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Items: 1 to 50 of 222

1.

Signalling profiles of a structurally diverse panel of synthetic cannabinoid receptor agonists.

Patel M, Manning JJ, Finlay DB, Javitch JA, Banister SD, Grimsey NL, Glass M.

Biochem Pharmacol. 2020 Feb 21;175:113871. doi: 10.1016/j.bcp.2020.113871. [Epub ahead of print]

PMID:
32088263
2.

X-ray structure of LeuT in an inward-facing occluded conformation reveals mechanism of substrate release.

Gotfryd K, Boesen T, Mortensen JS, Khelashvili G, Quick M, Terry DS, Missel JW, LeVine MV, Gourdon P, Blanchard SC, Javitch JA, Weinstein H, Loland CJ, Nissen P, Gether U.

Nat Commun. 2020 Feb 21;11(1):1005. doi: 10.1038/s41467-020-14735-w.

3.

Author Correction: Quantifying secondary transport at single-molecule resolution.

Fitzgerald GA, Terry DS, Warren AL, Quick M, Javitch JA, Blanchard SC.

Nature. 2020 Mar;579(7797):E6. doi: 10.1038/s41586-020-2029-y.

PMID:
32076274
4.

Distinct inactive conformations of the dopamine D2 and D3 receptors correspond to different extents of inverse agonism.

Lane JR, Abramyan AM, Adhikari P, Keen AC, Lee KH, Sanchez J, Verma RK, Lim HD, Yano H, Javitch JA, Shi L.

Elife. 2020 Jan 27;9. pii: e52189. doi: 10.7554/eLife.52189.

5.

Detection of G Protein-Coupled Receptor Complexes in Postmortem Human Brain by Proximity Ligation Assay.

Zhu Y, Dwork AJ, Trifilieff P, Javitch JA.

Curr Protoc Neurosci. 2020 Mar;91(1):e86. doi: 10.1002/cpns.86.

PMID:
31943888
6.

Dopamine D2 receptor overexpression in the nucleus accumbens core induces robust weight loss during scheduled fasting selectively in female mice.

Welch AC, Zhang J, Lyu J, McMurray MS, Javitch JA, Kellendonk C, Dulawa SC.

Mol Psychiatry. 2019 Dec 20. doi: 10.1038/s41380-019-0633-8. [Epub ahead of print]

PMID:
31863019
7.

Detecting G protein-coupled receptor complexes in postmortem human brain with proximity ligation assay and a Bayesian classifier.

Zhu Y, Mészáros J, Walle R, Fan R, Sun Z, Dwork AJ, Trifilieff P, Javitch JA.

Biotechniques. 2020 Mar;68(3):122-129. doi: 10.2144/btn-2019-0083. Epub 2019 Dec 20.

8.

Role of Tau Protein in Remodeling of Circadian Neuronal Circuits and Sleep.

Arnes M, Alaniz ME, Karam CS, Cho JD, Lopez G, Javitch JA, Santa-Maria I.

Front Aging Neurosci. 2019 Nov 21;11:320. doi: 10.3389/fnagi.2019.00320. eCollection 2019.

9.

Measuring the effects of ketamine on mGluR5 using [18F]FPEB and PET.

Holmes SE, Gallezot JD, Davis MT, DellaGioia N, Matuskey D, Nabulsi N, Krystal JH, Javitch JA, DeLorenzo C, Carson RE, Esterlis I.

J Cereb Blood Flow Metab. 2019 Nov 19:271678X19886316. doi: 10.1177/0271678X19886316. [Epub ahead of print] No abstract available.

PMID:
31744389
10.

Quantifying secondary transport at single-molecule resolution.

Fitzgerald GA, Terry DS, Warren AL, Quick M, Javitch JA, Blanchard SC.

Nature. 2019 Nov;575(7783):528-534. doi: 10.1038/s41586-019-1747-5. Epub 2019 Nov 13. Erratum in: Nature. 2020 Mar;579(7797):E6.

PMID:
31723269
11.

Do Toxic Synthetic Cannabinoid Receptor Agonists Have Signature in Vitro Activity Profiles? A Case Study of AMB-FUBINACA.

Finlay DB, Manning JJ, Ibsen MS, Macdonald CE, Patel M, Javitch JA, Banister SD, Glass M.

ACS Chem Neurosci. 2019 Oct 16;10(10):4350-4360. doi: 10.1021/acschemneuro.9b00429. Epub 2019 Sep 24.

PMID:
31513380
12.

Molecular Determinants of the Intrinsic Efficacy of the Antipsychotic Aripiprazole.

Klein Herenbrink C, Verma R, Lim HD, Kopinathan A, Keen A, Shonberg J, Draper-Joyce CJ, Scammells PJ, Christopoulos A, Javitch JA, Capuano B, Shi L, Lane JR.

ACS Chem Biol. 2019 Aug 16;14(8):1780-1792. doi: 10.1021/acschembio.9b00342. Epub 2019 Aug 5.

PMID:
31339684
13.

The allosteric mechanism of substrate-specific transport in SLC6 is mediated by a volumetric sensor.

LeVine MV, Terry DS, Khelashvili G, Siegel ZS, Quick M, Javitch JA, Blanchard SC, Weinstein H.

Proc Natl Acad Sci U S A. 2019 Aug 6;116(32):15947-15956. doi: 10.1073/pnas.1903020116. Epub 2019 Jul 19.

14.

Genetically Targeted Optical Control of an Endogenous G Protein-Coupled Receptor.

Donthamsetti PC, Broichhagen J, Vyklicky V, Stanley C, Fu Z, Visel M, Levitz JL, Javitch JA, Trauner D, Isacoff EY.

J Am Chem Soc. 2019 Jul 24;141(29):11522-11530. doi: 10.1021/jacs.9b02895. Epub 2019 Jul 10.

PMID:
31291105
15.

7-Hydroxymitragynine Is an Active Metabolite of Mitragynine and a Key Mediator of Its Analgesic Effects.

Kruegel AC, Uprety R, Grinnell SG, Langreck C, Pekarskaya EA, Le Rouzic V, Ansonoff M, Gassaway MM, Pintar JE, Pasternak GW, Javitch JA, Majumdar S, Sames D.

ACS Cent Sci. 2019 Jun 26;5(6):992-1001. doi: 10.1021/acscentsci.9b00141. Epub 2019 May 29.

16.

Come Fly with Me: An overview of dopamine receptors in Drosophila melanogaster.

Karam CS, Jones SK, Javitch JA.

Basic Clin Pharmacol Toxicol. 2019 Jun 20. doi: 10.1111/bcpt.13277. [Epub ahead of print] Review.

PMID:
31219669
17.

Cannabinoid CB1 and CB2 Receptor-Mediated Arrestin Translocation: Species, Subtype, and Agonist-Dependence.

Ibsen MS, Finlay DB, Patel M, Javitch JA, Glass M, Grimsey NL.

Front Pharmacol. 2019 Apr 10;10:350. doi: 10.3389/fphar.2019.00350. eCollection 2019.

18.

The differential actions of clozapine and other antipsychotic drugs on the translocation of dopamine D2 receptors to the cell surface.

Schrader JM, Irving CM, Octeau JC, Christian JA, Aballo TJ, Kareemo DJ, Conti J, Camberg JL, Lane JR, Javitch JA, Kovoor A.

J Biol Chem. 2019 Apr 5;294(14):5604-5615. doi: 10.1074/jbc.RA118.004682. Epub 2019 Jan 22.

19.

New roles for dopamine D2 and D3 receptors in pancreatic beta cell insulin secretion.

Farino ZJ, Morgenstern TJ, Maffei A, Quick M, De Solis AJ, Wiriyasermkul P, Freyberg RJ, Aslanoglou D, Sorisio D, Inbar BP, Free RB, Donthamsetti P, Mosharov EV, Kellendonk C, Schwartz GJ, Sibley DR, Schmauss C, Zeltser LM, Moore H, Harris PE, Javitch JA, Freyberg Z.

Mol Psychiatry. 2019 Jan 9. doi: 10.1038/s41380-018-0344-6. [Epub ahead of print]

20.

Reply to 'Antipsychotics with similar association kinetics at dopamine D2 receptors differ in extrapyramidal side-effects'.

Sykes DA, Lane JR, Szabo M, Capuano B, Javitch JA, Charlton SJ.

Nat Commun. 2018 Sep 3;9(1):3568. doi: 10.1038/s41467-018-05678-4. No abstract available.

21.

Arrestin recruitment to dopamine D2 receptor mediates locomotion but not incentive motivation.

Donthamsetti P, Gallo EF, Buck DC, Stahl EL, Zhu Y, Lane JR, Bohn LM, Neve KA, Kellendonk C, Javitch JA.

Mol Psychiatry. 2018 Aug 17. doi: 10.1038/s41380-018-0212-4. [Epub ahead of print]

22.

The LeuT-fold neurotransmitter:sodium symporter MhsT has two substrate sites.

Quick M, Abramyan AM, Wiriyasermkul P, Weinstein H, Shi L, Javitch JA.

Proc Natl Acad Sci U S A. 2018 Aug 21;115(34):E7924-E7931. doi: 10.1073/pnas.1717444115. Epub 2018 Aug 6.

23.

Luciferase complementation based-detection of G-protein-coupled receptor activity.

Yano H, Cai NS, Javitch JA, Ferré S.

Biotechniques. 2018 Jul;65(1):9-14. doi: 10.2144/btn-2018-0039.

24.

Exploring Substrate Binding in the Extracellular Vestibule of MhsT by Atomistic Simulations and Markov Models.

Abramyan AM, Quick M, Xue C, Javitch JA, Shi L.

J Chem Inf Model. 2018 Jun 25;58(6):1244-1252. doi: 10.1021/acs.jcim.8b00175. Epub 2018 Jun 11.

25.

Regional Heterogeneity of D2-Receptor Signaling in the Dorsal Striatum and Nucleus Accumbens.

Marcott PF, Gong S, Donthamsetti P, Grinnell SG, Nelson MN, Newman AH, Birnbaumer L, Martemyanov KA, Javitch JA, Ford CP.

Neuron. 2018 May 2;98(3):575-587.e4. doi: 10.1016/j.neuron.2018.03.038. Epub 2018 Apr 12.

26.

Accumbens dopamine D2 receptors increase motivation by decreasing inhibitory transmission to the ventral pallidum.

Gallo EF, Meszaros J, Sherman JD, Chohan MO, Teboul E, Choi CS, Moore H, Javitch JA, Kellendonk C.

Nat Commun. 2018 Mar 14;9(1):1086. doi: 10.1038/s41467-018-03272-2.

27.

Phosphorylation of the Amino Terminus of the Dopamine Transporter: Regulatory Mechanisms and Implications for Amphetamine Action.

Karam CS, Javitch JA.

Adv Pharmacol. 2018;82:205-234. doi: 10.1016/bs.apha.2017.09.002. Epub 2017 Oct 25. Review.

28.

Gs- versus Golf-dependent functional selectivity mediated by the dopamine D1 receptor.

Yano H, Cai NS, Xu M, Verma RK, Rea W, Hoffman AF, Shi L, Javitch JA, Bonci A, Ferré S.

Nat Commun. 2018 Feb 5;9(1):486. doi: 10.1038/s41467-017-02606-w.

29.

The action of a negative allosteric modulator at the dopamine D2 receptor is dependent upon sodium ions.

Draper-Joyce CJ, Verma RK, Michino M, Shonberg J, Kopinathan A, Klein Herenbrink C, Scammells PJ, Capuano B, Abramyan AM, Thal DM, Javitch JA, Christopoulos A, Shi L, Lane JR.

Sci Rep. 2018 Jan 19;8(1):1208. doi: 10.1038/s41598-018-19642-1.

30.

The E2.65A mutation disrupts dynamic binding poses of SB269652 at the dopamine D2 and D3 receptors.

Verma RK, Abramyan AM, Michino M, Free RB, Sibley DR, Javitch JA, Lane JR, Shi L.

PLoS Comput Biol. 2018 Jan 16;14(1):e1005948. doi: 10.1371/journal.pcbi.1005948. eCollection 2018 Jan.

31.

A partially-open inward-facing intermediate conformation of LeuT is associated with Na+ release and substrate transport.

Terry DS, Kolster RA, Quick M, LeVine MV, Khelashvili G, Zhou Z, Weinstein H, Javitch JA, Blanchard SC.

Nat Commun. 2018 Jan 15;9(1):230. doi: 10.1038/s41467-017-02202-y.

32.

The structural determinants of the bitopic binding mode of a negative allosteric modulator of the dopamine D2 receptor.

Draper-Joyce CJ, Michino M, Verma RK, Klein Herenbrink C, Shonberg J, Kopinathan A, Scammells PJ, Capuano B, Thal DM, Javitch JA, Christopoulos A, Shi L, Lane JR.

Biochem Pharmacol. 2018 Feb;148:315-328. doi: 10.1016/j.bcp.2018.01.002. Epub 2018 Jan 9.

33.

Optical Control of Dopamine Receptors Using a Photoswitchable Tethered Inverse Agonist.

Donthamsetti PC, Winter N, Schönberger M, Levitz J, Stanley C, Javitch JA, Isacoff EY, Trauner D.

J Am Chem Soc. 2017 Dec 27;139(51):18522-18535. doi: 10.1021/jacs.7b07659. Epub 2017 Dec 13.

34.

Dopamine D2 Receptors in the Paraventricular Thalamus Attenuate Cocaine Locomotor Sensitization.

Clark AM, Leroy F, Martyniuk KM, Feng W, McManus E, Bailey MR, Javitch JA, Balsam PD, Kellendonk C.

eNeuro. 2017 Oct 24;4(5). pii: ENEURO.0227-17.2017. doi: 10.1523/ENEURO.0227-17.2017. eCollection 2017 Sep-Oct.

35.

Development of novel biosensors to study receptor-mediated activation of the G-protein α subunits Gs and Golf.

Yano H, Provasi D, Cai NS, Filizola M, Ferré S, Javitch JA.

J Biol Chem. 2017 Dec 8;292(49):19989-19998. doi: 10.1074/jbc.M117.800698. Epub 2017 Oct 17.

36.

Extrapyramidal side effects of antipsychotics are linked to their association kinetics at dopamine D2 receptors.

Sykes DA, Moore H, Stott L, Holliday N, Javitch JA, Lane JR, Charlton SJ.

Nat Commun. 2017 Oct 2;8(1):763. doi: 10.1038/s41467-017-00716-z.

37.

Neuronal Depolarization Drives Increased Dopamine Synaptic Vesicle Loading via VGLUT.

Aguilar JI, Dunn M, Mingote S, Karam CS, Farino ZJ, Sonders MS, Choi SJ, Grygoruk A, Zhang Y, Cela C, Choi BJ, Flores J, Freyberg RJ, McCabe BD, Mosharov EV, Krantz DE, Javitch JA, Sulzer D, Sames D, Rayport S, Freyberg Z.

Neuron. 2017 Aug 30;95(5):1074-1088.e7. doi: 10.1016/j.neuron.2017.07.038. Epub 2017 Aug 17.

38.

Single-molecule analysis of ligand efficacy in β2AR-G-protein activation.

Gregorio GG, Masureel M, Hilger D, Terry DS, Juette M, Zhao H, Zhou Z, Perez-Aguilar JM, Hauge M, Mathiasen S, Javitch JA, Weinstein H, Kobilka BK, Blanchard SC.

Nature. 2017 Jul 6;547(7661):68-73. doi: 10.1038/nature22354. Epub 2017 Jun 7.

39.

Phospho-specific antibodies targeting the amino terminus of the human dopamine transporter.

Karam CS, Sen N, Javitch JA.

J Chem Neuroanat. 2017 Oct;83-84:91-98. doi: 10.1016/j.jchemneu.2017.05.003. Epub 2017 May 30.

40.

Electronic tuning of self-healing fluorophores for live-cell and single-molecule imaging.

Zheng Q, Jockusch S, Zhou Z, Altman RB, Zhao H, Asher W, Holsey M, Mathiasen S, Geggier P, Javitch JA, Blanchard SC.

Chem Sci. 2017 Jan 1;8(1):755-762. doi: 10.1039/C6SC02976K. Epub 2016 Sep 7.

41.

The role of transmembrane segment 5 (TM5) in Na2 release and the conformational transition of neurotransmitter:sodium symporters toward the inward-open state.

Stolzenberg S, Li Z, Quick M, Malinauskaite L, Nissen P, Weinstein H, Javitch JA, Shi L.

J Biol Chem. 2017 May 5;292(18):7372-7384. doi: 10.1074/jbc.M116.757153. Epub 2017 Mar 20.

42.

The Behavioral Effects of the Antidepressant Tianeptine Require the Mu-Opioid Receptor.

Samuels BA, Nautiyal KM, Kruegel AC, Levinstein MR, Magalong VM, Gassaway MM, Grinnell SG, Han J, Ansonoff MA, Pintar JE, Javitch JA, Sames D, Hen R.

Neuropsychopharmacology. 2017 Sep;42(10):2052-2063. doi: 10.1038/npp.2017.60. Epub 2017 Mar 17.

43.

Potentiating SLC transporter activity: Emerging drug discovery opportunities.

Rives ML, Javitch JA, Wickenden AD.

Biochem Pharmacol. 2017 Jul 1;135:1-11. doi: 10.1016/j.bcp.2017.02.010. Epub 2017 Feb 16. Review.

PMID:
28214518
44.

Toward Understanding the Structural Basis of Partial Agonism at the Dopamine D3 Receptor.

Michino M, Boateng CA, Donthamsetti P, Yano H, Bakare OM, Bonifazi A, Ellenberger MP, Keck TM, Kumar V, Zhu C, Verma R, Deschamps JR, Javitch JA, Newman AH, Shi L.

J Med Chem. 2017 Jan 26;60(2):580-593. doi: 10.1021/acs.jmedchem.6b01148. Epub 2017 Jan 5.

45.

In vivo variation in same-day estimates of metabotropic glutamate receptor subtype 5 binding using [11C]ABP688 and [18F]FPEB.

DeLorenzo C, Gallezot JD, Gardus J, Yang J, Planeta B, Nabulsi N, Ogden RT, Labaree DC, Huang YH, Mann JJ, Gasparini F, Lin X, Javitch JA, Parsey RV, Carson RE, Esterlis I.

J Cereb Blood Flow Metab. 2017 Aug;37(8):2716-2727. doi: 10.1177/0271678X16673646. Epub 2016 Jan 1.

46.

Conformational Dynamics on the Extracellular Side of LeuT Controlled by Na+ and K+ Ions and the Protonation State of Glu290.

Khelashvili G, Schmidt SG, Shi L, Javitch JA, Gether U, Loland CJ, Weinstein H.

J Biol Chem. 2016 Sep 16;291(38):19786-99. doi: 10.1074/jbc.M116.731455. Epub 2016 Jul 29.

47.

Development and Antiparkinsonian Activity of VU0418506, a Selective Positive Allosteric Modulator of Metabotropic Glutamate Receptor 4 Homomers without Activity at mGlu2/4 Heteromers.

Niswender CM, Jones CK, Lin X, Bubser M, Thompson Gray A, Blobaum AL, Engers DW, Rodriguez AL, Loch MT, Daniels JS, Lindsley CW, Hopkins CR, Javitch JA, Conn PJ.

ACS Chem Neurosci. 2016 Sep 21;7(9):1201-11. doi: 10.1021/acschemneuro.6b00036. Epub 2016 Aug 5.

48.

Synthetic and Receptor Signaling Explorations of the Mitragyna Alkaloids: Mitragynine as an Atypical Molecular Framework for Opioid Receptor Modulators.

Kruegel AC, Gassaway MM, Kapoor A, Váradi A, Majumdar S, Filizola M, Javitch JA, Sames D.

J Am Chem Soc. 2016 Jun 1;138(21):6754-64. doi: 10.1021/jacs.6b00360. Epub 2016 May 18.

49.

Novel Analogues of (R)-5-(Methylamino)-5,6-dihydro-4H-imidazo[4,5,1-ij]quinolin-2(1H)-one (Sumanirole) Provide Clues to Dopamine D2/D3 Receptor Agonist Selectivity.

Zou MF, Keck TM, Kumar V, Donthamsetti P, Michino M, Burzynski C, Schweppe C, Bonifazi A, Free RB, Sibley DR, Janowsky A, Shi L, Javitch JA, Newman AH.

J Med Chem. 2016 Apr 14;59(7):2973-88. doi: 10.1021/acs.jmedchem.5b01612. Epub 2016 Apr 1.

50.

The role of kinetic context in apparent biased agonism at GPCRs.

Klein Herenbrink C, Sykes DA, Donthamsetti P, Canals M, Coudrat T, Shonberg J, Scammells PJ, Capuano B, Sexton PM, Charlton SJ, Javitch JA, Christopoulos A, Lane JR.

Nat Commun. 2016 Feb 24;7:10842. doi: 10.1038/ncomms10842.

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