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Items: 1 to 50 of 109

1.

Correction: The selective estrogen receptor downregulator GDC-0810 is efficacious in diverse models of ER+ breast cancer.

Joseph JD, Darimont B, Zhou W, Arrazate A, Young A, Ingalla E, Walter K, Blake RA, Nonomiya J, Guan Z, Kategaya L, Govek SP, Lai AG, Kahraman M, Brigham D, Sensintaffar J, Lu N, Shao G, Qian J, Grillot K, Moon M, Prudente R, Bischoff E, Lee KJ, Bonnefous C, Douglas KL, Julien JD, Nagasawa JY, Aparicio A, Kaufman J, Haley B, Giltnane JM, Wertz IE, Lackner MR, Nannini MA, Sampath D, Schwarz L, Manning HC, Tantawy MN, Arteaga CL, Heyman RA, Rix PJ, Friedman L, Smith ND, Metcalfe C, Hager JH.

Elife. 2019 Jan 7;8. pii: e44851. doi: 10.7554/eLife.44851.

2.

The selective estrogen receptor downregulator GDC-0810 is efficacious in diverse models of ER+ breast cancer.

Joseph JD, Darimont B, Zhou W, Arrazate A, Young A, Ingalla E, Walter K, Blake RA, Nonomiya J, Guan Z, Kategaya L, Govek SP, Lai AG, Kahraman M, Brigham D, Sensintaffar J, Lu N, Shao G, Qian J, Grillot K, Moon M, Prudente R, Bischoff E, Lee KJ, Bonnefous C, Douglas KL, Julien JD, Nagasawa JY, Aparicio A, Kaufman J, Haley B, Giltnane JM, Wertz IE, Lackner MR, Nannini MA, Sampath D, Schwarz L, Manning HC, Tantawy MN, Arteaga CL, Heyman RA, Rix PJ, Friedman L, Smith ND, Metcalfe C, Hager JH.

Elife. 2016 Jul 13;5. pii: e15828. doi: 10.7554/eLife.15828. Erratum in: Elife. 2019 Jan 07;8:.

3.

ARN-509: a novel antiandrogen for prostate cancer treatment.

Clegg NJ, Wongvipat J, Joseph JD, Tran C, Ouk S, Dilhas A, Chen Y, Grillot K, Bischoff ED, Cai L, Aparicio A, Dorow S, Arora V, Shao G, Qian J, Zhao H, Yang G, Cao C, Sensintaffar J, Wasielewska T, Herbert MR, Bonnefous C, Darimont B, Scher HI, Smith-Jones P, Klang M, Smith ND, De Stanchina E, Wu N, Ouerfelli O, Rix PJ, Heyman RA, Jung ME, Sawyers CL, Hager JH.

Cancer Res. 2012 Mar 15;72(6):1494-503. doi: 10.1158/0008-5472.CAN-11-3948. Epub 2012 Jan 20.

4.

Synthesis and SAR of 2-aryl-3-aminomethylquinolines as agonists of the bile acid receptor TGR5.

Herbert MR, Siegel DL, Staszewski L, Cayanan C, Banerjee U, Dhamija S, Anderson J, Fan A, Wang L, Rix P, Shiau AK, Rao TS, Noble SA, Heyman RA, Bischoff E, Guha M, Kabakibi A, Pinkerton AB.

Bioorg Med Chem Lett. 2010 Oct 1;20(19):5718-21. doi: 10.1016/j.bmcl.2010.08.014. Epub 2010 Aug 10.

PMID:
20801037
5.

Biological characterization of a heterodimer-selective retinoid X receptor modulator: potential benefits for the treatment of type 2 diabetes.

Leibowitz MD, Ardecky RJ, Boehm MF, Broderick CL, Carfagna MA, Crombie DL, D'Arrigo J, Etgen GJ, Faul MM, Grese TA, Havel H, Hein NI, Heyman RA, Jolley D, Klausing K, Liu S, Mais DE, Mapes CM, Marschke KB, Michellys PY, Montrose-Rafizadeh C, Ogilvie KM, Pascual B, Rungta D, Tyhonas JS, Urcan MS, Wardlow M, Yumibe N, Reifel-Miller A.

Endocrinology. 2006 Feb;147(2):1044-53. Epub 2005 Nov 3.

PMID:
16269450
6.

FXR, a therapeutic target for bile acid and lipid disorders.

Westin S, Heyman RA, Martin R.

Mini Rev Med Chem. 2005 Aug;5(8):719-27. Review.

PMID:
16101408
7.

A multimodal approach to managing the symptoms of multiple sclerosis.

Crayton H, Heyman RA, Rossman HS.

Neurology. 2004 Dec 14;63(11 Suppl 5):S12-8. Review.

PMID:
15596731
8.

Macrophage liver X receptor is required for antiatherogenic activity of LXR agonists.

Levin N, Bischoff ED, Daige CL, Thomas D, Vu CT, Heyman RA, Tangirala RK, Schulman IG.

Arterioscler Thromb Vasc Biol. 2005 Jan;25(1):135-42. Epub 2004 Nov 11.

PMID:
15539622
9.

Regulation of PPARgamma coactivator 1alpha (PGC-1alpha) signaling by an estrogen-related receptor alpha (ERRalpha) ligand.

Willy PJ, Murray IR, Qian J, Busch BB, Stevens WC Jr, Martin R, Mohan R, Zhou S, Ordentlich P, Wei P, Sapp DW, Horlick RA, Heyman RA, Schulman IG.

Proc Natl Acad Sci U S A. 2004 Jun 15;101(24):8912-7. Epub 2004 Jun 7.

10.

The flip side: Identifying small molecule regulators of nuclear receptors.

Schulman IG, Heyman RA.

Chem Biol. 2004 May;11(5):639-46. Review.

11.

The selective estrogen receptor modulator arzoxifene and the rexinoid LG100268 cooperate to promote transforming growth factor beta-dependent apoptosis in breast cancer.

Rendi MH, Suh N, Lamph WW, Krajewski S, Reed JC, Heyman RA, Berchuck A, Liby K, Risingsong R, Royce DB, Williams CR, Sporn MB.

Cancer Res. 2004 May 15;64(10):3566-71.

12.

Bile acids lower triglyceride levels via a pathway involving FXR, SHP, and SREBP-1c.

Watanabe M, Houten SM, Wang L, Moschetta A, Mangelsdorf DJ, Heyman RA, Moore DD, Auwerx J.

J Clin Invest. 2004 May;113(10):1408-18.

13.

Erralpha and Gabpa/b specify PGC-1alpha-dependent oxidative phosphorylation gene expression that is altered in diabetic muscle.

Mootha VK, Handschin C, Arlow D, Xie X, St Pierre J, Sihag S, Yang W, Altshuler D, Puigserver P, Patterson N, Willy PJ, Schulman IG, Heyman RA, Lander ES, Spiegelman BM.

Proc Natl Acad Sci U S A. 2004 Apr 27;101(17):6570-5. Epub 2004 Apr 20. Erratum in: Proc Natl Acad Sci U S A. 2005 Jul 19;102(29):10405.

14.

Orphan nuclear receptor modulators.

Mohan R, Heyman RA.

Curr Top Med Chem. 2003;3(14):1637-47. Review.

PMID:
14683519
15.

Nurr1-RXR heterodimers mediate RXR ligand-induced signaling in neuronal cells.

Wallen-Mackenzie A, Mata de Urquiza A, Petersson S, Rodriguez FJ, Friling S, Wagner J, Ordentlich P, Lengqvist J, Heyman RA, Arenas E, Perlmann T.

Genes Dev. 2003 Dec 15;17(24):3036-47. Epub 2003 Dec 17.

16.

Activation of the retinoid X receptor suppresses appetite in the rat.

Ogilvie KM, Saladin R, Nagy TR, Urcan MS, Heyman RA, Leibowitz MD.

Endocrinology. 2004 Feb;145(2):565-73. Epub 2003 Nov 6.

PMID:
14605005
17.

Promoter-specific roles for liver X receptor/corepressor complexes in the regulation of ABCA1 and SREBP1 gene expression.

Wagner BL, Valledor AF, Shao G, Daige CL, Bischoff ED, Petrowski M, Jepsen K, Baek SH, Heyman RA, Rosenfeld MG, Schulman IG, Glass CK.

Mol Cell Biol. 2003 Aug;23(16):5780-9.

18.

Novel (2E,4E,6Z)-7-(2-alkoxy-3,5-dialkylbenzene)-3-methylocta-2,4,6-trienoic acid retinoid X receptor modulators are active in models of type 2 diabetes.

Michellys PY, Ardecky RJ, Chen JH, Crombie DL, Etgen GJ, Faul MM, Faulkner AL, Grese TA, Heyman RA, Karanewsky DS, Klausing K, Leibowitz MD, Liu S, Mais DA, Mapes CM, Marschke KB, Reifel-Miller A, Ogilvie KM, Rungta D, Thompson AW, Tyhonas JS, Boehm MF.

J Med Chem. 2003 Jun 19;46(13):2683-96.

PMID:
12801232
19.

Identification of the antineoplastic agent 6-mercaptopurine as an activator of the orphan nuclear hormone receptor Nurr1.

Ordentlich P, Yan Y, Zhou S, Heyman RA.

J Biol Chem. 2003 Jul 4;278(27):24791-9. Epub 2003 Apr 22.

20.

Retinoic acid receptor ligands based on the 6-cyclopropyl-2,4-hexadienoic acid.

Farmer LJ, Zhi L, Jeong S, Lamph WW, Osburn DL, Croston G, Flatten KS, Heyman RA, Nadzan AM.

Bioorg Med Chem Lett. 2003 Jan 20;13(2):261-4.

PMID:
12482435
21.

Prevention and treatment of experimental breast cancer with the combination of a new selective estrogen receptor modulator, arzoxifene, and a new rexinoid, LG 100268.

Suh N, Lamph WW, Glasebrook AL, Grese TA, Palkowitz AD, Williams CR, Risingsong R, Farris MR, Heyman RA, Sporn MB.

Clin Cancer Res. 2002 Oct;8(10):3270-5.

22.

Identification of macrophage liver X receptors as inhibitors of atherosclerosis.

Tangirala RK, Bischoff ED, Joseph SB, Wagner BL, Walczak R, Laffitte BA, Daige CL, Thomas D, Heyman RA, Mangelsdorf DJ, Wang X, Lusis AJ, Tontonoz P, Schulman IG.

Proc Natl Acad Sci U S A. 2002 Sep 3;99(18):11896-901. Epub 2002 Aug 22.

23.

Redundant pathways for negative feedback regulation of bile acid production.

Wang L, Lee YK, Bundman D, Han Y, Thevananther S, Kim CS, Chua SS, Wei P, Heyman RA, Karin M, Moore DD.

Dev Cell. 2002 Jun;2(6):721-31.

24.

A natural product that lowers cholesterol as an antagonist ligand for FXR.

Urizar NL, Liverman AB, Dodds DT, Silva FV, Ordentlich P, Yan Y, Gonzalez FJ, Heyman RA, Mangelsdorf DJ, Moore DD.

Science. 2002 May 31;296(5573):1703-6. Epub 2002 May 2.

25.

The rexinoid LG100754 is a novel RXR:PPARgamma agonist and decreases glucose levels in vivo.

Cesario RM, Klausing K, Razzaghi H, Crombie D, Rungta D, Heyman RA, Lala DS.

Mol Endocrinol. 2001 Aug;15(8):1360-9.

PMID:
11463859
26.

Differential effects of rexinoids and thiazolidinediones on metabolic gene expression in diabetic rodents.

Singh Ahuja H, Liu S, Crombie DL, Boehm M, Leibowitz MD, Heyman RA, Depre C, Nagy L, Tontonoz P, Davies PJ.

Mol Pharmacol. 2001 Apr;59(4):765-73.

PMID:
11259621
27.

Reduction of atherosclerosis in apolipoprotein E knockout mice by activation of the retinoid X receptor.

Claudel T, Leibowitz MD, Fiévet C, Tailleux A, Wagner B, Repa JJ, Torpier G, Lobaccaro JM, Paterniti JR, Mangelsdorf DJ, Heyman RA, Auwerx J.

Proc Natl Acad Sci U S A. 2001 Feb 27;98(5):2610-5. Epub 2001 Feb 20.

28.

Metabolic effects of rexinoids: tissue-specific regulation of lipoprotein lipase activity.

Davies PJ, Berry SA, Shipley GL, Eckel RH, Hennuyer N, Crombie DL, Ogilvie KM, Peinado-Onsurbe J, Fievet C, Leibowitz MD, Heyman RA, Auwerx J.

Mol Pharmacol. 2001 Feb;59(2):170-6.

PMID:
11160850
29.

Regulation of absorption and ABC1-mediated efflux of cholesterol by RXR heterodimers.

Repa JJ, Turley SD, Lobaccaro JA, Medina J, Li L, Lustig K, Shan B, Heyman RA, Dietschy JM, Mangelsdorf DJ.

Science. 2000 Sep 1;289(5484):1524-9.

30.

Retinoid X receptor agonists have anti-obesity effects and improve insulin sensitivity in Zucker fa/fa rats.

Liu YL, Sennitt MV, Hislop DC, Crombie DL, Heyman RA, Cawthorne MA.

Int J Obes Relat Metab Disord. 2000 Aug;24(8):997-1004.

PMID:
10951538
31.

Three amino acids specify coactivator choice by retinoid X receptors.

Shao G, Heyman RA, Schulman IG.

Mol Endocrinol. 2000 Aug;14(8):1198-209.

PMID:
10935544
32.

Identification of receptor-selective retinoids that are potent inhibitors of the growth of human head and neck squamous cell carcinoma cells.

Sun SY, Yue P, Mao L, Dawson MI, Shroot B, Lamph WW, Heyman RA, Chandraratna RA, Shudo K, Hong WK, Lotan R.

Clin Cancer Res. 2000 Apr;6(4):1563-73.

33.
34.

November 1999: 56 year old woman with left facial numbness.

Lacomis D, Heyman RA.

Brain Pathol. 2000 Jan;10(1):175-6. No abstract available.

PMID:
10668910
35.

Effect of the retinoid X receptor-selective ligand LGD1069 on mammary carcinoma after tamoxifen failure.

Bischoff ED, Heyman RA, Lamph WW.

J Natl Cancer Inst. 1999 Dec 15;91(24):2118.

PMID:
10601384
36.

Novel nonsecosteroidal vitamin D mimics exert VDR-modulating activities with less calcium mobilization than 1,25-dihydroxyvitamin D3.

Boehm MF, Fitzgerald P, Zou A, Elgort MG, Bischoff ED, Mere L, Mais DE, Bissonnette RP, Heyman RA, Nadzan AM, Reichman M, Allegretto EA.

Chem Biol. 1999 May;6(5):265-75.

37.

Teaching memory strategies to persons with multiple sclerosis.

Allen DN, Goldstein G, Heyman RA, Rondinelli T.

J Rehabil Res Dev. 1998 Oct;35(4):405-10.

PMID:
10220218
38.
39.

Retinoid-induced apoptosis in normal and neoplastic tissues.

Nagy L, Thomazy VA, Heyman RA, Davies PJ.

Cell Death Differ. 1998 Jan;5(1):11-9. Review.

40.

Synthesis of retinoid X receptor-specific ligands that are potent inducers of adipogenesis in 3T3-L1 cells.

Canan Koch SS, Dardashti LJ, Cesario RM, Croston GE, Boehm MF, Heyman RA, Nadzan AM.

J Med Chem. 1999 Feb 25;42(4):742-50.

PMID:
10052980
41.

Activity of 9-cis-retinoic acid and receptor-selective retinoids in small cell lung cancer cell lines.

Rosati R, Ramnath N, Adil MR, Ou X, Ali MA, Heyman RA, Kalemkerian GP.

Anticancer Res. 1998 Nov-Dec;18(6A):4071-5.

PMID:
9891447
42.

Retinoid-X receptor signalling in the developing spinal cord.

Solomin L, Johansson CB, Zetterström RH, Bissonnette RP, Heyman RA, Olson L, Lendahl U, Frisén J, Perlmann T.

Nature. 1998 Sep 24;395(6700):398-402.

PMID:
9759732
44.

RXR agonists activate PPARalpha-inducible genes, lower triglycerides, and raise HDL levels in vivo.

Mukherjee R, Strasser J, Jow L, Hoener P, Paterniti JR Jr, Heyman RA.

Arterioscler Thromb Vasc Biol. 1998 Feb;18(2):272-6.

PMID:
9484993
45.

Beyond tamoxifen: the retinoid X receptor-selective ligand LGD1069 (TARGRETIN) causes complete regression of mammary carcinoma.

Bischoff ED, Gottardis MM, Moon TE, Heyman RA, Lamph WW.

Cancer Res. 1998 Feb 1;58(3):479-84.

46.

Differential effects of synthetic nuclear retinoid receptor-selective retinoids on the growth of human non-small cell lung carcinoma cells.

Sun SY, Yue P, Dawson MI, Shroot B, Michel S, Lamph WW, Heyman RA, Teng M, Chandraratna RA, Shudo K, Hong WK, Lotan R.

Cancer Res. 1997 Nov 1;57(21):4931-9.

47.
48.

Activation of the orphan nuclear receptor steroidogenic factor 1 by oxysterols.

Lala DS, Syka PM, Lazarchik SB, Mangelsdorf DJ, Parker KL, Heyman RA.

Proc Natl Acad Sci U S A. 1997 May 13;94(10):4895-900.

49.

Sensitization of diabetic and obese mice to insulin by retinoid X receptor agonists.

Mukherjee R, Davies PJ, Crombie DL, Bischoff ED, Cesario RM, Jow L, Hamann LG, Boehm MF, Mondon CE, Nadzan AM, Paterniti JR Jr, Heyman RA.

Nature. 1997 Mar 27;386(6623):407-10.

PMID:
9121558
50.

Expression and characterization of retinoid receptors in yeast.

Allegretto EA, Heyman RA.

Methods Enzymol. 1997;282:25-32. No abstract available.

PMID:
9330274

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