Role of thyroid receptor β in lipid metabolism

Biochimica et Biophysica Acta - Molecular Basis of Disease

Volumn 1812, Issue 8, 2011, Pages 929-937

  Pramfalk, Camilla ^a   Pedrelli, Matteo ^a   Parini, Paolo ^a  

^a KAROLINSKA UNIVERSITY HOSPITAL   (Sweden)

Author keywords

Atherosclerosis; Cholesterol; Reverse cholesterol transport; Thyroid hormone; Thyroid receptor; Triglyceride

Indexed keywords

3,5 DIBROMO 3' (2,3 DIHYDRO 3 OXO 6 PYRIDAZINYLMETHYL)THYRONINE; 3,5 DIIODOTHYROPROPIONIC; ACETIC ACID DERIVATIVE; ANTILIPEMIC AGENT; ATORVASTATIN; CGH 509A; CGS 23425; CHOLESTEROL; DEXTROTHYROXINE; EPROTIROME; EZETIMIBE; KB 141; KB 3495; LIOTHYRONINE; LOW DENSITY LIPOPROTEIN RECEPTOR; M 07811; MB 07811; SIMVASTATIN; SOBETIROME; T 0681; TETRAIODOTHYROACETIC ACID; THYROID HORMONE; THYROID HORMONE RECEPTOR ALPHA; THYROID HORMONE RECEPTOR BETA; THYROID HORMONE RECEPTOR BETA1; THYROPROPIC ACID; THYROXINE; TIRATRICOL; TRIACYLGLYCEROL; UNCLASSIFIED DRUG; ZINC FINGER PROTEIN;

CHOLESTEROL BLOOD LEVEL; CHOLESTEROL METABOLISM; CONGESTIVE HEART FAILURE; CORONARY RISK; DISEASE ASSOCIATION; DOSE RESPONSE; DRUG EFFICACY; HORMONAL REGULATION; HORMONAL THERAPY; HORMONE SYNTHESIS; HUMAN; HYPERCHOLESTEROLEMIA; HYPERTHYROIDISM; HYPOTHYROIDISM; ISCHEMIC HEART DISEASE; LIGAND BINDING; LIPID METABOLISM; METABOLIC REGULATION; MONOTHERAPY; MYXEDEMA; NONHUMAN; NUCLEOTIDE BINDING SITE; OBESITY; PRIORITY JOURNAL; PROTEIN DNA BINDING; PROTEIN DOMAIN; PROTEIN MOTIF; REVIEW; TRIACYLGLYCEROL BLOOD LEVEL;

ALTERNATIVE SPLICING; HUMANS; LIPID METABOLISM; RECEPTORS, THYROID HORMONE; THYROID HORMONES;

EID: 79958257526     PISSN: 09254439     EISSN: 1879260X     Source Type: Journal    
DOI: 10.1016/j.bbadis.2010.12.019     Document Type: Review

References (131)

1. Glomset J.A. The plasma lecithins:cholesterol acyltransferase reaction. J. Lipid Res. 1968, 9:155-167.
2. van der Velde A.E., Vrins C.L., van den Oever K., Kunne C., Oude Elferink R.P., Kuipers F., Groen A.K. Direct intestinal cholesterol secretion contributes significantly to total fecal neutral sterol excretion in mice. Gastroenterology 2007, 133:967-975.
3. Kamstrup P.R., Benn M., Tybjaerg-Hansen A., Nordestgaard B.G. Extreme lipoprotein(a) levels and risk of myocardial infarction in the general population: the Copenhagen City Heart Study. Circulation 2008, 117:176-184.
4. Gudnason V. Lipoprotein(a): a causal independent risk factor for coronary heart disease?. Curr. Opin. Cardiol. 2009, 24:490-495.
5. Executive summary of the third report of The National Cholesterol Education Program (NCEP) expert panel on detection, evaluation, and treatment of high blood cholesterol in adults (Adult Treatment Panel III). Jama 2001, 285:2486-2497.
6. Baigent C., Keech A., Kearney P.M., Blackwell L., Buck G., Pollicino C., Kirby A., Sourjina T., Peto R., Collins R., Simes R. Efficacy and safety of cholesterol-lowering treatment: prospective meta-analysis of data from 90,056 participants in 14 randomised trials of statins. Lancet 2005, 366:1267-1278.
7. Gordon T., Castelli W.P., Hjortland M.C., Kannel W.B., Dawber T.R. High density lipoprotein as a protective factor against coronary heart disease. The Framingham study. Am. J. Med. 1977, 62:707-714.
8. Singh I.M., Shishehbor M.H., Ansell B.J. High-density lipoprotein as a therapeutic target: a systematic review. Jama 2007, 298:786-798.
9. Moreno M., de Lange P., Lombardi A., Silvestri E., Lanni A., Goglia F. Metabolic effects of thyroid hormone derivatives. Thyroid 2008, 18:239-253.
10. Oetting A., Yen P.M. New insights into thyroid hormone action. Best Pract. Res. 2007, 21:193-208.
11. Johansson L., Rudling M., Scanlan T.S., Lundasen T., Webb P., Baxter J., Angelin B., Parini P. Selective thyroid receptor modulation by GC-1 reduces serum lipids and stimulates steps of reverse cholesterol transport in euthyroid mice. Proc. Natl Acad. Sci. USA 2005, 102:10297-10302.
12. Tancevski I., Demetz E., Eller P., Duwensee K., Hoefer J., Heim C., Stanzl U., Wehinger A., Auer K., Karer R., Huber J., Schgoer W., Van Eck M., Vanhoutte J., Fievet C., Stellaard F., Rudling M., Patsch J.R., Ritsch A. The liver-selective thyromimetic T-0681 influences reverse cholesterol transport and atherosclerosis development in mice. PloS One 2010, 5:e8722.
13. Tancevski I., Wehinger A., Demetz E., Hoefer J., Eller P., Huber E., Stanzl U., Duwensee K., Auer K., Schgoer W., Kuhn V., Fievet C., Stellaard F., Rudling M., Foeger B., Patsch J.R., Ritsch A. The thyromimetic T-0681 protects from atherosclerosis. J. Lipid Res. 2009, 50:938-944.
14. Tancevski I., Wehinger A., Demetz E., Eller P., Duwensee K., Huber J., Hochegger K., Schgoer W., Fievet C., Stellaard F., Rudling M., Patsch J.R., Ritsch A. Reduced plasma high-density lipoprotein cholesterol in hyperthyroid mice coincides with decreased hepatic adenosine 5'-triphosphate-binding cassette transporter 1 expression. Endocrinology 2008, 149:3708-3712.
15. Bjorkhem I., Lund E., Rudling M. Coordinate regulation of cholesterol 7 alpha-hydroxylase and HMG-CoA reductase in the liver. Subcell. Biochem. 1997, 28:23-55.
16. Russell D.W., Setchell K.D. Bile acid biosynthesis. Biochemistry 1992, 31:4737-4749.
17. Kris-Etherton P.M., Fosmire M.A., Mela D.J., Etherton T.D. Studies on the etiology of increased tissue cholesterol concentration in cholesterol-fed hypothyroid rats. J. Nutr. 1982, 112:2324-2332.
18. Rudling M., Angelin B. Loss of resistance to dietary cholesterol in the rat after hypophysectomy: importance of the presence of growth hormone for hepatic low density lipoprotein-receptor expression. Proc. Natl Acad. Sci. USA 1993, 90:8851-8855.
19. Kohrle J. The selenoenzyme family of deiodinase isozymes controls local thyroid hormone availability. Rev. Endocr. Metab. Disord. 2000, 1:49-58.
20. St Germain D.L., Galton V.A., Hernandez A. Minireview: defining the roles of the iodothyronine deiodinases: current concepts and challenges. Endocrinology 2009, 150:1097-1107.
21. Engler D., Burger A.G. The deiodination of the iodothyronines and of their derivatives in man. Endocr. Rev. 1984, 5:151-184.
22. Maia A.L., Kim B.W., Huang S.A., Harney J.W., Larsen P.R. Type 2 iodothyronine deiodinase is the major source of plasma T3 in euthyroid humans. J. Clin. Investig. 2005, 115:2524-2533.
23. Farwell A.P., Dubord-Tomasetti S.A., Pietrzykowski A.Z., Leonard J.L. Dynamic nongenomic actions of thyroid hormone in the developing rat brain. Endocrinology 2006, 147:2567-2574.
24. Robbins J. Factors altering thyroid hormone metabolism. Environ. Health Perspect. 1981, 38:65-70.
25. Kester M.H., Kaptein E., Van Dijk C.H., Roest T.J., Tibboel D., Coughtrie M.W., Visser T.J. Characterization of iodothyronine sulfatase activities in human and rat liver and placenta. Endocrinology 2002, 143:814-819.
26. Visser T.J. Pathways of thyroid hormone metabolism. Acta Med. Austriaca 1996, 23:10-16.
27. Tata J.R., Widnell C.C. Ribonucleic acid synthesis during the early action of thyroid hormones. Biochem. J. 1966, 98:604-620.
28. Samuels H.H., Tsai J.S. Thyroid hormone action in cell culture: demonstration of nuclear receptors in intact cells and isolated nuclei. Proc. Natl Acad. Sci. USA 1973, 70:3488-3492.
29. Oppenheimer J.H., Schwartz H.L., Surks M.I. Tissue differences in the concentration of triiodothyronine nuclear binding sites in the rat: liver, kidney, pituitary, heart, brain, spleen, and testis. Endocrinology 1974, 95:897-903.
30. Weinberger C., Thompson C.C., Ong E.S., Lebo R., Gruol D.J., Evans R.M. The c-erb-A gene encodes a thyroid hormone receptor. Nature 1986, 324:641-646.
31. Sap J., Munoz A., Damm K., Goldberg Y., Ghysdael J., Leutz A., Beug H., Vennstrom B. The c-erb-A protein is a high-affinity receptor for thyroid hormone. Nature 1986, 324:635-640.
32. Mitsuhashi T., Tennyson G.E., Nikodem V.M. Alternative splicing generates messages encoding rat c-erbA proteins that do not bind thyroid hormone. Proc. Natl Acad. Sci. USA 1988, 85:5804-5808.
33. Plateroti M., Gauthier K., Domon-Dell C., Freund J.N., Samarut J., Chassande O. Functional interference between thyroid hormone receptor alpha (TRalpha) and natural truncated TRDeltaalpha isoforms in the control of intestine development. Mol. Cell. Biol. 2001, 21:4761-4772.
34. Williams G.R. Cloning and characterization of two novel thyroid hormone receptor beta isoforms. Mol. Cell. Biol. 2000, 20:8329-8342.
35. Hodin R.A., Lazar M.A., Chin W.W. Differential and tissue-specific regulation of the multiple rat c-erbA messenger RNA species by thyroid hormone. J. Clin. Investig. 1990, 85:101-105.
36. Yen P.M., Sunday M.E., Darling D.S., Chin W.W. Isoform-specific thyroid hormone receptor antibodies detect multiple thyroid hormone receptors in rat and human pituitaries. Endocrinology 1992, 130:1539-1546.
37. Cook C.B., Kakucska I., Lechan R.M., Koenig R.J. Expression of thyroid hormone receptor beta 2 in rat hypothalamus. Endocrinology 1992, 130:1077-1079.
38. Lazar M.A. Thyroid hormone receptors: multiple forms, multiple possibilities. Endocr. Rev. 1993, 14:184-193.
39. Yen P.M. Physiological and molecular basis of thyroid hormone action. Physiol. Rev. 2001, 81:1097-1142.
40. Zhang J., Lazar M.A. The mechanism of action of thyroid hormones. Annu. Rev. Physiol. 2000, 62:439-466.
41. Perissi V., Staszewski L.M., McInerney E.M., Kurokawa R., Krones A., Rose D.W., Lambert M.H., Milburn M.V., Glass C.K., Rosenfeld M.G. Molecular determinants of nuclear receptor-corepressor interaction. Genes Dev. 1999, 13:3198-3208.
42. Nagy L., Kao H.Y., Love J.D., Li C., Banayo E., Gooch J.T., Krishna V., Chatterjee K., Evans R.M., Schwabe J.W. Mechanism of corepressor binding and release from nuclear hormone receptors. Genes Dev. 1999, 13:3209-3216.
43. Hu X., Lazar M.A. The CoRNR motif controls the recruitment of corepressors by nuclear hormone receptors. Nature 1999, 402:93-96.
44. Onate S.A., Tsai S.Y., Tsai M.J., O'Malley B.W. Sequence and characterization of a coactivator for the steroid hormone receptor superfamily. Science 1995, 270:1354-1357.
45. Ito M., Roeder R.G. The TRAP/SMCC/Mediator complex and thyroid hormone receptor function. Trends Endocrinol. Metab.: TEM 2001, 12:127-134.
46. Flores-Morales A., Gullberg H., Fernandez L., Stahlberg N., Lee N.H., Vennstrom B., Norstedt G. Patterns of liver gene expression governed by TRbeta. Mol. Endocrinol. (Baltim. Md.) 2002, 16:1257-1268.
47. Cheng S.Y., Leonard J.L., Davis P.J. Molecular aspects of thyroid hormone actions. Endocrine reviews 2010, 31:139-170.
48. Mitchell C.S., Savage D.B., Dufour S., Schoenmakers N., Murgatroyd P., Befroy D., Halsall D., Northcott S., Raymond-Barker P., Curran S., Henning E., Keogh J., Owen P., Lazarus J., Rothman D.L., Farooqi I.S., Shulman G.I., Chatterjee K., Petersen K.F. Resistance to thyroid hormone is associated with raised energy expenditure, muscle mitochondrial uncoupling, and hyperphagia. J. Clin. Investig. 2010, 120:1345-1354.
49. Maruyama T., Miyamoto Y., Nakamura T., Tamai Y., Okada H., Sugiyama E., Nakamura T., Itadani H., Tanaka K. Identification of membrane-type receptor for bile acids (M-BAR). Biochem. Biophys. Res. Commun. 2002, 298:714-719.
50. Kawamata Y., Fujii R., Hosoya M., Harada M., Yoshida H., Miwa M., Fukusumi S., Habata Y., Itoh T., Shintani Y., Hinuma S., Fujisawa Y., Fujino M. A G protein-coupled receptor responsive to bile acids. J. Biol. Chem. 2003, 278:9435-9440.
51. Vassileva G., Golovko A., Markowitz L., Abbondanzo S.J., Zeng M., Yang S., Hoos L., Tetzloff G., Levitan D., Murgolo N.J., Keane K., Davis H.R., Hedrick J., Gustafson E.L. Targeted deletion of Gpbar1 protects mice from cholesterol gallstone formation. Biochem. J. 2006, 398:423-430.
52. Watanabe M., Houten S.M., Mataki C., Christoffolete M.A., Kim B.W., Sato H., Messaddeq N., Harney J.W., Ezaki O., Kodama T., Schoonjans K., Bianco A.C., Auwerx J. Bile acids induce energy expenditure by promoting intracellular thyroid hormone activation. Nature 2006, 439:484-489.
53. Croteau W., Davey J.C., Galton V.A., St.Germain D.L. Cloning of the mammalian type II iodothyronine deiodinase. A selenoprotein differentially expressed and regulated in human and rat brain and other tissues. J. Clin. Invest. 1996, 98:405-417.
54. Hosoi Y., Murakami M., Mizuma H., Ogiwara T., Imamura M., Mori M. Expression and regulation of type II iodothyronine deiodinase in cultured human skeletal muscle cells. J. Clin. Endocrinol. Metab. 1999, 84:3293-3300.
55. Staels B., Van Tol A., Chan L., Will H., Verhoeven G., Auwerx J. Alterations in thyroid status modulate apolipoprotein, hepatic triglyceride lipase, and low density lipoprotein receptor in rats. Endocrinology 1990, 127:1144-1152.
56. Salter A.M., Hayashi R., Al-Seeni M., Brown N.F., Bruce J., Sorensen O., Atkinson E.A., Middleton B., Bleackley R.C., Brindley D.N. Effects of hypothyroidism and high-fat feeding on mRNA concentrations for the low-density-lipoprotein receptor and on acyl-CoA:cholesterol acyltransferase activities in rat liver. Biochem. J. 1991, 276(Pt 3):825-832.
57. Meyer B.J., Ha Y.C., Barter P.J. Effects of experimental hypothyroidism on the distribution of lipids and lipoproteins in the plasma of rats. Biochim. Biophys. Acta 1989, 1004:73-79.
58. Gross G., Sykes M., Arellano R., Fong B., Angel A. HDL clearance and receptor-mediated catabolism of LDL are reduced in hypothyroid rats. Atherosclerosis 1987, 66:269-275.
59. Apostolopoulos J.J., Marshall J.F., Howlett G.J. Triiodothyronine increases rat apolipoprotein A-I synthesis and alters high-density lipoprotein composition in vivo. Eur. J. Biochem. 1990, 194:147-154.
60. Cappola A.R., Ladenson P.W. Hypothyroidism and atherosclerosis. J. Clin. Endocrinol. Metab. 2003, 88:2438-2444.
61. Friis T., Pedersen L.R. Serum lipids in hyper- and hypothyroidism before and after treatment. Clin. Chim. Acta 1987, 162:155-163.
62. Scottolini A.G., Bhagavan N.V., Oshiro T.H., Abe S.Y. Serum high-density lipoprotein cholesterol concentrations in hypo- and hyperthyroidism. Clin. Chem. 1980, 26:584-587.
63. Lee W.Y., Suh J.Y., Rhee E.J., Park J.S., Sung K.C., Kim S.W. Plasma CRP, apolipoprotein A-1, apolipoprotein B and Lpa levels according to thyroid function status. Arch. Med. Res. 2004, 35:540-545.
64. Muls E., Rosseneu M., Blaton V., Lesaffre E., Lamberigts G., de Moor P. Serum lipids and apolipoproteins A-I, A-II and B in primary hypothyroidism before and during treatment. Eur. J. Clin. Invest. 1984, 14:12-15.
65. Abrams J.J., Grundy S.M. Cholesterol metabolism in hypothyroidism and hyperthyroidism in man. J. Lipid Res. 1981, 22:323-338.
66. Agdeppa D., Macaron C., Mallik T., Schnuda N.D. Plasma high density lipoprotein cholesterol in thyroid disease. J. Clin. Endocrinol. Metab. 1979, 49:726-729.
67. Tulloch B.R., Lewis B., Fraser T.R. Triglyceride metabolism in thyroid disease. Lancet 1973, 1:391-394.
68. Danesh J., Collins R., Peto R. Lipoprotein(a) and coronary heart disease. Meta-analysis of prospective studies. Circulation 2000, 102:1082-1085.
69. de Bruin T.W., van Barlingen H., van Linde-Sibenius Trip M., van Vuurst de Vries A.R., Akveld M.J., Erkelens D.W. Lipoprotein(a) and apolipoprotein B plasma concentrations in hypothyroid, euthyroid, and hyperthyroid subjects. J. Clin. Endocrinol. Metab. 1993, 76:121-126.
70. Miettinen T.A. Mechanism of serum cholesterol reduction by thyroid hormones in hypothyroidism. J. Lab. Clin. Med. 1968, 71:537-547.
71. Nikkila E.A., Kekki M. Plasma triglyceride metabolism in thyroid disease. J. Clin. Investig. 1972, 51:2103-2114.
72. Osman F., Franklyn J.A., Holder R.L., Sheppard M.C., Gammage M.D. Cardiovascular manifestations of hyperthyroidism before and after antithyroid therapy: a matched case-control study. J. Am. Coll. Cardiol. 2007, 49:71-81.
73. Ochs N., Auer R., Bauer D.C., Nanchen D., Gussekloo J., Cornuz J., Rodondi N. Meta-analysis: subclinical thyroid dysfunction and the risk for coronary heart disease and mortality. Ann. Intern. Med. 2008, 148:832-845.
74. Kahaly G.J., Dillmann W.H. Thyroid hormone action in the heart. Endocr. Rev. 2005, 26:704-728.
75. Muls E., Blaton V., Rosseneu M., Lesaffre E., Lamberigts G., De Moor P. Serum lipids and apolipoproteins A-I, A-II, and B in hyperthyroidism before and after treatment. J. Clin. Endocrinol. Metab. 1982, 55:459-464.
76. Strisower B., Gofman J.W., Galioni E.F., Almada A.A., Simon A. Effect of thyroid extract on serum lipoproteins and serum cholesterol. Metabolism 1954, 3:218-227.
77. Strisower B., Gofman J.W., Galioni E., Rubinger J.H., O'Brien G.W., Simon A. Effect of long-term administration of desiccated thyroid on serum lipoprotein and cholesterol levels. J. Clin. Endocrinol. Metab. 1955, 15:73-80.
78. Galioni E.F., Gofman J.W., Guzvich P., Pouteau J., Rubinger J.H., Strisower B. Long-term effect of dried thyroid on serum-lipoprotein and serum-cholesterol levels. Lancet 1957, 272:120-123.
79. Rawson R.W., Money W.L., Kroc R.L., Kumaoka S., Benua R.S., Leeper R.D. A dissociation of thyroid hormonal effects by structural alterations of the thyroxine molecule. Am. J. Med. Sci. 1959, 238:261-273.
80. Leeper R.D., Mead A.W., Money W.L., Rawson R.W. Metabolic effects and therapeutic applications of triiodothyropropionic acid. Clin. Pharmacol. Ther. 1961, 2:13-21.
81. Hill S.R., Barker S.B., Mc N.J., Tingley J.O., Hibbett L.L. The metabolic effects of the acetic and propionic acid analogs of thyroxine and triiodothyronine. J. Clin. Investig. 1960, 39:523-533.
82. Pennock G.D., Raya T.E., Bahl J.J., Goldman S., Morkin E. Cardiac effects of 3,5-diiodothyropropionic acid, a thyroid hormone analog with inotropic selectivity. J. Pharmacol. Exp. Ther. 1992, 263:163-169.
83. Morkin E., Pennock G., Spooner P.H., Bahl J.J., Underhill Fox K., Goldman S. Pilot studies on the use of 3,5-diiodothyropropionic acid, a thyroid hormone analog, in the treatment of congestive heart failure. Cardiology 2002, 97:218-225.
84. Lerman J., Pitt-Rivers R. Physiologic activity of triiodo- and tetraiodo-thyroacetic acid in human myxedema. J. Clin. Endocrinol. Metab. 1956, 16:1470-1479.
85. Sherman S.I., Ladenson P.W. Organ-specific effects of tiratricol: a thyroid hormone analog with hepatic, not pituitary, superagonist effects. J. Clin. Endocrinol. Metab. 1992, 75:901-905.
86. Schueler P.A., Schwartz H.L., Strait K.A., Mariash C.N., Oppenheimer J.H. Binding of 3,5,3'-triiodothyronine (T3) and its analogs to the in vitro translational products of c-erbA protooncogenes: differences in the affinity of the alpha- and beta-forms for the acetic acid analog and failure of the human testis and kidney alpha-2 products to bind T3. Mol. Endocrinol. 1990, 4:227-234.
87. Sherman S.I., Ringel M.D., Smith M.J., Kopelen H.A., Zoghbi W.A., Ladenson P.W. Augmented hepatic and skeletal thyromimetic effects of tiratricol in comparison with levothyroxine. J. Clin. Endocrinol. Metab. 1997, 82:2153-2158.
88. The coronary drug project. Findings leading to further modifications of its protocol with respect to dextrothyroxine. The coronary drug project research group. Jama 1972, 220:996-1008.
89. Young W.F., Gorman C.A., Jiang N.S., Machacek D., Hay I.D. l-thyroxine contamination of pharmaceutical d-thyroxine: probable cause of therapeutic effect. Clin. Pharmacol. Ther. 1984, 36:781-787.
90. Baxter J.D., Dillmann W.H., West B.L., Huber R., Furlow J.D., Fletterick R.J., Webb P., Apriletti J.W., Scanlan T.S. Selective modulation of thyroid hormone receptor action. J. Steroid Biochem. Mol. Biol. 2001, 76:31-42.
91. Forrest D., Hanebuth E., Smeyne R.J., Everds N., Stewart C.L., Wehner J.M., Curran T. Recessive resistance to thyroid hormone in mice lacking thyroid hormone receptor beta: evidence for tissue-specific modulation of receptor function. EMBO J. 1996, 15:3006-3015.
92. Gothe S., Wang Z., Ng L., Kindblom J.M., Barros A.C., Ohlsson C., Vennstrom B., Forrest D. Mice devoid of all known thyroid hormone receptors are viable but exhibit disorders of the pituitary-thyroid axis, growth, and bone maturation. Genes Dev. 1999, 13:1329-1341.
93. Ng L., Hurley J.B., Dierks B., Srinivas M., Salto C., Vennstrom B., Reh T.A., Forrest D. A thyroid hormone receptor that is required for the development of green cone photoreceptors. Nat. Genet. 2001, 27:94-98.
94. Ng L., Rusch A., Amma L.L., Nordstrom K., Erway L.C., Vennstrom B., Forrest D. Suppression of the deafness and thyroid dysfunction in Thrb-null mice by an independent mutation in the Thra thyroid hormone receptor alpha gene. Hum. Mol. Genet. 2001, 10:2701-2708.
95. Salto C., Kindblom J.M., Johansson C., Wang Z., Gullberg H., Nordstrom K., Mansen A., Ohlsson C., Thoren P., Forrest D., Vennstrom B. Ablation of TRalpha2 and a concomitant overexpression of alpha1 yields a mixed hypo- and hyperthyroid phenotype in mice. Mol. Endocrinol. 2001, 15:2115-2128.
96. Wikstrom L., Johansson C., Salto C., Barlow C., Campos Barros A., Baas F., Forrest D., Thoren P., Vennstrom B. Abnormal heart rate and body temperature in mice lacking thyroid hormone receptor alpha 1. EMBO J. 1998, 17:455-461.
97. Gloss B., Trost S., Bluhm W., Swanson E., Clark R., Winkfein R., Janzen K., Giles W., Chassande O., Samarut J., Dillmann W. Cardiac ion channel expression and contractile function in mice with deletion of thyroid hormone receptor alpha or beta. Endocrinology 2001, 142:544-550.
98. Johansson C., Vennstrom B., Thoren P. Evidence that decreased heart rate in thyroid hormone receptor-alpha1-deficient mice is an intrinsic defect. Am. J. Physiol. 1998, 275:R640-R646.
99. Gullberg H., Rudling M., Salto C., Forrest D., Angelin B., Vennstrom B. Requirement for thyroid hormone receptor beta in T3 regulation of cholesterol metabolism in mice. Mol. Endocrinol. 2002, 16:1767-1777.
100. Leeson P.D., Ellis D., Emmett J.C., Shah V.P., Showell G.A., Underwood A.H. Thyroid hormone analogues. Synthesis of 3'-substituted 3,5-diiodo-l-thyronines and quantitative structure-activity studies of in vitro and in vivo thyromimetic activities in rat liver and heart. J. Med. Chem. 1988, 31:37-54.
101. Underwood A.H., Emmett J.C., Ellis D., Flynn S.B., Leeson P.D., Benson G.M., Novelli R., Pearce N.J., Shah V.P. A thyromimetic that decreases plasma cholesterol levels without increasing cardiac activity. Nature 1986, 324:425-429.
102. Grover G.J., Egan D.M., Sleph P.G., Beehler B.C., Chiellini G., Nguyen N.H., Baxter J.D., Scanlan T.S. Effects of the thyroid hormone receptor agonist GC-1 on metabolic rate and cholesterol in rats and primates: selective actions relative to 3,5,3'-triiodo-l-thyronine. Endocrinology 2004, 145:1656-1661.
103. Grover G.J., Mellstrom K., Ye L., Malm J., Li Y.L., Bladh L.G., Sleph P.G., Smith M.A., George R., Vennstrom B., Mookhtiar K., Horvath R., Speelman J., Egan D., Baxter J.D. Selective thyroid hormone receptor-beta activation: a strategy for reduction of weight, cholesterol, and lipoprotein (a) with reduced cardiovascular liability. Proc. Natl Acad. Sci. USA 2003, 100:10067-10072.
104. Trost S.U., Swanson E., Gloss B., Wang-Iverson D.B., Zhang H., Volodarsky T., Grover G.J., Baxter J.D., Chiellini G., Scanlan T.S., Dillmann W.H. The thyroid hormone receptor-beta-selective agonist GC-1 differentially affects plasma lipids and cardiac activity. Endocrinology 2000, 141:3057-3064.
105. Erion M.D., Cable E.E., Ito B.R., Jiang H., Fujitaki J.M., Finn P.D., Zhang B.H., Hou J., Boyer S.H., van Poelje P.D., Linemeyer D.L. Targeting thyroid hormone receptor-beta agonists to the liver reduces cholesterol and triglycerides and improves the therapeutic index. Proc. Natl Acad. Sci. USA 2007, 104:15490-15495.
106. Ito B.R., Zhang B.H., Cable E.E., Song X., Fujitaki J.M., MacKenna D.A., Wilker C.E., Chi B., van Poelje P.D., Linemeyer D.L., Erion M.D. Thyroid hormone beta receptor activation has additive cholesterol lowering activity in combination with atorvastatin in rabbits, dogs and monkeys. Br. J. Pharmacol. 2009, 156:454-465.
107. Bryzgalova G., Effendic S., Khan A., Rehnmark S., Barbounis P., Boulet J., Dong G., Singh R., Shapses S., Malm J., Webb P., Baxter J.D., Grover G.J. Anti-obesity, anti-diabetic, and lipid lowering effects of the thyroid receptor beta subtype selective agonist KB-141. J. Steroid Biochem. Mol. Biol. 2008, 111:262-267.
108. Taylor A.H., Stephan Z.F., Steele R.E., Wong N.C. Beneficial effects of a novel thyromimetic on lipoprotein metabolism. Mol. Pharmacol. 1997, 52:542-547.
109. Scanlan T.S. Sobetirome: a case history of bench-to-clinic drug discovery and development. Heart Fail. Rev. 2010, 15:177-182.
110. 2008. http://www.quatrx.com/news/01_29_08.htm.
111. Berkenstam A., Kristensen J., Mellstrom K., Carlsson B., Malm J., Rehnmark S., Garg N., Andersson C.M., Rudling M., Sjoberg F., Angelin B., Baxter J.D. The thyroid hormone mimetic compound KB2115 lowers plasma LDL cholesterol and stimulates bile acid synthesis without cardiac effects in humans. Proc. Natl Acad. Sci. USA 2008, 105:663-667.
112. Bjorkhem I., Araya Z., Rudling M., Angelin B., Einarsson C., Wikvall K. Differences in the regulation of the classical and the alternative pathway for bile acid synthesis in human liver. No coordinate regulation of CYP7A1 and CYP27A1. J. Biol. Chem. 2002, 277:26804-26807.
113. Axelson M., Aly A., Sjovall J. Levels of 7 alpha-hydroxy-4-cholesten-3-one in plasma reflect rates of bile acid synthesis in man. FEBS Lett. 1988, 239:324-328.
114. Axelson M., Bjorkhem I., Reihner E., Einarsson K. The plasma level of 7 alpha-hydroxy-4-cholesten-3-one reflects the activity of hepatic cholesterol 7 alpha-hydroxylase in man. FEBS Lett. 1991, 284:216-218.
115. Sauter G., Berr F., Beuers U., Fischer S., Paumgartner G. Serum concentrations of 7alpha-hydroxy-4-cholesten-3-one reflect bile acid synthesis in humans. Hepatology (Baltim. Md.) 1996, 24:123-126.
116. Galman C., Arvidsson I., Angelin B., Rudling M. Monitoring hepatic cholesterol 7alpha-hydroxylase activity by assay of the stable bile acid intermediate 7alpha-hydroxy-4-cholesten-3-one in peripheral blood. J. Lipid Res. 2003, 44:859-866.
117. (2009). http://www.thyroid.org/ann_mtg/2009_80th/documents/2009_ATA_short_call_abstracts.pdf.
118. Ladenson P.W., Kristensen J.D., Ridgway E.C., Olsson A.G., Carlsson B., Klein I., Baxter J.D., Angelin B. Use of the thyroid hormone analogue eprotirome in statin-treated dyslipidemia. N. Engl. J. Med. 2010, 362:906-916.
119. (2008). http://seekingalpha.com/article/105864-metabasis-therapeutics-incorporated-q3-2008-earnings-call-transcript.
120. (2009). http://clinicaltrials.gov/ct2/show/NCT00879112.
121. Bakker O., Hudig F., Meijssen S., Wiersinga W.M. Effects of triiodothyronine and amiodarone on the promoter of the human LDL receptor gene. Biochem. Biophys. Res. Commun. 1998, 249:517-521.
122. Lopez D., Abisambra Socarras J.F., Bedi M., Ness G.C. Activation of the hepatic LDL receptor promoter by thyroid hormone. Biochim. Biophys. Acta 2007, 1771:1216-1225.
123. Ness G.C., Pendleton L.C., Li Y.C., Chiang J.Y. Effect of thyroid hormone on hepatic cholesterol 7 alpha hydroxylase, LDL receptor, HMG-CoA reductase, farnesyl pyrophosphate synthetase and apolipoprotein A-I mRNA levels in hypophysectomized rats. Biochem. Biophys. Res. Commun. 1990, 172:1150-1156.
124. Gullberg H., Rudling M., Forrest D., Angelin B., Vennstrom B. Thyroid hormone receptor beta-deficient mice show complete loss of the normal cholesterol 7alpha-hydroxylase (CYP7A) response to thyroid hormone but display enhanced resistance to dietary cholesterol. Mol. Endocrinol. 2000, 14:1739-1749.
125. Hashimoto K., Cohen R.N., Yamada M., Markan K.R., Monden T., Satoh T., Mori M., Wondisford F.E. Cross-talk between thyroid hormone receptor and liver X receptor regulatory pathways is revealed in a thyroid hormone resistance mouse model. J. Biol. Chem. 2006, 281:295-302.
126. Hashimoto K., Yamada M., Matsumoto S., Monden T., Satoh T., Mori M. Mouse sterol response element binding protein-1c gene expression is negatively regulated by thyroid hormone. Endocrinology 2006, 147:4292-4302.
127. Tancevski I., Demetz E., Eller P., Duwensee K., Hoefer J., Heim C., Stanzl U., Wehinger A., Auer K., Karer R., Huber J., Schgoer W., Van Eck M., Vanhoutte J., Fievet C., Stellaard F., Rudling M., Patsch J.R., Ritsch A. The liver-selective thyromimetic T-0681 influences reverse cholesterol transport and atherosclerosis development in mice. PLoS ONE 2010, 5:e8722.
128. Pandak W.M., Heuman D.M., Redford K., Stravitz R.T., Chiang J.Y., Hylemon P.B., Vlahcevic Z.R. Hormonal regulation of cholesterol 7alpha-hydroxylase specific activity, mRNA levels, and transcriptional activity in vivo in the rat. J. Lipid Res. 1997, 38:2483-2491.
129. Galman C., Bonde Y., Matasconi M., Angelin B., Rudling M. Dramatically increased intestinal absorption of cholesterol following hypophysectomy is normalized by thyroid hormone. Gastroenterology 2008, 134:1127-1136.
130. Nilsson L., Rehnmark S., Dovoodpour P., Larsson L., Parini P. Thyroid hormone receptor modulation reduces the atherosclerotic process through increased reverse cholesterol transport. Artherioscl. Thromb. Vasc. Biol. 2009, 29:P325.
131. Cuchel M., Rader D.J. Macrophage reverse cholesterol transport: key to the regression of atherosclerosis?. Circulation 2006, 113:2548-2555.