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Items: 13

1.

Discovery of a Novel 2,6-Disubstituted Glucosamine Series of Potent and Selective Hexokinase 2 Inhibitors.

Lin H, Zeng J, Xie R, Schulz MJ, Tedesco R, Qu J, Erhard KF, Mack JF, Raha K, Rendina AR, Szewczuk LM, Kratz PM, Jurewicz AJ, Cecconie T, Martens S, McDevitt PJ, Martin JD, Chen SB, Jiang Y, Nickels L, Schwartz BJ, Smallwood A, Zhao B, Campobasso N, Qian Y, Briand J, Rominger CM, Oleykowski C, Hardwicke MA, Luengo JI.

ACS Med Chem Lett. 2015 Dec 28;7(3):217-22. doi: 10.1021/acsmedchemlett.5b00214. eCollection 2016 Mar 10.

2.

[3a,4]-Dihydropyrazolo[1,5a]pyrimidines: Novel, Potent, and Selective Phosphatidylinositol-3-kinase β Inhibitors.

Yu H, Moore ML, Erhard K, Hardwicke MA, Lin H, Luengo JI, McSurdy-Freed J, Plant R, Qu J, Raha K, Rominger CM, Schaber MD, Spengler MD, Rivero RA.

ACS Med Chem Lett. 2013 Jan 10;4(2):230-4. doi: 10.1021/ml300330m. eCollection 2013 Feb 14.

3.

Rational Design, Synthesis, and SAR of a Novel Thiazolopyrimidinone Series of Selective PI3K-beta Inhibitors.

Lin H, Schulz MJ, Xie R, Zeng J, Luengo JI, Squire MD, Tedesco R, Qu J, Erhard K, Mack JF, Raha K, Plant R, Rominger CM, Ariazi JL, Sherk CS, Schaber MD, McSurdy-Freed J, Spengler MD, Davis CB, Hardwicke MA, Rivero RA.

ACS Med Chem Lett. 2012 May 29;3(7):524-9. doi: 10.1021/ml300045b. eCollection 2012 Jul 12.

4.

Synthesis and structure-activity relationships of 1,2,4-triazolo[1,5-a]pyrimidin-7(3H)-ones as novel series of potent β isoform selective phosphatidylinositol 3-kinase inhibitors.

Sanchez RM, Erhard K, Hardwicke MA, Lin H, McSurdy-Freed J, Plant R, Raha K, Rominger CM, Schaber MD, Spengler MD, Moore ML, Yu H, Luengo JI, Tedesco R, Rivero RA.

Bioorg Med Chem Lett. 2012 May 1;22(9):3198-202. doi: 10.1016/j.bmcl.2012.03.039. Epub 2012 Mar 16.

PMID:
22475557
5.

Synthesis and structure-activity relationships of imidazo[1,2-a]pyrimidin-5(1H)-ones as a novel series of beta isoform selective phosphatidylinositol 3-kinase inhibitors.

Lin H, Erhard K, Hardwicke MA, Luengo JI, Mack JF, McSurdy-Freed J, Plant R, Raha K, Rominger CM, Sanchez RM, Schaber MD, Schulz MJ, Spengler MD, Tedesco R, Xie R, Zeng JJ, Rivero RA.

Bioorg Med Chem Lett. 2012 Mar 15;22(6):2230-4. doi: 10.1016/j.bmcl.2012.01.092. Epub 2012 Feb 4.

PMID:
22361133
6.

Development of potent B-RafV600E inhibitors containing an arylsulfonamide headgroup.

Stellwagen JC, Adjabeng GM, Arnone MR, Dickerson SH, Han C, Hornberger KR, King AJ, Mook RA Jr, Petrov KG, Rheault TR, Rominger CM, Rossanese OW, Smitheman KN, Waterson AG, Uehling DE.

Bioorg Med Chem Lett. 2011 Aug 1;21(15):4436-40. doi: 10.1016/j.bmcl.2011.06.021. Epub 2011 Jun 16.

PMID:
21733693
7.

GSK1120212 (JTP-74057) is an inhibitor of MEK activity and activation with favorable pharmacokinetic properties for sustained in vivo pathway inhibition.

Gilmartin AG, Bleam MR, Groy A, Moss KG, Minthorn EA, Kulkarni SG, Rominger CM, Erskine S, Fisher KE, Yang J, Zappacosta F, Annan R, Sutton D, Laquerre SG.

Clin Cancer Res. 2011 Mar 1;17(5):989-1000. doi: 10.1158/1078-0432.CCR-10-2200. Epub 2011 Jan 18. Erratum in: Clin Cancer Res. 2012 Apr 15;18(8):2413.

8.

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
9.

An intrinsic ATPase activity of phospho-MEK-1 uncoupled from downstream ERK phosphorylation.

Rominger CM, Schaber MD, Yang J, Gontarek RR, Weaver KL, Broderick T, Carter L, Copeland RA, May EW.

Arch Biochem Biophys. 2007 Aug 1;464(1):130-7. Epub 2007 Apr 17.

PMID:
17490600
10.

Demonstration of a genetic therapeutic index for tumors expressing oncogenic BRAF by the kinase inhibitor SB-590885.

King AJ, Patrick DR, Batorsky RS, Ho ML, Do HT, Zhang SY, Kumar R, Rusnak DW, Takle AK, Wilson DM, Hugger E, Wang L, Karreth F, Lougheed JC, Lee J, Chau D, Stout TJ, May EW, Rominger CM, Schaber MD, Luo L, Lakdawala AS, Adams JL, Contractor RG, Smalley KS, Herlyn M, Morrissey MM, Tuveson DA, Huang PS.

Cancer Res. 2006 Dec 1;66(23):11100-5.

11.

Binding sites of gamma-secretase inhibitors in rodent brain: distribution, postnatal development, and effect of deafferentation.

Yan XX, Li T, Rominger CM, Prakash SR, Wong PC, Olson RE, Zaczek R, Li YW.

J Neurosci. 2004 Mar 24;24(12):2942-52.

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

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