setola, V., Irwin, J., Laggner, C., Abbas, A., Hufesein, S.., Jensen, N., Kuijer, M., Matos, R., Tran, T.B., Whaley, R., Glennon, R.A., Hert, J., Thomas, K.L.H., Edwards, D.D., Shoichet, B.K.* and Roth, B.L*. (2009) Predicting new molecular targets for known drugs. Nature 462: 175-181, 2009. PMC2784146. (*BLR and BKS=Co-Corresponding authors) Abstract

  • Besnard, J.., Ruda, G.F., Setola, V., Abecassis, K., Rodriguez, R.M., Huang, X-P., Norval, S., Sassano, M.F., Shin, A.I., Webster, L.A., Simeons, F.R.C., Stojanovski, L., Prat, A., Seidah, N.G., Constam, D.B., Bickerton, G.R., Read, K.D., Wetsel, W.C., Gilbert, I.H., Roth, B.L.* and Hopkins, A.L*. (2012) Automated design of ligands with polypharmacology profiles. Nature 492: 215-220. PMID:23235874. (*BLR and ALH=Co-Corresponding Authors). Abstract

  • Fenalti, G., Giguere, P., Katrich, S., Huang, X-P., Thompson, A., Cherezov, A., Roth, B.L. and Stevensm R.C. (2014) Molecular Control of δ-Opioid Receptor Signaling, Nature, Jan. 12, doi: 10.1038/nature12944. [Epub ahead of print] PMCID:24413399. (*BLR and RCS=Co-corresponding authors). Abstract

  • Alexander, G.M., Rogan, A.C., Abbas, A.I., Armbruster, B.N., Pei, Y., Allen, J.A., Nonneman, R.J., Hartmann, J., Moy, S.S., Nicolelis, M.A., McNamara, J.O. and Roth, B.L.  Remote control of neuronal activity in transgenic mice expressing evolved G protein coupled receptors. Neuron 63(1):27-39. PMC2751885. Abstract

  • Wacke, D., Wang, C., Katritch, V., Han, G.W., Huang, X.P., Vardy, E., McCorvy, J.D., Jiang, Y., Chu, M., Siu, F., Liu, W., Xu, H.E., Cherezov, V., Roth, B.L. and Stevens, R.C. (2013) Structural Features for Functional Selectivity at Serotonin Receptors. Science 340(6132): 615-9. PMID:23519210.  (*BLR and *RCS=Co-corresponding authors) Abstract



Contact Information


Office Location:
4072 Genetic Medicine

Mailing Address:
CB # 7365
UNC-CH School of Medicine
Chapel Hill, NC 27599-7365

Office Phone: 919-966-7535
Fax: 919-966-5640
bryan_roth[at]med.unc.edu

 

 

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