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Highlighted Publications

Keiser MJ, Setola V, Irwin JJ, Laggner C, Abbas AI, Hufeisen SJ, Jensen NH, Kuijer MB, Matos RC, Tran TB, Whaley R, Glennon RA, Hert J, Thomas KL, Edwards DD, Shoichet BK, Roth BL. Predicting new molecular targets for known drugs..  Nature. 2009 Nov 1. [Epub ahead of print]
Jones KA, Srivastava DP, Allen JA, Strachan RT, Roth BL, Penzes P. Rapid modulation of spine morphology by the 5-HT2A serotonin receptor through kalirin-7 signaling..  Proc Natl Acad Sci U S A. 2009 Nov 4. [Epub ahead of print]
Jean-Marc Guettier, Dinesh Gautam, Marco Scarselli, Inigo Ruiz de Azua, Jian Hua Li, Erica Rosemond, Xiaochao Ma, Frank J. Gonzalez, Blaine N. Armbruster, Huiyan Lu, Bryan L. Roth, and Jürgen Wess. A chemical-genetic approach to study G protein regulation of Beta cell function in vivo..  PNAS published online before print October 26, 2009, doi:10.1073/pnas.0906593106
Alexander GM, Rogan SC, Abbas AI, Armbruster BN, Pei Y, Allen JA, Nonneman RJ, Hartmann J, Moy SS, Nicolelis MA, McNamara JO, Roth BL. Remote control of neuronal activity in transgenic mice expressing evolved G protein-coupled receptors..  Neuron. 2009 Jul 16;63(1):27-39.
Conklin BR, Hsiao EC, Claeysen S, Dumuis A, Srinivasan S, Forsayeth JR, Guettier JM, Chang WC, Pei Y, McCarthy KD, Nissenson RA, Wess J, Bockaert J, Roth BL. Engineering GPCR signaling pathways with RASSLs.   Nat Methods. 2008 Aug;5(8):673-8.
Keiser MJ, Roth BL, Armbruster BN, Ernsberger P, Irwin JJ, Shoichet BK. Relating protein pharmacology by ligand chemistry.  Nat Biotechnol. 2007 Feb;25(2):197-206
Blaine N. Armbruster, Xiang Li., Mark H. Pausch., Stefan Herlitze., and Bryan L. Roth. Evolving the lock to fit the key to create a family of G protein-coupled receptors potently activated by an inert ligand.  PNAS published March 2, 2007, 10.1073/pnas.0700293104
Roth BL. Drugs and valvular heart disease.  N Engl J Med. 2007 Jan 4;356(1):6-9.
Vortherms TA, Mosier PD, Westkaemper RB, Roth BL. Differential Helical Orientations among Related G Protein-coupled Receptors Provide a Novel Mechanism for Selectivity: STUDIES WITH SALVINORIN A AND THE {kappa}-OPIOID RECEPTOR..  J Biol Chem. 2007 Feb 2;282(5):3146-56. Epub 2006 Nov 22
Elphick GF, Querbes W, Jordan JA, Gee GV, Eash S, Manley K, Dugan A, Stanifer M, Bhatnagar A, Kroeze WK, Roth BL, Atwood WJ. The human polyomavirus, JCV, uses serotonin receptors to infect cells.  Science. 2004 Nov 19;306(5700):1380-3
Goldberg MS, Pisani A, Haburcak M, Vortherms TA, Kitada T, Costa C, Tong Y, Martella G, Tscherter A, Martins A, Bernardi G, Roth BL, Pothos EN, Calabresi P, Shen J. Nigrostriatal Dopaminergic Deficits and Hypokinesia Caused by Inactivation of the Familial Parkinsonism-Linked Gene DJ-1.  Neuron, Vol 45, Issue 4, 3 February 2005
Yan F, Mosier PD, Westkaemper RB, Stewart J, Zjawiony JK, Vortherms TA, Sheffler DJ, Roth BL. Identification of the Molecular Mechanisms by Which the Diterpenoid Salvinorin A Binds to kappa-Opioid Receptors.  Biochemistry. 2005 Jun 21;44(24):8643-8651
Goldberg MS, Fleming SM, Palacino JJ, Cepeda C, Lam HA, Bhatnagar A, Meloni EG, Wu N, Ackerson LC, Klapstein GJ, Gajendiran M, Roth BL, Chesselet MF, Maidment NT, Levine MS, Shen J. Parkin-deficient mice exhibit nigrostriatal deficits but not loss of dopaminergic neurons.  J Biol Chem 2003 Oct 31;278(44):43628-35. Epub 2003 Aug 20
Setola V, Dukat M, Glennon RA, Roth BL. Molecular Determinants for the Interaction of the Valvulopathic Anorexigen Norfenfluramine with the 5-HT2B Receptor.  Mol Pharmacol. 2005 Jul;68(1):20-33. Epub 2005 Apr 14
Bhatnagar A, Sheffler DJ, Kroeze WK, Compton-Toth BA, Roth BL. Caveolin-1 interacts with 5-HT2A serotonin receptors and profoundly modulates the signaling of selected Gaq-coupled GPCRs .  J. Biol. Chem. published 9 June 2004, 10.1074/jbc.M404673200
Gray JA, Compton-Toth BA, Roth BL. Identification of two serine residues essential for agonist-induced 5-HT2A receptor desensitization.  Biochemistry 2003 Sep 16;42(36):10853-62
Xia Z, Gray JA, Compton-Toth BA, Roth BL. A direct interaction of PSD-95 with 5-HT2A serotonin receptors regulates receptor trafficking and signal transduction.  J Biol Chem 2003 Jun 13;278(24):21901-8. Epub 2003 Apr 07
Roth BL, Baner K, Westkaemper R, Siebert D, Rice KC, Steinberg S, Ernsberger P, Rothman RB. Salvinorin A: a potent naturally occurring nonnitrogenous kappa opioid selective agonist.  Proc Natl Acad Sci U S A 2002 Sep 3;99(18):11934-9. Epub 2002 Aug 21
Shapiro DA, Kristiansen K, Weiner DM, Kroeze WK, Roth BL. Evidence for a model of agonist-induced activation of 5-hydroxytryptamine 2A serotonin receptors that involves the disruption of a strong ionic interaction between helices 3 and 6.  J Biol Chem 2002 Mar 29;277(13):11441-9. Epub 2002 Jan 18
Munro TA, Rizzacasa MA, Roth BL, Toth BA, Yan F. Studies toward the pharmacophore of Salvinorin A. a potent kappa opiod receptor agonist.  J Med Chem. 2005 Jan 27;48(2):345-8
Sheffler DJ, Kroeze WK, Garcia BG, Deutch AY, Hufeisen SJ, Leahy P, Bruning JC, Roth BL. p90 ribosomal S6 kinase 2 exerts a tonic brake on G protein-coupled receptor signaling..  Proc Natl Acad Sci U S A. 2006 Mar 10; [Epub ahead of print]
Kozikowski AP, Roth B, Tropsha A. Why Academic Drug Discovery Makes Sense.  Science. 2006 Sep 1;313(5791):1235-6

Highlighted Reviews/Perspectives

Roth BL, Sheffler DJ, Kroeze WK. Opinion: Magic shotguns versus magic bullets: selectively non-selective drugs for mood disorders and schizophrenia.  Nat Rev Drug Discov. 2004 Apr;3(4):353-9
Armbruster BN, Roth BL. Mining the receptorome.  J. Biol. Chem, 10.1074/jbc.R400030200
Sheffler DJ, Roth BL. Salvinorin A: the "magic mint" hallucinogen finds a molecular target in the kappa opioid receptor.  Trends Pharmacol Sci 2003 Mar;24(3):107-9
JA Gray and BL Roth. A last GASP for GPCR's?.  Science 297: 529-531,2002
Kroeze, W.K., K. Kristiansen and BL Roth. Molecular biology of serotonin receptors: structure and function at the molecular level.  Curr Top Med Chem 2:507-528, 2002
Roth BL. Neuronal Signal Transduction Pathways: Wasteland or the Promised Land? Science (STKE).  http://www.stke.org/cgi/content/full/OC_sigtrans;2000/45/pe1
Roth BL, Willins D. What's all the RAVE about receptor internalization?.  Neuron. 23:629-631