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Items: 47


Delta opioid receptor agonists are effective for multiple types of headache disorders.

Moye LS, Tipton AF, Dripps I, Sheets Z, Crombie A, Violin JD, Pradhan AA.

Neuropharmacology. 2019 Apr;148:77-86. doi: 10.1016/j.neuropharm.2018.12.017. Epub 2018 Dec 14.


TRV0109101, a G Protein-Biased Agonist of the µ-Opioid Receptor, Does Not Promote Opioid-Induced Mechanical Allodynia following Chronic Administration.

Koblish M, Carr R 3rd, Siuda ER, Rominger DH, Gowen-MacDonald W, Cowan CL, Crombie AL, Violin JD, Lark MW.

J Pharmacol Exp Ther. 2017 Aug;362(2):254-262. doi: 10.1124/jpet.117.241117. Epub 2017 May 22.


Biased mu-opioid receptor ligands: a promising new generation of pain therapeutics.

Siuda ER, Carr R 3rd, Rominger DH, Violin JD.

Curr Opin Pharmacol. 2017 Feb;32:77-84. doi: 10.1016/j.coph.2016.11.007. Epub 2016 Dec 7. Review.


Cardiac myosin light chain phosphorylation and inotropic effects of a biased ligand, TRV120023, in a dilated cardiomyopathy model.

Tarigopula M, Davis RT 3rd, Mungai PT, Ryba DM, Wieczorek DF, Cowan CL, Violin JD, Wolska BM, Solaro RJ.

Cardiovasc Res. 2015 Jul 15;107(2):226-34. doi: 10.1093/cvr/cvv162. Epub 2015 Jun 4.


Heart failure therapeutics on the basis of a biased ligand of the angiotensin-2 type 1 receptor. Rationale and design of the BLAST-AHF study (Biased Ligand of the Angiotensin Receptor Study in Acute Heart Failure).

Felker GM, Butler J, Collins SP, Cotter G, Davison BA, Ezekowitz JA, Filippatos G, Levy PD, Metra M, Ponikowski P, Soergel DG, Teerlink JR, Violin JD, Voors AA, Pang PS.

JACC Heart Fail. 2015 Mar;3(3):193-201. doi: 10.1016/j.jchf.2014.09.008. Epub 2015 Jan 28. Review.


Biased agonism of the μ-opioid receptor by TRV130 increases analgesia and reduces on-target adverse effects versus morphine: A randomized, double-blind, placebo-controlled, crossover study in healthy volunteers.

Soergel DG, Subach RA, Burnham N, Lark MW, James IE, Sadler BM, Skobieranda F, Violin JD, Webster LR.

Pain. 2014 Sep;155(9):1829-35. doi: 10.1016/j.pain.2014.06.011. Epub 2014 Jun 19.


Biased ligands at G-protein-coupled receptors: promise and progress.

Violin JD, Crombie AL, Soergel DG, Lark MW.

Trends Pharmacol Sci. 2014 Jul;35(7):308-16. doi: 10.1016/ Epub 2014 May 28. Review. Erratum in: Trends Pharmacol Sci. 2014 Sep;35(9):489.


Biased ligands: pathway validation for novel GPCR therapeutics.

Rominger DH, Cowan CL, Gowen-MacDonald W, Violin JD.

Curr Opin Pharmacol. 2014 Jun;16:108-15. doi: 10.1016/j.coph.2014.04.002. Epub 2014 May 14. Review.


Divergent transducer-specific molecular efficacies generate biased agonism at a G protein-coupled receptor (GPCR).

Strachan RT, Sun JP, Rominger DH, Violin JD, Ahn S, Rojas Bie Thomsen A, Zhu X, Kleist A, Costa T, Lefkowitz RJ.

J Biol Chem. 2014 May 16;289(20):14211-24. doi: 10.1074/jbc.M114.548131. Epub 2014 Mar 25.


Intramolecular conformational changes optimize protein kinase C signaling.

Antal CE, Violin JD, Kunkel MT, Skovsø S, Newton AC.

Chem Biol. 2014 Apr 24;21(4):459-469. doi: 10.1016/j.chembiol.2014.02.008. Epub 2014 Mar 13.


First clinical experience with TRV130: pharmacokinetics and pharmacodynamics in healthy volunteers.

Soergel DG, Subach RA, Sadler B, Connell J, Marion AS, Cowan CL, Violin JD, Lark MW.

J Clin Pharmacol. 2014 Mar;54(3):351-7. doi: 10.1002/jcph.207. Epub 2014 Jan 28.


Structure-activity relationships and discovery of a G protein biased μ opioid receptor ligand, [(3-methoxythiophen-2-yl)methyl]({2-[(9R)-9-(pyridin-2-yl)-6-oxaspiro-[4.5]decan-9-yl]ethyl})amine (TRV130), for the treatment of acute severe pain.

Chen XT, Pitis P, Liu G, Yuan C, Gotchev D, Cowan CL, Rominger DH, Koblish M, Dewire SM, Crombie AL, Violin JD, Yamashita DS.

J Med Chem. 2013 Oct 24;56(20):8019-31. doi: 10.1021/jm4010829. Epub 2013 Oct 14.


The β-arrestin-biased ligand TRV120023 inhibits angiotensin II-induced cardiac hypertrophy while preserving enhanced myofilament response to calcium.

Monasky MM, Taglieri DM, Henze M, Warren CM, Utter MS, Soergel DG, Violin JD, Solaro RJ.

Am J Physiol Heart Circ Physiol. 2013 Sep 15;305(6):H856-66. doi: 10.1152/ajpheart.00327.2013. Epub 2013 Jul 19.


First clinical experience with TRV027: pharmacokinetics and pharmacodynamics in healthy volunteers.

Soergel DG, Subach RA, Cowan CL, Violin JD, Lark MW.

J Clin Pharmacol. 2013 Sep;53(9):892-9. doi: 10.1002/jcph.111. Epub 2013 Jun 29.


GPCR biased ligands as novel heart failure therapeutics.

Violin JD, Soergel DG, Boerrigter G, Burnett JC Jr, Lark MW.

Trends Cardiovasc Med. 2013 Oct;23(7):242-9. doi: 10.1016/j.tcm.2013.01.002. Epub 2013 Mar 15. Review.


A G protein-biased ligand at the μ-opioid receptor is potently analgesic with reduced gastrointestinal and respiratory dysfunction compared with morphine.

DeWire SM, Yamashita DS, Rominger DH, Liu G, Cowan CL, Graczyk TM, Chen XT, Pitis PM, Gotchev D, Yuan C, Koblish M, Lark MW, Violin JD.

J Pharmacol Exp Ther. 2013 Mar;344(3):708-17. doi: 10.1124/jpet.112.201616. Epub 2013 Jan 8.


β-Arrestin-biased AT1R stimulation promotes cell survival during acute cardiac injury.

Kim KS, Abraham D, Williams B, Violin JD, Mao L, Rockman HA.

Am J Physiol Heart Circ Physiol. 2012 Oct 15;303(8):H1001-10. doi: 10.1152/ajpheart.00475.2012. Epub 2012 Aug 10.


Competing G protein-coupled receptor kinases balance G protein and β-arrestin signaling.

Heitzler D, Durand G, Gallay N, Rizk A, Ahn S, Kim J, Violin JD, Dupuy L, Gauthier C, Piketty V, Crépieux P, Poupon A, Clément F, Fages F, Lefkowitz RJ, Reiter E.

Mol Syst Biol. 2012 Jun 26;8:590. doi: 10.1038/msb.2012.22.


Cardiorenal actions of TRV120027, a novel ß-arrestin-biased ligand at the angiotensin II type I receptor, in healthy and heart failure canines: a novel therapeutic strategy for acute heart failure.

Boerrigter G, Lark MW, Whalen EJ, Soergel DG, Violin JD, Burnett JC Jr.

Circ Heart Fail. 2011 Nov;4(6):770-8. doi: 10.1161/CIRCHEARTFAILURE.111.962571. Epub 2011 Aug 11.


Biased ligands for better cardiovascular drugs: dissecting G-protein-coupled receptor pharmacology.

DeWire SM, Violin JD.

Circ Res. 2011 Jul 8;109(2):205-16. doi: 10.1161/CIRCRESAHA.110.231308. Review.


Quantifying ligand bias at seven-transmembrane receptors.

Rajagopal S, Ahn S, Rominger DH, Gowen-MacDonald W, Lam CM, Dewire SM, Violin JD, Lefkowitz RJ.

Mol Pharmacol. 2011 Sep;80(3):367-77. doi: 10.1124/mol.111.072801. Epub 2011 May 24.


Selectively engaging β-arrestins at the angiotensin II type 1 receptor reduces blood pressure and increases cardiac performance.

Violin JD, DeWire SM, Yamashita D, Rominger DH, Nguyen L, Schiller K, Whalen EJ, Gowen M, Lark MW.

J Pharmacol Exp Ther. 2010 Dec;335(3):572-9. doi: 10.1124/jpet.110.173005. Epub 2010 Aug 26.


beta-Arrestin mediates beta1-adrenergic receptor-epidermal growth factor receptor interaction and downstream signaling.

Tilley DG, Kim IM, Patel PA, Violin JD, Rockman HA.

J Biol Chem. 2009 Jul 24;284(30):20375-86. doi: 10.1074/jbc.M109.005793. Epub 2009 Jun 9.


Selective engagement of G protein coupled receptor kinases (GRKs) encodes distinct functions of biased ligands.

Zidar DA, Violin JD, Whalen EJ, Lefkowitz RJ.

Proc Natl Acad Sci U S A. 2009 Jun 16;106(24):9649-54. doi: 10.1073/pnas.0904361106. Epub 2009 Jun 2.


beta-Arrestin1 mediates nicotinic acid-induced flushing, but not its antilipolytic effect, in mice.

Walters RW, Shukla AK, Kovacs JJ, Violin JD, DeWire SM, Lam CM, Chen JR, Muehlbauer MJ, Whalen EJ, Lefkowitz RJ.

J Clin Invest. 2009 May;119(5):1312-21. doi: 10.1172/JCI36806. Epub 2009 Apr 6.


Beta-blockers alprenolol and carvedilol stimulate beta-arrestin-mediated EGFR transactivation.

Kim IM, Tilley DG, Chen J, Salazar NC, Whalen EJ, Violin JD, Rockman HA.

Proc Natl Acad Sci U S A. 2008 Sep 23;105(38):14555-60. doi: 10.1073/pnas.0804745105. Epub 2008 Sep 11.


Distinct conformational changes in beta-arrestin report biased agonism at seven-transmembrane receptors.

Shukla AK, Violin JD, Whalen EJ, Gesty-Palmer D, Shenoy SK, Lefkowitz RJ.

Proc Natl Acad Sci U S A. 2008 Jul 22;105(29):9988-93. doi: 10.1073/pnas.0804246105. Epub 2008 Jul 11.


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.


beta-arrestin-biased agonism at the beta2-adrenergic receptor.

Drake MT, Violin JD, Whalen EJ, Wisler JW, Shenoy SK, Lefkowitz RJ.

J Biol Chem. 2008 Feb 29;283(9):5669-76. Epub 2007 Dec 17.


beta2-adrenergic receptor signaling and desensitization elucidated by quantitative modeling of real time cAMP dynamics.

Violin JD, DiPilato LM, Yildirim N, Elston TC, Zhang J, Lefkowitz RJ.

J Biol Chem. 2008 Feb 1;283(5):2949-61. Epub 2007 Nov 28.


A unique mechanism of beta-blocker action: carvedilol stimulates beta-arrestin signaling.

Wisler JW, DeWire SM, Whalen EJ, Violin JD, Drake MT, Ahn S, Shenoy SK, Lefkowitz RJ.

Proc Natl Acad Sci U S A. 2007 Oct 16;104(42):16657-62. Epub 2007 Oct 9.


Beta-arrestin-mediated beta1-adrenergic receptor transactivation of the EGFR confers cardioprotection.

Noma T, Lemaire A, Naga Prasad SV, Barki-Harrington L, Tilley DG, Chen J, Le Corvoisier P, Violin JD, Wei H, Lefkowitz RJ, Rockman HA.

J Clin Invest. 2007 Sep;117(9):2445-58.


Beta-arrestin-biased ligands at seven-transmembrane receptors.

Violin JD, Lefkowitz RJ.

Trends Pharmacol Sci. 2007 Aug;28(8):416-22. Epub 2007 Jul 20. Review.


Regulation of beta-adrenergic receptor signaling by S-nitrosylation of G-protein-coupled receptor kinase 2.

Whalen EJ, Foster MW, Matsumoto A, Ozawa K, Violin JD, Que LG, Nelson CD, Benhar M, Keys JR, Rockman HA, Koch WJ, Daaka Y, Lefkowitz RJ, Stamler JS.

Cell. 2007 May 4;129(3):511-22.


Beta-arrestin2-mediated inotropic effects of the angiotensin II type 1A receptor in isolated cardiac myocytes.

Rajagopal K, Whalen EJ, Violin JD, Stiber JA, Rosenberg PB, Premont RT, Coffman TM, Rockman HA, Lefkowitz RJ.

Proc Natl Acad Sci U S A. 2006 Oct 31;103(44):16284-9. Epub 2006 Oct 23.


Beta-arrestin 2-dependent angiotensin II type 1A receptor-mediated pathway of chemotaxis.

Hunton DL, Barnes WG, Kim J, Ren XR, Violin JD, Reiter E, Milligan G, Patel DD, Lefkowitz RJ.

Mol Pharmacol. 2005 Apr;67(4):1229-36. Epub 2005 Jan 5.


beta-Arrestin 1 and Galphaq/11 coordinately activate RhoA and stress fiber formation following receptor stimulation.

Barnes WG, Reiter E, Violin JD, Ren XR, Milligan G, Lefkowitz RJ.

J Biol Chem. 2005 Mar 4;280(9):8041-50. Epub 2004 Dec 16.


Pathway illuminated: visualizing protein kinase C signaling.

Violin JD, Newton AC.

IUBMB Life. 2003 Dec;55(12):653-60. Review.


A genetically encoded fluorescent reporter reveals oscillatory phosphorylation by protein kinase C.

Violin JD, Zhang J, Tsien RY, Newton AC.

J Cell Biol. 2003 Jun 9;161(5):899-909. Epub 2003 Jun 2.


Partitioning of lipid-modified monomeric GFPs into membrane microdomains of live cells.

Zacharias DA, Violin JD, Newton AC, Tsien RY.

Science. 2002 May 3;296(5569):913-6.


PKA, PKC, and AKAP localization in and around the neuromuscular junction.

Perkins GA, Wang L, Huang LJ, Humphries K, Yao VJ, Martone M, Deerinck TJ, Barraclough DM, Violin JD, Smith D, Newton A, Scott JD, Taylor SS, Ellisman MH.

BMC Neurosci. 2001;2:17. Epub 2001 Oct 23.


Modeling the developmental neurotoxicity of chlorpyrifos in vitro: macromolecule synthesis in PC12 cells.

Song X, Violin JD, Seidler FJ, Slotkin TA.

Toxicol Appl Pharmacol. 1998 Jul;151(1):182-91.


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