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Items: 30

1.

Discovery of 3-Cyano- N-(3-(1-isobutyrylpiperidin-4-yl)-1-methyl-4-(trifluoromethyl)-1 H-pyrrolo[2,3- b]pyridin-5-yl)benzamide: A Potent, Selective, and Orally Bioavailable Retinoic Acid Receptor-Related Orphan Receptor C2 Inverse Agonist.

Schnute ME, Wennerstål M, Alley J, Bengtsson M, Blinn JR, Bolten CW, Braden T, Bonn T, Carlsson B, Caspers N, Chen M, Choi C, Collis LP, Crouse K, Färnegårdh M, Fennell KF, Fish S, Flick AC, Goos-Nilsson A, Gullberg H, Harris PK, Heasley SE, Hegen M, Hromockyj AE, Hu X, Husman B, Janosik T, Jones P, Kaila N, Kallin E, Kauppi B, Kiefer JR, Knafels J, Koehler K, Kruger L, Kurumbail RG, Kyne RE Jr, Li W, Löfstedt J, Long SA, Menard CA, Mente S, Messing D, Meyers MJ, Napierata L, Nöteberg D, Nuhant P, Pelc MJ, Prinsen MJ, Rhönnstad P, Backström-Rydin E, Sandberg J, Sandström M, Shah F, Sjöberg M, Sundell A, Taylor AP, Thorarensen A, Trujillo JI, Trzupek JD, Unwalla R, Vajdos FF, Weinberg RA, Wood DC, Xing L, Zamaratski E, Zapf CW, Zhao Y, Wilhelmsson A, Berstein G.

J Med Chem. 2018 Dec 13;61(23):10415-10439. doi: 10.1021/acs.jmedchem.8b00392. Epub 2018 Sep 9.

PMID:
30130103
2.

Motivation to uphold physical activity in women with breast cancer during adjuvant chemotherapy treatment.

Wilhelmsson A, Roos M, Hagberg L, Wengström Y, Blomberg K.

Eur J Oncol Nurs. 2017 Aug;29:17-22. doi: 10.1016/j.ejon.2017.03.008. Epub 2017 May 3.

PMID:
28720261
3.

Synthesis of 4-(3-biaryl)quinoline sulfones as potent liver X receptor agonists.

Ullrich JW, Morris R, Bernotas RC, Travins JM, Jetter J, Unwalla R, Quinet E, Nambi P, Feingold I, Huselton C, Enroth C, Wilhelmsson A, Goos-Nilsson A, Wrobel J.

Bioorg Med Chem Lett. 2010 May 1;20(9):2903-7. doi: 10.1016/j.bmcl.2010.03.031. Epub 2010 Mar 9.

PMID:
20382019
4.

Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist.

Hu B, Unwalla RJ, Goljer I, Jetter JW, Quinet EM, Berrodin TJ, Basso MD, Feingold IB, Nilsson AG, Wilhelmsson A, Evans MJ, Wrobel JE.

J Med Chem. 2010 Apr 22;53(8):3296-304. doi: 10.1021/jm100034x.

PMID:
20350005
5.

1-(3-Aryloxyaryl)benzimidazole sulfones are liver X receptor agonists.

Travins JM, Bernotas RC, Kaufman DH, Quinet E, Nambi P, Feingold I, Huselton C, Wilhelmsson A, Goos-Nilsson A, Wrobel J.

Bioorg Med Chem Lett. 2010 Jan 15;20(2):526-30. doi: 10.1016/j.bmcl.2009.11.099. Epub 2009 Nov 23.

PMID:
20006495
6.

3-(3-Aryloxyaryl)imidazo[1,2-a]pyridine sulfones as liver X receptor agonists.

Singhaus RR, Bernotas RC, Steffan R, Matelan E, Quinet E, Nambi P, Feingold I, Huselton C, Wilhelmsson A, Goos-Nilsson A, Wrobel J.

Bioorg Med Chem Lett. 2010 Jan 15;20(2):521-5. doi: 10.1016/j.bmcl.2009.11.098. Epub 2009 Nov 23.

PMID:
20005711
7.

Quinoline-3-carboxamide containing sulfones as liver X receptor (LXR) agonists with binding selectivity for LXRbeta and low blood-brain penetration.

Hu B, Bernotas R, Unwalla R, Collini M, Quinet E, Feingold I, Goos-Nilsson A, Wilhelmsson A, Nambi P, Evans M, Wrobel J.

Bioorg Med Chem Lett. 2010 Jan 15;20(2):689-93. doi: 10.1016/j.bmcl.2009.11.062. Epub 2009 Dec 3.

PMID:
19962892
8.

4-(3-Aryloxyaryl)quinoline sulfones are potent liver X receptor agonists.

Bernotas RC, Singhaus RR, Kaufman DH, Travins JM, Ullrich JW, Unwalla R, Quinet E, Evans M, Nambi P, Olland A, Kauppi B, Wilhelmsson A, Goos-Nilsson A, Wrobel J.

Bioorg Med Chem Lett. 2010 Jan 1;20(1):209-12. doi: 10.1016/j.bmcl.2009.10.132. Epub 2009 Oct 31.

PMID:
19932617
9.

4-(3-aryloxyaryl)quinoline alcohols are liver X receptor agonists.

Bernotas RC, Kaufman DH, Singhaus RR, Ullrich J, Unwalla R, Quinet E, Nambi P, Wilhelmsson A, Goos-Nilsson A, Wrobel J.

Bioorg Med Chem. 2009 Dec 1;17(23):8086-92. doi: 10.1016/j.bmc.2009.10.001. Epub 2009 Oct 4.

PMID:
19853462
10.

Biarylether amide quinolines as liver X receptor agonists.

Bernotas RC, Singhaus RR, Kaufman DH, Ullrich J, Fletcher H 3rd, Quinet E, Nambi P, Unwalla R, Wilhelmsson A, Goos-Nilsson A, Farnegardh M, Wrobel J.

Bioorg Med Chem. 2009 Feb 15;17(4):1663-70. doi: 10.1016/j.bmc.2008.12.048. Epub 2008 Dec 27.

PMID:
19162487
11.

Indazole-based liver X receptor (LXR) modulators with maintained atherosclerotic lesion reduction activity but diminished stimulation of hepatic triglyceride synthesis.

Wrobel J, Steffan R, Bowen SM, Magolda R, Matelan E, Unwalla R, Basso M, Clerin V, Gardell SJ, Nambi P, Quinet E, Reminick JI, Vlasuk GP, Wang S, Feingold I, Huselton C, Bonn T, Farnegardh M, Hansson T, Nilsson AG, Wilhelmsson A, Zamaratski E, Evans MJ.

J Med Chem. 2008 Nov 27;51(22):7161-8. doi: 10.1021/jm800799q.

PMID:
18973288
12.

Carboxylic acid based quinolines as liver X receptor modulators that have LXRbeta receptor binding selectivity.

Hu B, Quinet E, Unwalla R, Collini M, Jetter J, Dooley R, Andraka D, Nogle L, Savio D, Halpern A, Goos-Nilsson A, Wilhelmsson A, Nambi P, Wrobel J.

Bioorg Med Chem Lett. 2008 Jan 1;18(1):54-9. Epub 2007 Nov 9.

PMID:
18023179
13.

Further modification on phenyl acetic acid based quinolines as liver X receptor modulators.

Hu B, Jetter J, Kaufman D, Singhaus R, Bernotas R, Unwalla R, Quinet E, Savio D, Halpern A, Basso M, Keith J, Clerin V, Chen L, Liu QY, Feingold I, Huselton C, Azam F, Goos-Nilsson A, Wilhelmsson A, Nambi P, Wrobel J.

Bioorg Med Chem. 2007 May 15;15(10):3321-33. Epub 2007 Mar 12.

PMID:
17391964
14.

Discovery of phenyl acetic acid substituted quinolines as novel liver X receptor agonists for the treatment of atherosclerosis.

Hu B, Collini M, Unwalla R, Miller C, Singhaus R, Quinet E, Savio D, Halpern A, Basso M, Keith J, Clerin V, Chen L, Resmini C, Liu QY, Feingold I, Huselton C, Azam F, Farnegardh M, Enroth C, Bonn T, Goos-Nilsson A, Wilhelmsson A, Nambi P, Wrobel J.

J Med Chem. 2006 Oct 19;49(21):6151-4.

PMID:
17034119
15.

The three-dimensional structure of the liver X receptor beta reveals a flexible ligand-binding pocket that can accommodate fundamentally different ligands.

Färnegårdh M, Bonn T, Sun S, Ljunggren J, Ahola H, Wilhelmsson A, Gustafsson JA, Carlquist M.

J Biol Chem. 2003 Oct 3;278(40):38821-8. Epub 2003 Jun 20.

16.

Process-induced changes on bioactive compounds in whole grain rye.

Liukkonen KH, Katina K, Wilhelmsson A, Myllymäki O, Lampi AM, Kariluoto S, Piironen V, Heinonen SM, Nurmi T, Adlercreutz H, Peltoketo A, Pihlava JM, Hietaniemi V, Poutanen K.

Proc Nutr Soc. 2003 Feb;62(1):117-22. Review.

PMID:
12740066
17.
18.

Purification of the DNA binding form of dioxin receptor. Role of the Arnt cofactor in regulation of dioxin receptor function.

Mason GG, Witte AM, Whitelaw ML, Antonsson C, McGuire J, Wilhelmsson A, Poellinger L, Gustafsson JA.

J Biol Chem. 1994 Feb 11;269(6):4438-49.

19.

Dioxin receptor and C/EBP regulate the function of the glutathione S-transferase Ya gene xenobiotic response element.

Pimental RA, Liang B, Yee GK, Wilhelmsson A, Poellinger L, Paulson KE.

Mol Cell Biol. 1993 Jul;13(7):4365-73.

20.

Ligand-dependent recruitment of the Arnt coregulator determines DNA recognition by the dioxin receptor.

Whitelaw M, Pongratz I, Wilhelmsson A, Gustafsson JA, Poellinger L.

Mol Cell Biol. 1993 Apr;13(4):2504-14.

21.
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24.

Activation of the dioxin and glucocorticoid receptors to a DNA binding state under cell-free conditions.

Nemoto T, Mason GG, Wilhelmsson A, Cuthill S, Hapgood J, Gustafsson JA, Poellinger L.

J Biol Chem. 1990 Feb 5;265(4):2269-77.

25.

The specific DNA binding activity of the dioxin receptor is modulated by the 90 kd heat shock protein.

Wilhelmsson A, Cuthill S, Denis M, Wikström AC, Gustafsson JA, Poellinger L.

EMBO J. 1990 Jan;9(1):69-76.

26.

Structural differences between the glucocorticoid, dioxin and oxysterol receptors from rat liver cytosol.

Denis M, Wilhelmsson A, Cuthill S, Poellinger L, Gustafsson JA.

Biochem Biophys Res Commun. 1989 Aug 30;163(1):444-51.

PMID:
2549994
27.

Ligand-dependent interaction of the dioxin receptor with target DNA.

Cuthill S, Hapgood J, Denis M, Wilhelmsson A, Mason G, Nemoto T, Widmark E, Poellinger L, Gustafsson JA.

J Steroid Biochem. 1989;34(1-6):375-7.

PMID:
2560518
28.

The dioxin receptor: characterization of its DNA-binding properties.

Mason GG, Wilhelmsson A, Cuthill S, Gillner M, Poellinger L, Gustafsson JA.

J Steroid Biochem. 1988;30(1-6):307-10.

PMID:
3386258
29.

The dioxin receptor: a comparison with the glucocorticoid receptor.

Cuthill S, Wilhelmsson A, Mason GG, Gillner M, Poellinger L, Gustafsson JA.

J Steroid Biochem. 1988;30(1-6):277-80.

PMID:
3386253
30.

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