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Items: 1 to 50 of 118

1.

Ghrelin receptor antagonism of hyperlocomotion in cocaine-sensitized mice requires βarrestin-2.

Toth K, Slosky LM, Pack TF, Urs NM, Boone P, Mao L, Abraham D, Caron MG, Barak LS.

Synapse. 2018 Jan;72(1). doi: 10.1002/syn.22012. Epub 2017 Oct 7.

2.

Design, synthesis and biological evaluation of GPR55 agonists.

Fakhouri L, Cook CD, Al-Huniti MH, Console-Bram LM, Hurst DP, Spano MBS, Nasrallah DJ, Caron MG, Barak LS, Reggio PH, Abood ME, Croatt MP.

Bioorg Med Chem. 2017 Aug 15;25(16):4355-4367. doi: 10.1016/j.bmc.2017.06.016. Epub 2017 Jun 13.

3.

Inhibiting clathrin-mediated endocytosis of the leucine-rich G protein-coupled receptor-5 diminishes cell fitness.

Snyder JC, Rochelle LK, Ray C, Pack TF, Bock CB, Lubkov V, Lyerly HK, Waggoner AS, Barak LS, Caron MG.

J Biol Chem. 2017 Apr 28;292(17):7208-7222. doi: 10.1074/jbc.M116.756635. Epub 2017 Mar 8.

4.

Protamine is an antagonist of apelin receptor, and its activity is reversed by heparin.

Le Gonidec S, Chaves-Almagro C, Bai Y, Kang HJ, Smith A, Wanecq E, Huang XP, Prats H, Knibiehler B, Roth BL, Barak LS, Caron MG, Valet P, Audigier Y, Masri B.

FASEB J. 2017 Jun;31(6):2507-2519. doi: 10.1096/fj.201601074R. Epub 2017 Feb 27.

5.

Benzimidazole inhibitors from the Niclosamide chemotype inhibit Wnt/β-catenin signaling with selectivity over effects on ATP homeostasis.

Mook RA Jr, Ren XR, Wang J, Piao H, Barak LS, Kim Lyerly H, Chen W.

Bioorg Med Chem. 2017 Mar 15;25(6):1804-1816. doi: 10.1016/j.bmc.2017.01.046. Epub 2017 Feb 3.

6.

Probing the Allosteric Role of the α5 Subunit of α3β4α5 Nicotinic Acetylcholine Receptors by Functionally Selective Modulators and Ligands.

Ray C, Soderblom EJ, Bai Y, Carroll FI, Caron MG, Barak LS.

ACS Chem Biol. 2017 Mar 17;12(3):702-714. doi: 10.1021/acschembio.6b01117. Epub 2017 Jan 24.

7.

ML314: A Biased Neurotensin Receptor Ligand for Methamphetamine Abuse.

Barak LS, Bai Y, Peterson S, Evron T, Urs NM, Peddibhotla S, Hedrick MP, Hershberger P, Maloney PR, Chung TD, Rodriguiz RM, Wetsel WC, Thomas JB, Hanson GR, Pinkerton AB, Caron MG.

ACS Chem Biol. 2016 Jul 15;11(7):1880-90. doi: 10.1021/acschembio.6b00291. Epub 2016 May 5.

8.

Design, synthesis, and analysis of antagonists of GPR55: Piperidine-substituted 1,3,4-oxadiazol-2-ones.

Meza-Aviña ME, Lingerfelt MA, Console-Bram LM, Gamage TF, Sharir H, Gettys KE, Hurst DP, Kotsikorou E, Shore DM, Caron MG, Rao N, Barak LS, Abood ME, Reggio PH, Croatt MP.

Bioorg Med Chem Lett. 2016 Apr 1;26(7):1827-1830. doi: 10.1016/j.bmcl.2016.02.030. Epub 2016 Feb 16.

9.

A rapid and affordable screening platform for membrane protein trafficking.

Snyder JC, Pack TF, Rochelle LK, Chakraborty SK, Zhang M, Eaton AW, Bai Y, Ernst LA, Barak LS, Waggoner AS, Caron MG.

BMC Biol. 2015 Dec 17;13:107. doi: 10.1186/s12915-015-0216-3.

10.

Structure-activity studies of Wnt/β-catenin inhibition in the Niclosamide chemotype: Identification of derivatives with improved drug exposure.

Mook RA Jr, Wang J, Ren XR, Chen M, Spasojevic I, Barak LS, Lyerly HK, Chen W.

Bioorg Med Chem. 2015 Sep 1;23(17):5829-38. doi: 10.1016/j.bmc.2015.07.001. Epub 2015 Aug 10.

11.

Perhexiline promotes HER3 ablation through receptor internalization and inhibits tumor growth.

Ren XR, Wang J, Osada T, Mook RA Jr, Morse MA, Barak LS, Lyerly HK, Chen W.

Breast Cancer Res. 2015 Feb 15;17:20. doi: 10.1186/s13058-015-0528-9.

12.

Lgr4 and Lgr5 drive the formation of long actin-rich cytoneme-like membrane protrusions.

Snyder JC, Rochelle LK, Marion S, Lyerly HK, Barak LS, Caron MG.

J Cell Sci. 2015 Mar 15;128(6):1230-40. doi: 10.1242/jcs.166322. Epub 2015 Feb 4.

13.

Phenotypic regulation of the sphingosine 1-phosphate receptor miles apart by G protein-coupled receptor kinase 2.

Burczyk M, Burkhalter MD, Blätte T, Matysik S, Caron MG, Barak LS, Philipp M.

Biochemistry. 2015 Jan 27;54(3):765-75. doi: 10.1021/bi501061h. Epub 2015 Jan 15.

14.

G Protein and β-arrestin signaling bias at the ghrelin receptor.

Evron T, Peterson SM, Urs NM, Bai Y, Rochelle LK, Caron MG, Barak LS.

J Biol Chem. 2014 Nov 28;289(48):33442-55. doi: 10.1074/jbc.M114.581397. Epub 2014 Sep 26.

15.

IL-6/STAT3 promotes regeneration of airway ciliated cells from basal stem cells.

Tadokoro T, Wang Y, Barak LS, Bai Y, Randell SH, Hogan BL.

Proc Natl Acad Sci U S A. 2014 Sep 2;111(35):E3641-9. doi: 10.1073/pnas.1409781111. Epub 2014 Aug 18.

16.

Discovery of ML314, a Brain Penetrant Non-Peptidic β-Arrestin Biased Agonist of the Neurotensin NTR1 Receptor.

Peddibhotla S, Hedrick MP, Hershberger P, Maloney PR, Li Y, Milewski M, Gosalia P, Gray W, Mehta A, Sugarman E, Hood B, Suyama E, Nguyen K, Heynen-Genel S, Vasile S, Salaniwal S, Stonich D, Su Y, Mangravita-Novo A, Vicchiarelli M, Roth GP, Smith LH, Chung TD, Hanson GR, Thomas JB, Caron MG, Barak LS, Pinkerton AB.

ACS Med Chem Lett. 2013 Jul 20;4(9):846-851.

17.

The stem cell-expressed receptor Lgr5 possesses canonical and functionally active molecular determinants critical to β-arrestin-2 recruitment.

Snyder JC, Rochelle LK, Barak LS, Caron MG.

PLoS One. 2013 Dec 27;8(12):e84476. doi: 10.1371/journal.pone.0084476. eCollection 2013. Erratum in: PLoS One. 2014;9(1). doi:10.1371/annotation/7f83735d-53d4-42f3-b3b2-b05dd5db059c.

18.

Imidazole-derived agonists for the neurotensin 1 receptor.

Hershberger PM, Hedrick MP, Peddibhotla S, Mangravita-Novo A, Gosalia P, Li Y, Gray W, Vicchiarelli M, Smith LH, Chung TD, Thomas JB, Caron MG, Pinkerton AB, Barak LS, Roth GP.

Bioorg Med Chem Lett. 2014 Jan 1;24(1):262-7. doi: 10.1016/j.bmcl.2013.11.026. Epub 2013 Nov 21.

19.

Identification of the GPR55 antagonist binding site using a novel set of high-potency GPR55 selective ligands.

Kotsikorou E, Sharir H, Shore DM, Hurst DP, Lynch DL, Madrigal KE, Heynen-Genel S, Milan LB, Chung TD, Seltzman HH, Bai Y, Caron MG, Barak LS, Croatt MP, Abood ME, Reggio PH.

Biochemistry. 2013 Dec 31;52(52):9456-69. doi: 10.1021/bi4008885. Epub 2013 Dec 17.

20.

Triphenylmethane dye activation of beta-arrestin.

Barak LS, Bai Y, Snyder JC, Wang J, Chen W, Caron MG.

Biochemistry. 2013 Aug 13;52(32):5403-14. doi: 10.1021/bi400217r. Epub 2013 Aug 1.

21.

Novel adamantyl cannabinoids as CB1 receptor probes.

Thakur GA, Bajaj S, Paronis C, Peng Y, Bowman AL, Barak LS, Caron MG, Parrish D, Deschamps JR, Makriyannis A.

J Med Chem. 2013 May 23;56(10):3904-21. doi: 10.1021/jm4000775. Epub 2013 May 14.

22.

Small molecule modulators of Wnt/β-catenin signaling.

Mook RA Jr, Chen M, Lu J, Barak LS, Lyerly HK, Chen W.

Bioorg Med Chem Lett. 2013 Apr 1;23(7):2187-91. doi: 10.1016/j.bmcl.2013.01.101. Epub 2013 Jan 30.

23.

Constitutive internalization of the leucine-rich G protein-coupled receptor-5 (LGR5) to the trans-Golgi network.

Snyder JC, Rochelle LK, Lyerly HK, Caron MG, Barak LS.

J Biol Chem. 2013 Apr 12;288(15):10286-97. doi: 10.1074/jbc.M112.447540. Epub 2013 Feb 25.

24.

The intestinal glucose-apelin cycle controls carbohydrate absorption in mice.

Dray C, Sakar Y, Vinel C, Daviaud D, Masri B, Garrigues L, Wanecq E, Galvani S, Negre-Salvayre A, Barak LS, Monsarrat B, Burlet-Schiltz O, Valet P, Castan-Laurell I, Ducroc R.

Gastroenterology. 2013 Apr;144(4):771-80. doi: 10.1053/j.gastro.2013.01.004. Epub 2013 Jan 10.

25.

Identification of a novel Smoothened antagonist that potently suppresses Hedgehog signaling.

Wang J, Mook RA Jr, Lu J, Gooden DM, Ribeiro A, Guo A, Barak LS, Lyerly HK, Chen W.

Bioorg Med Chem. 2012 Nov 15;20(22):6751-7. doi: 10.1016/j.bmc.2012.09.030. Epub 2012 Sep 23.

26.

BRET biosensors to study GPCR biology, pharmacology, and signal transduction.

Salahpour A, Espinoza S, Masri B, Lam V, Barak LS, Gainetdinov RR.

Front Endocrinol (Lausanne). 2012 Aug 29;3:105. doi: 10.3389/fendo.2012.00105. eCollection 2012.

27.

Selective GPR35 Antagonists - Probe 3.

Heynen-Genel S, Dahl R, Shi S, Sauer M, Hariharan S, Sergienko E, Dad S, Chung TDY, Stonich D, Su Y, Zhao P, Caron MG, Abood ME, Barak LS.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2011 Mar 29 [updated 2011 Nov 21].

28.

Discovery of Small Molecule Kappa Opioid Receptor Agonist and Antagonist Chemotypes through a HTS and Hit Refinement Strategy.

Frankowski KJ, Hedrick MP, Gosalia P, Li K, Shi S, Whipple D, Ghosh P, Prisinzano TE, Schoenen FJ, Su Y, Vasile S, Sergienko E, Gray W, Hariharan S, Milan L, Heynen-Genel S, Mangravita-Novo A, Vicchiarelli M, Smith LH, Streicher JM, Caron MG, Barak LS, Bohn LM, Chung TD, Aubé J.

ACS Chem Neurosci. 2012 Mar 21;3(3):221-236. Epub 2012 Jan 20.

29.

Polyclonal HER2-specific antibodies induced by vaccination mediate receptor internalization and degradation in tumor cells.

Ren XR, Wei J, Lei G, Wang J, Lu J, Xia W, Spector N, Barak LS, Clay TM, Osada T, Hamilton E, Blackwell K, Hobeika AC, Morse MA, Lyerly HK, Chen W.

Breast Cancer Res. 2012 Jun 7;14(3):R89.

30.

The insecticide synergist piperonyl butoxide inhibits hedgehog signaling: assessing chemical risks.

Wang J, Lu J, Mook RA Jr, Zhang M, Zhao S, Barak LS, Freedman JH, Lyerly HK, Chen W.

Toxicol Sci. 2012 Aug;128(2):517-23. doi: 10.1093/toxsci/kfs165. Epub 2012 May 1.

31.

Modeling of bias for the analysis of receptor signaling in biochemical systems.

Barak LS, Peterson S.

Biochemistry. 2012 Feb 14;51(6):1114-25. doi: 10.1021/bi201308s. Epub 2012 Feb 2.

32.

Glucocorticoid hedgehog agonists in neurogenesis.

Wang J, Barak LS, Mook RA Jr, Chen W.

Vitam Horm. 2011;87:207-15. doi: 10.1016/B978-0-12-386015-6.00030-5. Review.

PMID:
22127244
33.

Screening for Selective Ligands for GPR55 - Antagonists.

Heynen-Genel S, Dahl R, Shi S, Milan L, Hariharan S, Sergienko E, Hedrick M, Dad S, Stonich D, Su Y, Vicchiarelli M, Mangravita-Novo A, Smith LH, Chung TDY, Sharir H, Caron MG, Barak LS, Abood ME.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2010 Oct 30 [updated 2011 May 26].

34.

Screening for Selective Ligands for GPR55 - Agonists.

Heynen-Genel S, Dahl R, Shi S, Milan L, Hariharan S, Bravo Y, Sergienko E, Hedrick M, Dad S, Stonich D, Su Y, Vicchiarelli M, Mangravita-Novo A, Smith LH, Chung TDY, Sharir H, Barak LS, Abood ME.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2010 Sep 29 [updated 2011 May 26].

35.

Antagonist for the Kappa Opioid Receptor.

Hedrick MP, Gosalia P, Li K, Frankowski KJ, Shi S, Prisinzano TE, Schoenen F, Aubé J, Su Y, Stonich D, Vasile S, Sergienko E, Gray W, Hariharan S, Milan L, Heynen-Genel S, Vicchiarelli M, Mangravita-Novo A, Streicher JM, Smith LH, Chung TDY, Caron M, Bohn LM, Barak LS.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2010 Oct 31 [updated 2011 May 26].

36.

Visualizing receptor endocytosis and trafficking.

Salahpour A, Barak LS.

Methods Mol Biol. 2011;756:311-23. doi: 10.1007/978-1-61779-160-4_18.

PMID:
21870235
37.

Functional interaction between trace amine-associated receptor 1 and dopamine D2 receptor.

Espinoza S, Salahpour A, Masri B, Sotnikova TD, Messa M, Barak LS, Caron MG, Gainetdinov RR.

Mol Pharmacol. 2011 Sep;80(3):416-25. doi: 10.1124/mol.111.073304. Epub 2011 Jun 13.

38.

Selective GPR35 Antagonists - Probes 1 & 2.

Heynen-Genel S, Dahl R, Shi S, Sauer M, Hariharan S, Sergienko E, Dad S, Chung TDY, Stonich D, Su Y, Caron M, Zhao P, Abood ME, Barak LS.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2010 Feb 28 [updated 2010 Oct 4].

39.

Selective KOP Receptor Agonists: Probe 1 & Probe 2.

Hedrick MP, Gosalia P, Frankowski K, Shi S, Prisinzano TE, Schoenen F, Aubé J, Su Y, Vasile S, Sergienko E, Gray W, Hariharan S, Ghosh P, Milan L, Heynen-Genel S, Chung TDY, Dad S, Caron M, Bohn LM, Barak LS.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2010 Feb 28 [updated 2010 Oct 4].

40.

Selective KOP Receptor Antagonists: Probe 1.

Hedrick MP, Gosalia P, Frankowski K, Whipple DA, Shi S, Prisinzano TE, Schoenen F, Aubé J, Su Y, Vasile S, Sergienko E, Gray W, Hariharan S, Milan L, Heynen-Genel S, Chung TDY, Dad S, Caron M, Bohn LM, Barak LS.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2010 Feb 28 [updated 2010 Oct 4].

41.

The dopamine metabolite 3-methoxytyramine is a neuromodulator.

Sotnikova TD, Beaulieu JM, Espinoza S, Masri B, Zhang X, Salahpour A, Barak LS, Caron MG, Gainetdinov RR.

PLoS One. 2010 Oct 18;5(10):e13452. doi: 10.1371/journal.pone.0013452. Erratum in: PLoS One. 2010;5(10) doi: 10.1371/annotation/a2019934-b1cc-4781-80cb-9e09fc7ff6dc..

42.

Targeting of the orphan receptor GPR35 by pamoic acid: a potent activator of extracellular signal-regulated kinase and β-arrestin2 with antinociceptive activity.

Zhao P, Sharir H, Kapur A, Cowan A, Geller EB, Adler MW, Seltzman HH, Reggio PH, Heynen-Genel S, Sauer M, Chung TD, Bai Y, Chen W, Caron MG, Barak LS, Abood ME.

Mol Pharmacol. 2010 Oct;78(4):560-8. doi: 10.1124/mol.110.066746. Epub 2010 Jul 22.

43.

Development of small molecules targeting the Wnt pathway for the treatment of colon cancer: a high-throughput screening approach.

Chen W, Chen M, Barak LS.

Am J Physiol Gastrointest Liver Physiol. 2010 Aug;299(2):G293-300. doi: 10.1152/ajpgi.00005.2010. Epub 2010 May 27. Review.

44.

Identification of select glucocorticoids as Smoothened agonists: potential utility for regenerative medicine.

Wang J, Lu J, Bond MC, Chen M, Ren XR, Lyerly HK, Barak LS, Chen W.

Proc Natl Acad Sci U S A. 2010 May 18;107(20):9323-8. doi: 10.1073/pnas.0910712107. Epub 2010 May 3.

45.

The anti-helminthic niclosamide inhibits Wnt/Frizzled1 signaling.

Chen M, Wang J, Lu J, Bond MC, Ren XR, Lyerly HK, Barak LS, Chen W.

Biochemistry. 2009 Nov 3;48(43):10267-74. doi: 10.1021/bi9009677.

46.

Atypical responsiveness of the orphan receptor GPR55 to cannabinoid ligands.

Kapur A, Zhao P, Sharir H, Bai Y, Caron MG, Barak LS, Abood ME.

J Biol Chem. 2009 Oct 23;284(43):29817-27. doi: 10.1074/jbc.M109.050187. Epub 2009 Sep 1.

47.

Smoothened signaling in vertebrates is facilitated by a G protein-coupled receptor kinase.

Philipp M, Fralish GB, Meloni AR, Chen W, MacInnes AW, Barak LS, Caron MG.

Mol Biol Cell. 2008 Dec;19(12):5478-89. doi: 10.1091/mbc.E08-05-0448. Epub 2008 Sep 24.

48.

Regulation of M2-type pyruvate kinase mediated by the high-affinity IgE receptors is required for mast cell degranulation.

Ryu H, Walker JK, Kim S, Koo N, Barak LS, Noguchi T, Kang BY, Kim KM.

Br J Pharmacol. 2008 Jul;154(5):1035-46. doi: 10.1038/bjp.2008.148. Epub 2008 Apr 21.

49.

Pharmacological characterization of membrane-expressed human trace amine-associated receptor 1 (TAAR1) by a bioluminescence resonance energy transfer cAMP biosensor.

Barak LS, Salahpour A, Zhang X, Masri B, Sotnikova TD, Ramsey AJ, Violin JD, Lefkowitz RJ, Caron MG, Gainetdinov RR.

Mol Pharmacol. 2008 Sep;74(3):585-594. doi: 10.1124/mol.108.048884. Epub 2008 Jun 4.

50.

Ubiquitination of beta-arrestin links seven-transmembrane receptor endocytosis and ERK activation.

Shenoy SK, Barak LS, Xiao K, Ahn S, Berthouze M, Shukla AK, Luttrell LM, Lefkowitz RJ.

J Biol Chem. 2007 Oct 5;282(40):29549-62. Epub 2007 Jul 31.

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