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Items: 15

1.

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.

PMID:
28533287
2.

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.

PMID:
27936408
3.

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.

PMID:
24834870
4.

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.

5.

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.

PMID:
24063433
6.

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.

PMID:
23300227
7.

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.

8.

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.

PMID:
20801892
9.

Myelosuppression and kinase selectivity of multikinase angiogenesis inhibitors.

Kumar R, Crouthamel MC, Rominger DH, Gontarek RR, Tummino PJ, Levin RA, King AG.

Br J Cancer. 2009 Nov 17;101(10):1717-23. doi: 10.1038/sj.bjc.6605366. Epub 2009 Oct 20.

10.

Evidence for allosteric interactions of antagonist binding to the smoothened receptor.

Rominger CM, Bee WL, Copeland RA, Davenport EA, Gilmartin A, Gontarek R, Hornberger KR, Kallal LA, Lai Z, Lawrie K, Lu Q, McMillan L, Truong M, Tummino PJ, Turunen B, Will M, Zuercher WJ, Rominger DH.

J Pharmacol Exp Ther. 2009 Jun;329(3):995-1005. doi: 10.1124/jpet.109.152090. Epub 2009 Mar 20. Erratum in: J Pharmacol Exp Ther. 2010 Feb;332(2):690.

PMID:
19304771
11.

Pharmacological characterization of a novel nonpeptide antagonist radioligand, (+/-)-N-[2-methyl-4-methoxyphenyl]-1-(1-(methoxymethyl) propyl)-6-methyl-1H-1,2,3-triazolo[4,5-c]pyridin-4-amine ([3H]SN003) for corticotropin-releasing factor1 receptors.

Zhang G, Huang N, Li YW, Qi X, Marshall AP, Yan XX, Hill G, Rominger C, Prakash SR, Bakthavatchalam R, Rominger DH, Gilligan PJ, Zaczek R.

J Pharmacol Exp Ther. 2003 Apr;305(1):57-69.

PMID:
12649353
12.

Presenilin-1 and -2 are molecular targets for gamma-secretase inhibitors.

Seiffert D, Bradley JD, Rominger CM, Rominger DH, Yang F, Meredith JE Jr, Wang Q, Roach AH, Thompson LA, Spitz SM, Higaki JN, Prakash SR, Combs AP, Copeland RA, Arneric SP, Hartig PR, Robertson DW, Cordell B, Stern AM, Olson RE, Zaczek R.

J Biol Chem. 2000 Nov 3;275(44):34086-91.

13.

Characterization of [125I]sauvagine binding to CRH2 receptors: membrane homogenate and autoradiographic studies.

Rominger DH, Rominger CM, Fitzgerald LW, Grzanna R, Largent BL, Zaczek R.

J Pharmacol Exp Ther. 1998 Jul;286(1):459-68.

PMID:
9655891
14.

Two new potent neurotransmitter release enhancers, 10,10-bis(4-pyridinylmethyl)-9(10H)-anthracenone and 10,10-bis(2-fluoro-4-pyridinylmethyl)-9(10H)-anthracenone: comparison to linopirdine.

Zaczek R, Chorvat RJ, Saye JA, Pierdomenico ME, Maciag CM, Logue AR, Fisher BN, Rominger DH, Earl RA.

J Pharmacol Exp Ther. 1998 May;285(2):724-30.

PMID:
9580619
15.

EXP063, a nonpeptide angiotensin II and beta adrenergic receptor antagonist.

Wong PC, Duncia JV, Chiu AT, Olson RE, Rominger DH, Tam SW, Timmermans PB.

J Pharmacol Exp Ther. 1993 Nov;267(2):641-7.

PMID:
7902431

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