In vivo activity of the thyroid hormone receptor β- and α-selective agonists GC-24 and CO23 on rat liver, heart, and brain

Endocrinology

Volumn 152, Issue 3, 2011, Pages 1136-1142

  Grijota Martínez, Carmen ^b   Samarut, Eric ^a   Scanlan, Thomas S ^c   Morte, Beatriz ^b   Bernal, Juan ^a,b  

^a CSIC   (Spain)

^b Center for Biomedical Research on Rare Diseases   (Spain)

^c OREGON HEALTH AND SCIENCE UNIVERSITY   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

CO23; GC 24; HORMONE RECEPTOR STIMULATING AGENT; THYROID HORMONE RECEPTOR ALPHA; THYROID HORMONE RECEPTOR BETA; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ARTICLE; BRAIN; DRUG ACTIVITY; DRUG EFFECT; GENE CONTROL; GENE EXPRESSION; HEART; IN VIVO STUDY; LIVER; NONHUMAN; PRIORITY JOURNAL; RAT;

ACETIC ACIDS; ANIMALS; BENZHYDRYL COMPOUNDS; BRAIN; GENE EXPRESSION REGULATION; HEART; HYDANTOINS; HYPOTHYROIDISM; LIVER; RATS; RATS, WISTAR; THYROID HORMONE RECEPTORS ALPHA; THYROID HORMONE RECEPTORS BETA; TRIIODOTHYRONINE;

EID: 79951904578     PISSN: 00137227     EISSN: 00137227     Source Type: Journal    
DOI: 10.1210/en.2010-0813     Document Type: Article

References (37)

1. Cheng SY, Leonard JL, Davis PJ 2010 Molecular aspects of thyroid hormone actions. Endocr Rev 31:139-170
2. Ercan-Fang S, Schwartz HL, Oppenheimer JH 1996 Isoform-specific 3,5,3′-triiodothyronine receptor binding capacity and messenger ribonucleic acid content in rat adenohypophysis: effect of thyroidal state and comparison with extrapituitary tissues. Endocrinology 137:3228-3233 (Pubitemid 26250168)
3. Forrest D, Hanebuth E, Smeyne RJ, Everds N, Stewart CL, Wehner JM, Curran T 1996 Recessive resistance to thyroid hormone in mice lacking thyroid hormone receptor β: evidence for tissue-specific modulation of receptor function. EMBO J 15:3006-3015
4. Wallis K, Sjögren M, van Hogerlinden M, Silberberg G, Fisahn A, Nordström K, Larsson L, Westerblad H, Morreale de Escobar G, Shupliakov O, Vennström B 2008 Locomotor deficiencies and aberrant development of subtype-specific GABAergic interneurons caused by an unliganded thyroid hormone receptor α1. J Neurosci 28:1904-1915 (Pubitemid 351302678)
5. Wikström L, Johansson C, Saltó C, Barlow C, Campos Barros A, Baas F, Forrest D, Thorén P, Vennström B 1998 Abnormal heart rate and body temperature in mice lacking thyroid hormone receptor α1. EMBO J 17:455-461 (Pubitemid 28045486)
6. Barca-Mayo O, Liao XH, Alonso-Sampedro M, Di Cosmo C, Refetoff S, Weiss RE Impairment of type 3 deiodinase (D3) contributes to the hypersensitivity to thyroid hormone (TH) of TRα knock out (TRaKO) mice. 92nd Annual Meeting of The Endocrine Society, San Diego, CA, 2010, p. S2541 (Abstract OR41-3)
7. Chiamolera MI, Matsumoto S, Ortiga-Carvalho TM, Wondisford FE Fundamentally different roles for thyroid hormone receptor isoforms in thyroid hormone pituitary feedback. 92nd Annual Meeting of The Endocrine Society, San Diego, CA, 2010, p. S2542, (Abstract OR41-4)
8. Manzano J, Morte B, Scanlan TS, Bernal J 2003 Differential effects of triiodothyronine and the thyroid hormone receptor β-specific agonist GC-1 on thyroid hormone target genes in the brain. Endocrinology 144:5480-5487 (Pubitemid 37476077)
9. Gloss B, Trost S, Bluhm W, Swanson E, Clark R, Winkfein R, Janzen K, Giles W, Chassande O, Samarut J, Dillmann W2 001 Cardiac ion channel expression and contractile function in mice with deletion of thyroid hormone receptor α or β. Endocrinology 142:544-550
10. Baxter JD, Webb P, Grover G, Scanlan TS 2004 Selective activation of thyroid hormone signaling pathways by GC-1: a new approach to controlling cholesterol and body weight. Trends Endocrinol Metab 15:154-157 (Pubitemid 38510494)
11. Erion MD, Cable EE, Ito BR, Jiang H, Fujitaki JM, Finn PD, Zhang BH, Hou J, Boyer SH, van Poelje PD, Linemeyer DL 2007 Targeting thyroid hormone receptor-β agonists to the liver reduces cholesterol and triglycerides and improves the therapeutic index. Proc Natl Acad Sci USA 104:15490-15495 (Pubitemid 47502944)
12. Borngraeber S, Budny MJ, Chiellini G, Cunha-Lima ST, Togashi M, Webb P, Baxter JD, Scanlan TS, Fletterick RJ 2003 Ligand selectivity by seeking hydrophobicity in thyroid hormone receptor. Proc Natl Acad Sci USA 100:15358-15363 (Pubitemid 38020994)
13. Grover GJ, Egan DM, Sleph PG, Beehler BC, Chiellini G, Nguyen NH, Baxter JD, Scanlan TS 2004 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 145:1656-1661 (Pubitemid 38402372)
14. Grover GJ, MellströmK, Ye L, Malm J, Li YL, Bladh LG, Sleph PG, Smith MA, George R, Vennström B, Mookhtiar K, Horvath R, Speelman J, Egan D, Baxter JD 2003 Selective thyroid hormone receptor-β activation: a strategy for reduction of weight, cholesterol, and lipoprotein (a) with reduced cardiovascular liability. Proc Natl Acad Sci USA 100:10067-10072 (Pubitemid 37098262)
15. Ladenson PW, Kristensen JD, Ridgway EC, Olsson AG, Carlsson B, Klein I, Baxter JD, Angelin B 2010 Use of the thyroid hormone analogue eprotirome in statin-treated dyslipidemia. N Engl J Med 362:906-916
16. Denver RJ, Hu F, Scanlan TS, Furlow JD 2009 Thyroid hormone receptor subtype specificity for hormone-dependent neurogenesis in Xenopus laevis. Dev Biol 326:155-168
17. Morte B, Manzano J, Scanlan T, Vennström B, Bernal J 2002 Deletion of the thyroid hormone receptor α1 prevents the structural alterations of the cerebellum induced by hypothyroidism. Proc Natl Acad Sci USA 99:3985-3989 (Pubitemid 34252217)
18. Morte B, Manzano J, Scanlan TS, Vennström B, Bernal J 2004 Aberrant maturation of astrocytes in thyroid hormone receptor α1 knockout mice reveals an interplay between thyroid hormone receptor isoforms. Endocrinology 145:1386-1391 (Pubitemid 38281023)
19. Ribeiro MO 2008 Effects of thyroid hormone analogs on lipid metabolism and thermogenesis. Thyroid 18:197-203 (Pubitemid 351271536)
20. Guadaño-Ferraz A, Benavides-Piccione R, Venero C, Lancha C, Vennström B, Sandi C, DeFelipe J, Bernal J 2003 Lack of thyroid hormone receptor α1 is associated with selective alterations in behavior and hippocampal circuits. Mol Psychiatry 8:30-38 (Pubitemid 36188571)
21. Venero C, Guadaño-Ferraz A, Herrero AI, Nordström K, Manzano J, de Escobar GM, Bernal J, Vennström B 2005 Anxiety, memory impairment, and locomotor dysfunction caused by a mutant thyroid hormone receptor α1 can be ameliorated by T3 treatment. Genes Dev 19:2152-2163 (Pubitemid 41330317)
22. Di Cosmo C, Liao XH, Dumitrescu AM, Weiss RE, Refetoff S 2009 A thyroid hormone analog with reduced dependence on the monocarboxylate transporter 8 for tissue transport. Endocrinology 150:4450-4458
23. Martínez L, Nascimento AS, Nunes FM, Phillips K, Aparicio R, Dias SM, Figueira AC, Lin JH, Nguyen P, Apriletti JW, Neves FA, Baxter JD, Webb P, Skaf MS, Polikarpov I 2009 Gaining ligand selectivity in thyroid hormone receptors via entropy. Proc Natl Acad Sci USA 106:20717-20722
24. Ocasio CA, Scanlan TS 2006 Design and characterization of a thyroid hormone receptor α (TRα)-specific agonist. ACS Chem Biol 1:585-593
25. Ocasio CA, Scanlan TS 2008 Characterization of thyroid hormone receptor α (TRα)-specific analogs with varying inner- and outer-ring substituents. Bioorg Med Chem 16:762-770
26. Ceballos A, Belinchon MM, Sanchez-Mendoza E, Grijota-Martinez C, Dumitrescu AM, Refetoff S, Morte B, Bernal J 2009 Importance of monocarboxylate transporter 8 for the blood-brain barrier-dependent availability of 3,5,3′-triiodo-L-thyronine. Endocrinology 150:2491-2496
27. Zavacki AM, Ying H, Christoffolete MA, Aerts G, So E, Harney JW, Cheng SY, Larsen PR, Bianco AC 2005 Type 1 iodothyronine deiodinase is a sensitive marker of peripheral thyroid status in the mouse. Endocrinology 146:1568-1575 (Pubitemid 40289348)
28. Caubín J, Iglesias T, Bernal J, Muñoz A, Márquez G, Barbero JL, Zaballos A 1994 Isolation of genomic DNA fragments corresponding to genes modulated in vivo by a transcription factor. Nucleic Acids Res 22:4132-4138 (Pubitemid 24322715)
29. Rohrer D, Dillmann WH 1988 Thyroid hormone markedly increases the mRNA coding for sarcoplasmic reticulum Ca2+-ATPase in the rat heart. J Biol Chem 263:6941-6944
30. Lompré AM, Nadal-Ginard B, Mahdavi V 1984 Expression of the cardiac ventricular α- and β-myosin heavy chain genes is developmentally and hormonally regulated. J Biol Chem 259:6437-6446
31. Lindholm D, Castrén E, Tsoulfas P, Kolbeck R, Berzaghi Mda P, Leingärtner A, Heisenberg CP, Tessarollo L, Parada LF, Thoenen H 1993 Neurotrophin-3 induced by tri-iodothyronine in cerebellar granule cells promotes Purkinje cell differentiation. J Cell Biol 122:443-450 (Pubitemid 23210470)
32. Thompson CC 1996 Thyroid hormone-responsive genes in developing cerebellum include a novel synaptotagmin and a hairless homolog. J Neurosci 16:7832-7840 (Pubitemid 26405046)
33. Johansson C, Göthe S, Forrest D, Vennström B, Thorén P 1999 Cardiovascular phenotype and temperature control in mice lacking thyroid hormone receptor-β or both α1 and β. Am J Physiol 276:H2006-H2012 (Pubitemid 29323485)
34. Gullberg H, Rudling M, Saltó C, Forrest D, Angelin B, Vennström B 2002 Requirement for thyroid hormone receptor β in T3 regulation of cholesterol metabolism in mice. Mol Endocrinol 16:1767-1777 (Pubitemid 34828087)
35. Zandieh Doulabi B, Platvoet-ter Schiphorst M, van Beeren HC, Labruyere WT, Lamers WH, Fliers E, Bakker O, Wiersinga WM 2002 TR(β)1 protein is preferentially expressed in the pericentral zone of rat liver and exhibits marked diurnal variation. Endocrinology 143:979-984 (Pubitemid 34164046)
36. Amma LL, Campos-Barros A, Wang Z, Vennström B, Forrest D 2001 Distinct tissue-specific roles for thyroid hormone receptors β and α1 in regulation of type 1 deiodinase expression. Mol Endocrinol 15:467-475 (Pubitemid 32221922)
37. Friesema EC, Jansen J, Milici C, Visser TJ 2005 Thyroid hormone transporters. Vitam Horm 70:137-167 (Pubitemid 43589022)