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Quantifying ligand bias at seven-transmembrane receptors.
Rajagopal S, Ahn S, Rominger DH, Gowen-MacDonald W, Lam CM, Dewire SM, Violin JD, Lefkowitz RJ. Rajagopal S, et al. Among authors: rominger dh. Mol Pharmacol. 2011 Sep;80(3):367-77. doi: 10.1124/mol.111.072801. Epub 2011 May 24. Mol Pharmacol. 2011. PMID: 21610196 Free PMC article.
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. DeWire SM, et al. Among authors: rominger dh. J Pharmacol Exp Ther. 2013 Mar;344(3):708-17. doi: 10.1124/jpet.112.201616. Epub 2013 Jan 8. J Pharmacol Exp Ther. 2013. PMID: 23300227
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. Chen XT, et al. Among authors: rominger dh. J Med Chem. 2013 Oct 24;56(20):8019-31. doi: 10.1021/jm4010829. Epub 2013 Oct 14. J Med Chem. 2013. PMID: 24063433
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. Rominger CM, et al. Among authors: rominger dh. J Pharmacol Exp Ther. 2009 Jun;329(3):995-1005. doi: 10.1124/jpet.109.152090. Epub 2009 Mar 20. J Pharmacol Exp Ther. 2009. PMID: 19304771
20 results