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Items: 1 to 20 of 172

1.

Structure-Based Discovery of New Antagonist and Biased Agonist Chemotypes for the Kappa Opioid Receptor.

Zheng Z, Huang XP, Mangano TJ, Zou R, Chen X, Zaidi SA, Roth BL, Stevens RC, Katritch V.

J Med Chem. 2017 Apr 13;60(7):3070-3081. doi: 10.1021/acs.jmedchem.7b00109. Epub 2017 Apr 3.

2.

In silico design of novel probes for the atypical opioid receptor MRGPRX2.

Lansu K, Karpiak J, Liu J, Huang XP, McCorvy JD, Kroeze WK, Che T, Nagase H, Carroll FI, Jin J, Shoichet BK, Roth BL.

Nat Chem Biol. 2017 May;13(5):529-536. doi: 10.1038/nchembio.2334. Epub 2017 Mar 13.

3.

Targeting the histone methyltransferase G9a activates imprinted genes and improves survival of a mouse model of Prader-Willi syndrome.

Kim Y, Lee HM, Xiong Y, Sciaky N, Hulbert SW, Cao X, Everitt JI, Jin J, Roth BL, Jiang YH.

Nat Med. 2017 Feb;23(2):213-222. doi: 10.1038/nm.4257. Epub 2016 Dec 26.

4.

Distinct cortical and striatal actions of a β-arrestin-biased dopamine D2 receptor ligand reveal unique antipsychotic-like properties.

Urs NM, Gee SM, Pack TF, McCorvy JD, Evron T, Snyder JC, Yang X, Rodriguiz RM, Borrelli E, Wetsel WC, Jin J, Roth BL, O'Donnell P, Caron MG.

Proc Natl Acad Sci U S A. 2016 Dec 13;113(50):E8178-E8186. Epub 2016 Dec 1.

5.

Structure-based discovery of opioid analgesics with reduced side effects.

Manglik A, Lin H, Aryal DK, McCorvy JD, Dengler D, Corder G, Levit A, Kling RC, Bernat V, Hübner H, Huang XP, Sassano MF, Giguère PM, Löber S, Da Duan, Scherrer G, Kobilka BK, Gmeiner P, Roth BL, Shoichet BK.

Nature. 2016 Sep 8;537(7619):185-190. doi: 10.1038/nature19112. Epub 2016 Aug 17.

6.

Development of CNS multi-receptor ligands: Modification of known D2 pharmacophores.

Etukala JR, Zhu XY, Eyunni SV, Onyameh EK, Ofori E, Bricker BA, Kang HJ, Huang XP, Roth BL, Ablordeppey SY.

Bioorg Med Chem. 2016 Aug 15;24(16):3671-9. doi: 10.1016/j.bmc.2016.06.011. Epub 2016 Jun 4.

7.

Design and synthesis of dual 5-HT1A and 5-HT7 receptor ligands.

Ofori E, Zhu XY, Etukala JR, Peprah K, Jordan KR, Adkins AA, Bricker BA, Kang HJ, Huang XP, Roth BL, Ablordeppey SY.

Bioorg Med Chem. 2016 Aug 15;24(16):3464-71. doi: 10.1016/j.bmc.2016.05.053. Epub 2016 May 27.

8.

Morphine paradoxically prolongs neuropathic pain in rats by amplifying spinal NLRP3 inflammasome activation.

Grace PM, Strand KA, Galer EL, Urban DJ, Wang X, Baratta MV, Fabisiak TJ, Anderson ND, Cheng K, Greene LI, Berkelhammer D, Zhang Y, Ellis AL, Yin HH, Campeau S, Rice KC, Roth BL, Maier SF, Watkins LR.

Proc Natl Acad Sci U S A. 2016 Jun 14;113(24):E3441-50. doi: 10.1073/pnas.1602070113. Epub 2016 May 31.

9.

σ1 receptor ligands control a switch between passive and active threat responses.

Rennekamp AJ, Huang XP, Wang Y, Patel S, Lorello PJ, Cade L, Gonzales AP, Yeh JR, Caldarone BJ, Roth BL, Kokel D, Peterson RT.

Nat Chem Biol. 2016 Jul;12(7):552-8. doi: 10.1038/nchembio.2089. Epub 2016 May 30.

10.

Zebrafish behavioral profiling identifies multitarget antipsychotic-like compounds.

Bruni G, Rennekamp AJ, Velenich A, McCarroll M, Gendelev L, Fertsch E, Taylor J, Lakhani P, Lensen D, Evron T, Lorello PJ, Huang XP, Kolczewski S, Carey G, Caldarone BJ, Prinssen E, Roth BL, Keiser MJ, Peterson RT, Kokel D.

Nat Chem Biol. 2016 Jul;12(7):559-66. doi: 10.1038/nchembio.2097. Epub 2016 May 30.

11.

Cre-dependent DREADD (Designer Receptors Exclusively Activated by Designer Drugs) mice.

Zhu H, Aryal DK, Olsen RH, Urban DJ, Swearingen A, Forbes S, Roth BL, Hochgeschwender U.

Genesis. 2016 Aug;54(8):439-46. doi: 10.1002/dvg.22949. Epub 2016 Jun 3.

12.

A Miniaturized Screen of a Schistosoma mansoni Serotonergic G Protein-Coupled Receptor Identifies Novel Classes of Parasite-Selective Inhibitors.

Chan JD, McCorvy JD, Acharya S, Johns ME, Day TA, Roth BL, Marchant JS.

PLoS Pathog. 2016 May 17;12(5):e1005651. doi: 10.1371/journal.ppat.1005651. eCollection 2016 May.

13.

In Vitro and In Vivo Characterization of the Alkaloid Nuciferine.

Farrell MS, McCorvy JD, Huang XP, Urban DJ, White KL, Giguere PM, Doak AK, Bernstein AI, Stout KA, Park SM, Rodriguiz RM, Gray BW, Hyatt WS, Norwood AP, Webster KA, Gannon BM, Miller GW, Porter JH, Shoichet BK, Fantegrossi WE, Wetsel WC, Roth BL.

PLoS One. 2016 Mar 10;11(3):e0150602. doi: 10.1371/journal.pone.0150602. eCollection 2016.

14.

DREADDs for Neuroscientists.

Roth BL.

Neuron. 2016 Feb 17;89(4):683-94. doi: 10.1016/j.neuron.2016.01.040. Review.

15.

New Technologies for Elucidating Opioid Receptor Function.

Bruchas MR, Roth BL.

Trends Pharmacol Sci. 2016 Apr;37(4):279-89. doi: 10.1016/j.tips.2016.01.001. Epub 2016 Jan 29. Review.

16.

A cellular chemical probe targeting the chromodomains of Polycomb repressive complex 1.

Stuckey JI, Dickson BM, Cheng N, Liu Y, Norris JL, Cholensky SH, Tempel W, Qin S, Huber KG, Sagum C, Black K, Li F, Huang XP, Roth BL, Baughman BM, Senisterra G, Pattenden SG, Vedadi M, Brown PJ, Bedford MT, Min J, Arrowsmith CH, James LI, Frye SV.

Nat Chem Biol. 2016 Mar;12(3):180-7. doi: 10.1038/nchembio.2007. Epub 2016 Jan 25.

17.

Allosteric ligands for the pharmacologically dark receptors GPR68 and GPR65.

Huang XP, Karpiak J, Kroeze WK, Zhu H, Chen X, Moy SS, Saddoris KA, Nikolova VD, Farrell MS, Wang S, Mangano TJ, Deshpande DA, Jiang A, Penn RB, Jin J, Koller BH, Kenakin T, Shoichet BK, Roth BL.

Nature. 2015 Nov 26;527(7579):477-83. doi: 10.1038/nature15699. Epub 2015 Nov 9.

18.

Elucidation of The Behavioral Program and Neuronal Network Encoded by Dorsal Raphe Serotonergic Neurons.

Urban DJ, Zhu H, Marcinkiewcz CA, Michaelides M, Oshibuchi H, Rhea D, Aryal DK, Farrell MS, Lowery-Gionta E, Olsen RH, Wetsel WC, Kash TL, Hurd YL, Tecott LH, Roth BL.

Neuropsychopharmacology. 2016 Apr;41(5):1404-15. doi: 10.1038/npp.2015.293. Epub 2015 Sep 18.

19.

NMR structure and dynamics of the agonist dynorphin peptide bound to the human kappa opioid receptor.

O'Connor C, White KL, Doncescu N, Didenko T, Roth BL, Czaplicki G, Stevens RC, Wüthrich K, Milon A.

Proc Natl Acad Sci U S A. 2015 Sep 22;112(38):11852-7. doi: 10.1073/pnas.1510117112. Epub 2015 Sep 8.

20.

Re-exploring the N-phenylpicolinamide derivatives to develop mGlu4 ligands with improved affinity and in vitro microsomal stability.

Zhang Z, Kil KE, Poutiainen P, Choi JK, Kang HJ, Huang XP, Roth BL, Brownell AL.

Bioorg Med Chem Lett. 2015 Sep 15;25(18):3956-60. doi: 10.1016/j.bmcl.2015.07.031. Epub 2015 Jul 17.

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