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Items: 1 to 50 of 67

1.

Discovery of a novel mechanism of steroid receptor antagonism: WAY-255348 modulates progesterone receptor cellular localization and promoter interactions.

Yudt MR, Russo LA, Berrodin TJ, Jelinsky SA, Ellis D, Cohen JC, Cooch N, Haglund E, Unwalla RJ, Fensome A, Wrobel J, Zhang Z, Nagpal S, Winneker RC.

Biochem Pharmacol. 2011 Dec 1;82(11):1709-19. doi: 10.1016/j.bcp.2011.08.006. Epub 2011 Aug 11.

PMID:
21854761
2.

Progress and prospects in treating postmenopausal vaginal atrophy.

Winneker RC, Harris HA.

Clin Pharmacol Ther. 2011 Jan;89(1):129-32. doi: 10.1038/clpt.2010.161. Epub 2010 Oct 13.

PMID:
20944561
3.

1-Methyl-1H-pyrrole-2-carbonitrile containing tetrahydronaphthalene derivatives as non-steroidal progesterone receptor antagonists.

Kern JC, Terefenko E, Trybulski E, Berrodin TJ, Cohen J, Winneker RC, Yudt MR, Zhang Z, Zhu Y, Zhang P.

Bioorg Med Chem Lett. 2010 Aug 15;20(16):4816-8. doi: 10.1016/j.bmcl.2010.06.109. Epub 2010 Jun 25.

PMID:
20638844
4.

A mouse model of androgenetic alopecia.

Crabtree JS, Kilbourne EJ, Peano BJ, Chippari S, Kenney T, McNally C, Wang W, Harris HA, Winneker RC, Nagpal S, Thompson CC.

Endocrinology. 2010 May;151(5):2373-80. doi: 10.1210/en.2009-1474. Epub 2010 Mar 16.

PMID:
20233794
5.

Loss of inhibitory insulin receptor substrate-1 phosphorylation is an early event in mammalian target of rapamycin-dependent endometrial hyperplasia and carcinoma.

McCampbell AS, Harris HA, Crabtree JS, Winneker RC, Walker CL, Broaddus RR.

Cancer Prev Res (Phila). 2010 Mar;3(3):290-300. doi: 10.1158/1940-6207.CAPR-09-0199. Epub 2010 Feb 23.

6.

5-Aryl indanones and derivatives as non-steroidal progesterone receptor modulators.

Kern JC, Terefenko E, Trybulski E, Berrodin TJ, Cohen J, Winneker RC, Yudt MR, Zhang Z, Zhu Y, Zhang P.

Bioorg Med Chem Lett. 2009 Dec 1;19(23):6666-9. doi: 10.1016/j.bmcl.2009.10.008. Epub 2009 Oct 7.

PMID:
19864132
7.

Dual acting norepinephrine reuptake inhibitors and 5-HT(2A) receptor antagonists: Identification, synthesis and activity of novel 4-aminoethyl-3-(phenylsulfonyl)-1H-indoles.

Heffernan GD, Coghlan RD, Manas ES, McDevitt RE, Li Y, Mahaney PE, Robichaud AJ, Huselton C, Alfinito P, Bray JA, Cosmi SA, Johnston GH, Kenney T, Koury E, Winneker RC, Deecher DC, Trybulski EJ.

Bioorg Med Chem. 2009 Nov 15;17(22):7802-15. doi: 10.1016/j.bmc.2009.09.023. Epub 2009 Sep 18.

PMID:
19836247
8.

Comparison of human and rat uterine leiomyomata: identification of a dysregulated mammalian target of rapamycin pathway.

Crabtree JS, Jelinsky SA, Harris HA, Choe SE, Cotreau MM, Kimberland ML, Wilson E, Saraf KA, Liu W, McCampbell AS, Dave B, Broaddus RR, Brown EL, Kao W, Skotnicki JS, Abou-Gharbia M, Winneker RC, Walker CL.

Cancer Res. 2009 Aug 1;69(15):6171-8. doi: 10.1158/0008-5472.CAN-08-4471. Epub 2009 Jul 21.

9.

Effects of various selective estrogen receptor modulators with or without conjugated estrogens on mouse mammary gland.

Peano BJ, Crabtree JS, Komm BS, Winneker RC, Harris HA.

Endocrinology. 2009 Apr;150(4):1897-903. doi: 10.1210/en.2008-1210. Epub 2008 Nov 20.

PMID:
19022889
10.

Novel progesterone receptor modulators with gene selective and context-dependent partial agonism.

Berrodin TJ, Jelinsky SA, Graciani N, Butera JA, Zhang Z, Nagpal S, Winneker RC, Yudt MR.

Biochem Pharmacol. 2009 Jan 15;77(2):204-15. doi: 10.1016/j.bcp.2008.10.016. Epub 2008 Nov 1.

PMID:
19013437
11.

Development of an early biomarker for the ovarian liability of selective estrogen receptor modulators in rats.

Harris HA, Chennathukuzhi VM, Zhang X, Mekonnen B, Jelinsky SA, Schelling SH, Patel VS, Huselton C, Negahban A, Azam F, Winneker RC.

J Steroid Biochem Mol Biol. 2008 Nov;112(1-3):40-6. doi: 10.1016/j.jsbmb.2008.08.008. Epub 2008 Sep 4.

PMID:
18824103
12.

1,5-Dihydro-benzo[e][1,4]oxazepin-2(1H)-ones containing a 7-(5'-cyanopyrrol-2-yl) group as nonsteroidal progesterone receptor modulators.

Kern JC, Terefenko EA, Fensome A, Unwalla R, Wrobel J, Cohen J, Zhu Y, Berrodin TJ, Yudt MR, Winneker RC, Zhang Z, Zhang P.

Bioorg Med Chem Lett. 2008 Sep 15;18(18):5015-7. doi: 10.1016/j.bmcl.2008.08.015. Epub 2008 Aug 9.

PMID:
18722119
13.

Molecular analysis of the vaginal response to estrogens in the ovariectomized rat and postmenopausal woman.

Jelinsky SA, Choe SE, Crabtree JS, Cotreau MM, Wilson E, Saraf K, Dorner AJ, Brown EL, Peano BJ, Zhang X, Winneker RC, Harris HA.

BMC Med Genomics. 2008 Jun 25;1:27. doi: 10.1186/1755-8794-1-27.

14.

In vitro and in vivo characterization of a novel nonsteroidal, species-specific progesterone receptor modulator, PRA-910.

Zhang Z, Lundeen SG, Slayden O, Zhu Y, Cohen J, Berrodin TJ, Bretz J, Chippari S, Wrobel J, Zhang P, Fensome A, Winneker RC, Yudt MR.

Ernst Schering Found Symp Proc. 2007;(1):171-97.

PMID:
18540573
15.

7-aryl 1,5-dihydro-benzo[e][1,4]oxazepin-2-ones and analogs as non-steroidal progesterone receptor antagonists.

Zhang P, Kern JC, Terefenko EA, Fensome A, Unwalla R, Zhang Z, Cohen J, Berrodin TJ, Yudt MR, Winneker RC, Wrobel J.

Bioorg Med Chem. 2008 Jul 1;16(13):6589-600. doi: 10.1016/j.bmc.2008.05.018. Epub 2008 May 10.

PMID:
18504132
16.

A new generation of progesterone receptor modulators.

Winneker RC, Fensome A, Zhang P, Yudt MR, McComas CC, Unwalla RJ.

Steroids. 2008 Aug;73(7):689-701. doi: 10.1016/j.steroids.2008.03.005. Epub 2008 Mar 28. Review.

PMID:
18472121
17.

Activity of three selective estrogen receptor modulators on hormone-dependent responses in the mouse uterus and mammary gland.

Crabtree JS, Peano BJ, Zhang X, Komm BS, Winneker RC, Harris HA.

Mol Cell Endocrinol. 2008 Jun 11;287(1-2):40-6. doi: 10.1016/j.mce.2008.01.027. Epub 2008 Feb 12.

PMID:
18367319
18.

Design, synthesis, and SAR of new pyrrole-oxindole progesterone receptor modulators leading to 5-(7-fluoro-3,3-dimethyl-2-oxo-2,3-dihydro-1H-indol-5-yl)-1-methyl-1H-pyrrole-2-carbonitrile (WAY-255348).

Fensome A, Adams WR, Adams AL, Berrodin TJ, Cohen J, Huselton C, Illenberger A, Kern JC, Hudak VA, Marella MA, Melenski EG, McComas CC, Mugford CA, Slayden OD, Yudt M, Zhang Z, Zhang P, Zhu Y, Winneker RC, Wrobel JE.

J Med Chem. 2008 Mar 27;51(6):1861-73. doi: 10.1021/jm701080t. Epub 2008 Mar 5.

PMID:
18318463
19.

Differing pharmacological activities of thiazolidinone analogs at the FSH receptor.

Arey BJ, Yanofsky SD, Claudia Pérez M, Holmes CP, Wrobel J, Gopalsamy A, Stevis PE, López FJ, Winneker RC.

Biochem Biophys Res Commun. 2008 Apr 11;368(3):723-8. doi: 10.1016/j.bbrc.2008.01.119. Epub 2008 Feb 4.

PMID:
18252197
20.

A study of 17beta-estradiol-regulated genes in the vagina of postmenopausal women with vaginal atrophy.

Cotreau MM, Chennathukuzhi VM, Harris HA, Han L, Dorner AJ, Apseloff G, Varadarajan U, Hatstat E, Zakaria M, Strahs AL, Crabtree JS, Winneker RC, Jelinsky SA.

Maturitas. 2007 Dec 20;58(4):366-76. Epub 2007 Nov 9.

PMID:
17997058
21.

5-(3-Cyclopentyl-2-thioxo-2,3-dihydro-1H-benzimidazol-5-yl)-1-methyl-1H-pyrrole-2-carbonitrile: A novel, highly potent, selective, and orally active non-steroidal progesterone receptor agonist.

Zhang P, Terefenko E, Kern J, Fensome A, Trybulski E, Unwalla R, Wrobel J, Lockhead S, Zhu Y, Cohen J, Lacava M, Winneker RC, Zhang Z.

Bioorg Med Chem. 2007 Oct 15;15(20):6556-64. Epub 2007 Jul 26.

PMID:
17681796
22.

Desvenlafaxine succinate identifies novel antagonist binding determinants in the human norepinephrine transporter.

Mason JN, Deecher DC, Richmond RL, Stack G, Mahaney PE, Trybulski E, Winneker RC, Blakely RD.

J Pharmacol Exp Ther. 2007 Nov;323(2):720-9. Epub 2007 Aug 2.

PMID:
17673606
23.

Development of a mouse model of mammary gland versus uterus tissue selectivity using estrogen- and progesterone-regulated gene markers.

Crabtree JS, Zhang X, Peano BJ, Zhang Z, Winneker RC, Harris HA.

J Steroid Biochem Mol Biol. 2006 Sep;101(1):11-21. Epub 2006 Aug 22.

PMID:
16920353
24.

The pathway-selective estrogen receptor ligand WAY-169916 displays differential activity in ischemia-reperfusion injury models.

Harnish DC, Liu X, Kenney T, Winneker RC, Chadwick C, Friedrichs GS, Kilbourne EJ.

J Cardiovasc Pharmacol. 2006 Jun;47(6):788-95.

PMID:
16810080
25.

Control of chronic inflammation with pathway selective estrogen receptor ligands.

Steffan RJ, Matelan E, Ashwell MA, Moore WJ, Solvibile WR, Trybulski E, Chadwick CC, Chippari S, Kenney T, Winneker RC, Eckert A, Borges-Marcucci L, Adelman SJ, Xu Z, Mosyak L, Harnish DC.

Curr Top Med Chem. 2006;6(2):103-11. Review.

PMID:
16454762
26.

Selective and opposing actions of progesterone receptor isoforms in human endometrial stromal cells.

Yudt MR, Berrodin TJ, Jelinsky SA, Hanna LA, Brown EL, Chippari S, Bhat RA, Winneker RC, Zhang Z.

Mol Cell Endocrinol. 2006 Mar 9;247(1-2):116-26. Epub 2006 Jan 25.

PMID:
16442706
27.
28.

Quantitative analysis of gene regulation by seven clinically relevant progestins suggests a highly similar mechanism of action through progesterone receptors in T47D breast cancer cells.

Bray JD, Jelinsky S, Ghatge R, Bray JA, Tunkey C, Saraf K, Jacobsen BM, Richer JK, Brown EL, Winneker RC, Horwitz KB, Lyttle CR.

J Steroid Biochem Mol Biol. 2005 Dec;97(4):328-41. Epub 2005 Sep 12.

PMID:
16157482
29.

Synthesis and structure-activity relationship of novel 6-aryl-1,4-dihydrobenzo[d][1,3]oxazine-2-thiones as progesterone receptor modulators leading to the potent and selective nonsteroidal progesterone receptor agonist tanaproget.

Fensome A, Bender R, Chopra R, Cohen J, Collins MA, Hudak V, Malakian K, Lockhead S, Olland A, Svenson K, Terefenko EA, Unwalla RJ, Wilhelm JM, Wolfrom S, Zhu Y, Zhang Z, Zhang P, Winneker RC, Wrobel J.

J Med Chem. 2005 Aug 11;48(16):5092-5.

PMID:
16078826
30.

Molecular and pharmacological properties of a potent and selective novel nonsteroidal progesterone receptor agonist tanaproget.

Zhang Z, Olland AM, Zhu Y, Cohen J, Berrodin T, Chippari S, Appavu C, Li S, Wilhem J, Chopra R, Fensome A, Zhang P, Wrobel J, Unwalla RJ, Lyttle CR, Winneker RC.

J Biol Chem. 2005 Aug 5;280(31):28468-75. Epub 2005 Jun 3.

31.

Differential effects of estrogens and progestins on the anticoagulant tissue factor pathway inhibitor in the rat.

Shirk RA, Zhang Z, Winneker RC.

J Steroid Biochem Mol Biol. 2005 Mar;94(4):361-8.

PMID:
15857755
32.

Nonsteroidal progesterone receptor modulators: structure activity relationships.

Winneker RC, Fensome A, Wrobel JE, Zhang Z, Zhang P.

Semin Reprod Med. 2005 Feb;23(1):46-57. Review.

PMID:
15714389
33.

Identification of pathway-selective estrogen receptor ligands that inhibit NF-kappaB transcriptional activity.

Chadwick CC, Chippari S, Matelan E, Borges-Marcucci L, Eckert AM, Keith JC Jr, Albert LM, Leathurby Y, Harris HA, Bhat RA, Ashwell M, Trybulski E, Winneker RC, Adelman SJ, Steffan RJ, Harnish DC.

Proc Natl Acad Sci U S A. 2005 Feb 15;102(7):2543-8. Epub 2005 Feb 7.

34.

Identification of novel estrogen receptor alpha antagonists.

Shao D, Berrodin TJ, Manas E, Hauze D, Powers R, Bapat A, Gonder D, Winneker RC, Frail DE.

J Steroid Biochem Mol Biol. 2004 Apr;88(4-5):351-60.

PMID:
15145444
35.

Novel pyrrole-containing progesterone receptor modulators.

Collins MA, Hudak V, Bender R, Fensome A, Zhang P, Miller L, Winneker RC, Zhang Z, Zhu Y, Cohen J, Unwalla RJ, Wrobel J.

Bioorg Med Chem Lett. 2004 May 3;14(9):2185-9.

PMID:
15081005
36.

Regulation of gene expression by PRA-910, a novel progesterone receptor modulator, in T47D cells.

Bray JD, Zhang Z, Winneker RC, Lyttle CR.

Steroids. 2003 Nov;68(10-13):995-1003.

PMID:
14667992
37.

The preclinical biology of a new potent and selective progestin: trimegestone.

Winneker RC, Bitran D, Zhang Z.

Steroids. 2003 Nov;68(10-13):915-20. Review.

PMID:
14667983
38.

Evaluation of an estrogen receptor-beta agonist in animal models of human disease.

Harris HA, Albert LM, Leathurby Y, Malamas MS, Mewshaw RE, Miller CP, Kharode YP, Marzolf J, Komm BS, Winneker RC, Frail DE, Henderson RA, Zhu Y, Keith JC Jr.

Endocrinology. 2003 Oct;144(10):4241-9. Erratum in: Endocrinology. 2006 May;147(5):2085.

PMID:
14500559
39.
40.

Rat uterine complement C3 expression as a model for progesterone receptor modulators: characterization of the new progestin trimegestone.

Lundeen SG, Zhang Z, Zhu Y, Carver JM, Winneker RC.

J Steroid Biochem Mol Biol. 2001 Aug;78(2):137-43.

PMID:
11566438
41.
44.

In vitro characterization of trimegestone: a new potent and selective progestin.

Zhang Z, Lundeen SG, Zhu Y, Carver JM, Winneker RC.

Steroids. 2000 Oct-Nov;65(10-11):637-43.

PMID:
11108870
45.

The effect of estrogens and antiestrogens in a rat model for hot flush.

Merchenthaler I, Funkhouser JM, Carver JM, Lundeen SG, Ghosh K, Winneker RC.

Maturitas. 1998 Nov 16;30(3):307-16.

PMID:
9881331
46.
47.

Characterization of the ovariectomized rat model for the evaluation of estrogen effects on plasma cholesterol levels.

Lundeen SG, Carver JM, McKean ML, Winneker RC.

Endocrinology. 1997 Apr;138(4):1552-8.

PMID:
9075715
48.

Non-steroidal glucocorticoid-like substances: receptor binding and in vivo activity.

Kumar V, Bell MR, Wetzel JR, Herrmann JL, McGarry R, Schane HP, Winneker RC, Snyder BW, Anzalone AJ.

J Med Chem. 1993 Oct 29;36(22):3278-85.

PMID:
8230118
49.

Antiandrogenic steroidal sulfonyl heterocycles. Utility of electrostatic complementarity in defining bioisosteric sulfonyl heterocycles.

Mallamo JP, Pilling GM, Wetzel JR, Kowalczyk PJ, Bell MR, Kullnig RK, Batzold FH, Juniewicz PE, Winneker RC, Luss HR.

J Med Chem. 1992 May 15;35(10):1663-70.

PMID:
1588549
50.

Antiandrogenic steroidal sulfonylpyrazoles.

Christiansen RG, Bell MR, D'Ambra TE, Mallamo JP, Herrmann JL, Ackerman JH, Opalka CJ, Kullnig RK, Winneker RC, Snyder BW, et al.

J Med Chem. 1990 Aug;33(8):2094-100.

PMID:
2374140

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