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Items: 1 to 20 of 80

1.

Discovery of novel indane derivatives as liver-selective thyroid hormone receptor β (TRβ) agonists for the treatment of dyslipidemia.

Shiohara H, Nakamura T, Kikuchi N, Ozawa T, Nagano R, Matsuzawa A, Ohnota H, Miyamoto T, Ichikawa K, Hashizume K.

Bioorg Med Chem. 2012 Jun 1;20(11):3622-34. doi: 10.1016/j.bmc.2012.03.056. Epub 2012 Apr 11.

PMID:
22542282
2.

Design, synthesis, and structure-activity relationship (SAR) of N-[7-(4-hydroxyphenoxy)-6-methylindan-4-yl]malonamic acids as thyroid hormone receptor β (TRβ) selective agonists.

Shiohara H, Nakamura T, Kikuchi N, Ozawa T, Matsuzawa A, Nagano R, Ohnota H, Miyamoto T, Ichikawa K, Hashizume K.

Bioorg Med Chem. 2013 Feb 1;21(3):592-607. doi: 10.1016/j.bmc.2012.12.002. Epub 2012 Dec 11.

PMID:
23276448
3.

Thyroid receptor ligands. 1. Agonist ligands selective for the thyroid receptor beta1.

Ye L, Li YL, Mellström K, Mellin C, Bladh LG, Koehler K, Garg N, Garcia Collazo AM, Litten C, Husman B, Persson K, Ljunggren J, Grover G, Sleph PG, George R, Malm J.

J Med Chem. 2003 Apr 24;46(9):1580-8.

PMID:
12699376
4.

Thyroid receptor ligands. Part 5: novel bicyclic agonist ligands selective for the thyroid hormone receptor beta.

Garcia Collazo AM, Koehler KF, Garg N, Färnegårdh M, Husman B, Ye L, Ljunggren J, Mellström K, Sandberg J, Grynfarb M, Ahola H, Malm J.

Bioorg Med Chem Lett. 2006 Mar 1;16(5):1240-4. Epub 2005 Dec 9.

PMID:
16338239
5.

Synthesis and biological evaluation of a series of liver-selective phosphonic acid thyroid hormone receptor agonists and their prodrugs.

Boyer SH, Jiang H, Jacintho JD, Reddy MV, Li H, Li W, Godwin JL, Schulz WG, Cable EE, Hou J, Wu R, Fujitaki JM, Hecker SJ, Erion MD.

J Med Chem. 2008 Nov 27;51(22):7075-93. doi: 10.1021/jm800824d.

PMID:
18975928
6.
7.

Targeting thyroid hormone receptor-beta agonists to the liver reduces cholesterol and triglycerides and improves the therapeutic index.

Erion MD, Cable EE, Ito BR, Jiang H, Fujitaki JM, Finn PD, Zhang BH, Hou J, Boyer SH, van Poelje PD, Linemeyer DL.

Proc Natl Acad Sci U S A. 2007 Sep 25;104(39):15490-5. Epub 2007 Sep 18.

8.
9.

Thyroid receptor ligands. Part 4: 4'-amido bioisosteric ligands selective for the thyroid hormone receptor beta.

Li YL, Litten C, Koehler KF, Mellström K, Garg N, Garcia Collazo AM, Färnegård M, Grynfarb M, Husman B, Sandberg J, Malm J.

Bioorg Med Chem Lett. 2006 Feb 15;16(4):884-6. Epub 2005 Nov 21.

PMID:
16303304
10.

Cardiac specific effects of thyroid hormone analogues.

Danzi S, Klein I.

Horm Metab Res. 2011 Oct;43(11):737-42. doi: 10.1055/s-0031-1291177. Epub 2011 Oct 18.

PMID:
22009366
11.

Design and synthesis of a novel series of [1-(4-hydroxy-benzyl)-1H-indol-5-yloxy]-acetic acid compounds as potent, selective, thyroid hormone receptor β agonists.

Burkholder TP, Cunningham BE, Clayton JR, Lander PA, Brown ML, Doti RA, Durst GL, Montrose-Rafizadeh C, King C, Osborne HE, Amos RM, Zink RW, Stramm LE, Burris TP, Cardona G, Konkol DL, Reidy C, Christe ME, Genin MJ.

Bioorg Med Chem Lett. 2015 Apr 1;25(7):1377-80. doi: 10.1016/j.bmcl.2015.02.062. Epub 2015 Mar 3.

PMID:
25752984
12.

Therapeutic potential for thyroid hormone receptor-beta selective agonists for treating obesity, hyperlipidemia and diabetes.

Grover GJ, Mellström K, Malm J.

Curr Vasc Pharmacol. 2007 Apr;5(2):141-54. Review.

PMID:
17430219
13.

Thyroid Hormone Mimetics: the Past, Current Status and Future Challenges.

Elbers LP, Kastelein JJ, Sjouke B.

Curr Atheroscler Rep. 2016 Mar;18(3):14. doi: 10.1007/s11883-016-0564-7. Review.

14.

Thyroid receptor ligands. Part 8: Thyromimetics derived from N-acylated-alpha-amino acid derivatives displaying modulated pharmacological selectivity compared with KB-141.

Garg N, Li YL, Garcia Collazo AM, Litten C, Ryono DE, Zhang M, Caringal Y, Brigance RP, Meng W, Washburn WN, Agback P, Mellström K, Rehnmark S, Rahimi-Ghadim M, Norin T, Grynfarb M, Sandberg J, Grover G, Malm J.

Bioorg Med Chem Lett. 2007 Aug 1;17(15):4131-4. Epub 2007 May 21.

PMID:
17543524
15.

Discovery of 2-[3,5-dichloro-4-(5-isopropyl-6-oxo-1,6-dihydropyridazin-3-yloxy)phenyl]-3,5-dioxo-2,3,4,5-tetrahydro[1,2,4]triazine-6-carbonitrile (MGL-3196), a Highly Selective Thyroid Hormone Receptor β agonist in clinical trials for the treatment of dyslipidemia.

Kelly MJ, Pietranico-Cole S, Larigan JD, Haynes NE, Reynolds CH, Scott N, Vermeulen J, Dvorozniak M, Conde-Knape K, Huang KS, So SS, Thakkar K, Qian Y, Banner B, Mennona F, Danzi S, Klein I, Taub R, Tilley J.

J Med Chem. 2014 May 22;57(10):3912-23. doi: 10.1021/jm4019299. Epub 2014 Apr 8.

PMID:
24712661
16.

Potential Role of Thyroid Receptor β Agonists in the Treatment of Hyperlipidemia.

Jakobsson T, Vedin LL, Parini P.

Drugs. 2017 Oct;77(15):1613-1621. doi: 10.1007/s40265-017-0791-4. Review.

17.

Thyroid hormone (T3) and TRbeta agonist GC-1 inhibit/reverse nonalcoholic fatty liver in rats.

Perra A, Simbula G, Simbula M, Pibiri M, Kowalik MA, Sulas P, Cocco MT, Ledda-Columbano GM, Columbano A.

FASEB J. 2008 Aug;22(8):2981-9. doi: 10.1096/fj.08-108464. Epub 2008 Apr 23.

PMID:
18434432
18.

Thyromimetics: a journey from bench to bed-side.

Tancevski I, Rudling M, Eller P.

Pharmacol Ther. 2011 Jul;131(1):33-9. doi: 10.1016/j.pharmthera.2011.04.003. Epub 2011 Apr 12. Review.

PMID:
21504761
19.

Design and synthesis of novel 3-hydroxy-cyclobut-3-ene-1,2-dione derivatives as thyroid hormone receptor beta (TR-beta) selective ligands.

Raval S, Raval P, Bandyopadhyay D, Soni K, Yevale D, Jogiya D, Modi H, Joharapurkar A, Gandhi N, Jain MR, Patel PR.

Bioorg Med Chem Lett. 2008 Jul 15;18(14):3919-24. doi: 10.1016/j.bmcl.2008.06.038. Epub 2008 Jun 14.

PMID:
18585912
20.

The thyroid hormone receptor-beta agonist GC-1 induces cell proliferation in rat liver and pancreas.

Columbano A, Pibiri M, Deidda M, Cossu C, Scanlan TS, Chiellini G, Muntoni S, Ledda-Columbano GM.

Endocrinology. 2006 Jul;147(7):3211-8. Epub 2006 Mar 30.

PMID:
16574785

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