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Volumn 16, Issue 25, 2009, Pages 3258-3266

Thyroid hormone antagonists: Potential medical applications and structure activity relationships

Author keywords

Amiodarone; Design strategy; Hyperthyroidism; Structure activity relationship; Thyroid hormone antagonist; Thyroid hormone receptor; Thyrotoxicosis; X ray structure

Indexed keywords

1 (4 HEXYLPHENYL)PROPENONE; 3 (3,5 DIBROMO 4 CYCLOHEXYLMETHOXYPHENYL)PROPIONIC ACID; 3 [3,5 DIBROMO 4 (3 BROMOBENZYLOXY)PHENYL]PROPIONIC ACID; 3 DIMETHYLAMINO 1 (4 HEXYLPHENYL)PROPAN 1 ONE; [4 [1 (4 HYDROXY 3 ISOPROPYLPHENYL)BUT 2 ENYL] 3,5 DIMETHYLPHENOXY]ACETIC ACID; [4 [4 HYDROXY 3 ISOPROPYL 5 (4 NITROPHENYL)BENZYL] 3,5 DIMETHYLPHENOXY]ACETIC ACID; [4 [4 HYDROXY 3 ISOPROPYL 5 (4 NITROPHENYLETHYNYL)BENZYL] 3,5 DIMETHYLPHENOXY]ACETIC ACID; [[(BUTYL METHYLCARBAMOYL)(4 HYDROXY 3 ISOPROPYLPHENYL)UNDECYL]DIMETHYLPHENOXY]ACETIC ACID; AMIODARONE; ANTITHYROID AGENT; CARBIMAZOLE; DEETHYLAMIODARONE; DRONEDARONE; GC 14; KB 130015; LIOTHYRONINE; LIVER X RECEPTOR; N BUTYL 11 (3,17BETA DIHYDROXYESTRA 1,3,5(10) TRIEN 7ALPHA YL) N METHYLUNDECANAMIDE; NH 3; O (4 HYDROXY 3,5 DIISOPROPYLPHENYL)TYROSINE; PERCHLORATE; PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR; PROPYLTHIOURACIL; RADIOACTIVE IODINE; RALOXIFENE; RETINOID X RECEPTOR; THIAMAZOLE; THYROID HORMONE ANTAGONIST; THYROID HORMONE DERIVATIVE; THYROID HORMONE RECEPTOR; THYROXINE; UNCLASSIFIED DRUG; UNINDEXED DRUG;

EID: 70349609525     PISSN: 09298673     EISSN: None     Source Type: Journal    
DOI: 10.2174/092986709788803277     Document Type: Review
Times cited : (21)

References (80)
  • 1
    • 0023913120 scopus 로고
    • The steroid and thyroid hormone receptor superfamily
    • Evans, R.M. The steroid and thyroid hormone receptor superfamily. Science, 1988, 240, 889-895.
    • (1988) Science , vol.240 , pp. 889-895
    • Evans, R.M.1
  • 3
    • 0028927035 scopus 로고
    • The nuclear hormone receptor gene superfamily
    • Ribeiro, R.C.; Kushner, P.J.; Baxter, J.D. The nuclear hormone receptor gene superfamily. Ann. Rev. Med., 1995, 46, 443-453.
    • (1995) Ann. Rev. Med. , vol.46 , pp. 443-453
    • Ribeiro, R.C.1    Kushner, P.J.2    Baxter, J.D.3
  • 4
    • 0027416347 scopus 로고
    • Thyroid hormone receptors: Multiple forms, multiple possibilities
    • DOI 10.1210/er.14.2.184
    • Lazar, M.A. Thyroid hormone receptors: multiple forms, multiple possibilities. Endocr. Rev., 1993, 14, 184-193. (Pubitemid 23118416)
    • (1993) Endocrine Reviews , vol.14 , Issue.2 , pp. 184-193
    • Lazar, M.A.1
  • 5
    • 0034964207 scopus 로고    scopus 로고
    • Physiological and molecular basis of thyroid hormone action
    • Yen, P.M. Physiological and molecular basis of thyroid hormone action. Phys. Rev., 2001, 81, 1097-1142.
    • (2001) Phys. Rev. , vol.81 , pp. 1097-1142
    • Yen, P.M.1
  • 6
    • 33751309187 scopus 로고    scopus 로고
    • Diagnosis of Thyrotoxicosis
    • Braverman LE, Utiger RD, Eds. 9th ed. Philadelphia: JB Lippincott Co.
    • Ladenson, P.W. In Diagnosis of Thyrotoxicosis. Braverman LE, Utiger RD, Eds. The Thyroid. 9th ed. Philadelphia: JB Lippincott Co., 2005, pp. 659-665.
    • (2005) The Thyroid , pp. 659-665
    • Ladenson, P.W.1
  • 8
    • 0033950142 scopus 로고    scopus 로고
    • Functions of thyroid hormone receptors in mice
    • Forrest, D.; Vennström, B. Functions of thyroid hormone receptors in mice. Thyroid, 2000, 10, 41-52. (Pubitemid 30090364)
    • (2000) Thyroid , vol.10 , Issue.1 , pp. 41-52
    • Forrest, D.1    Vennstrom, B.2
  • 9
    • 0026511358 scopus 로고
    • Recessive inheritance of thyroid hormone resistance caused by complete deletion of the protein-coding region of the thyroid hormone receptor-beta gene
    • Takeda, K.; Sakurai, A.; DeGroot, L.J.; Refetoff, S.J. Recessive inheritance of thyroid hormone resistance caused by complete deletion of the protein-coding region of the thyroid hormone receptor-beta gene. Clin. Endocrinol. Metab., 1992, 74, 49-55.
    • (1992) Clin. Endocrinol. Metab. , vol.74 , pp. 49-55
    • Takeda, K.1    Sakurai, A.2    Degroot, L.J.3    Refetoff, S.J.4
  • 11
    • 0034306499 scopus 로고    scopus 로고
    • Nuclear receptor ligand-binding domains: Three-dimensional structures, molecular interactions and pharmacological implications
    • DOI 10.1016/S0165-6147(00)01548-0, PII S0165614700015480
    • Bourguet, W.; Germain, P.; Gronemeyer, H. Nuclear receptor ligand-binding domains: three-dimensional structures, molecular interactions and pharmacological implications. Trends Pharmacol. Sci., 2000, 21, 381-388. (Pubitemid 30767867)
    • (2000) Trends in Pharmacological Sciences , vol.21 , Issue.10 , pp. 381-388
    • Bourguet, W.1    Germain, P.2    Gronemeyer, H.3
  • 12
    • 0029643769 scopus 로고
    • A structural role for hormone in the thyroid hormone receptor
    • DOI 10.1038/378690a0
    • Wagner, R.L.; Apriletti, J.W.; McGrath, M.E.; West, B.L.; Baxter, J.D.; Fletterick, R.J. A structural role for hormone in the thyroid hormone receptor. Nature, 1995, 378, 690-697. (Pubitemid 3009997)
    • (1995) Nature , vol.378 , Issue.6558 , pp. 690-697
    • Wagner, R.L.1    Apriletti, J.W.2    McGrath, M.E.3    West, B.L.4    Baxter, J.D.5    Fletterick, R.J.6
  • 21
    • 0029012163 scopus 로고
    • Crystal structure of the ligand-binding domain of the human nuclear receptor RXR-alpha
    • Bourguet, W.; Ruff, M.; Chambon, P.; Gronemeyer, H.; Moras, D. Crystal structure of the ligand-binding domain of the human nuclear receptor RXR-alpha. Nature, 1995, 375, 377-382.
    • (1995) Nature , vol.375 , pp. 377-382
    • Bourguet, W.1    Ruff, M.2    Chambon, P.3    Gronemeyer, H.4    Moras, D.5
  • 24
    • 0142223221 scopus 로고    scopus 로고
    • The three-dimensional structure of the liver X receptor beta reveals a flexible ligand-binding pocket that can accommodate fundamentally different ligands
    • DOI 10.1074/jbc.M304842200
    • Färnegårdh, M.; Bonn, T.; Sun, S.; Ljunggren, J.; Ahola, H.; Wilhelmsson, A.; Gustafsson, J.A.; Carlquist, M. The three-dimensional structure of the liver X receptor beta reveals a flexible ligand-binding pocket that can accommodate fundamentally different ligands. J. Biol. Chem., 2003, 40, 38821-38828. (Pubitemid 37229066)
    • (2003) Journal of Biological Chemistry , vol.278 , Issue.40 , pp. 38821-38828
    • Farnegardh, M.1    Bonn, T.2    Sun, S.3    Ljunggren, J.4    Ahola, H.5    Wilhelmsson, A.6    Gustafsson, J.-A.7    Carlquist, M.8
  • 26
    • 24144439756 scopus 로고    scopus 로고
    • Molecular dynamics simulations reveal multiple pathways of ligand dissociation from thyroid hormone receptors
    • DOI 10.1529/biophysj.105.063818
    • Martínez, L.; Sonoda, M.T.; Webb, P.; Baxter, J.D.; Skaf, M.S.; Polikarpovz, I. Molecular dynamics simulations reveal multiple pathways of ligand dissociation from thyroid hormone receptors. Biophys. J., 2005, 89, 2011-2023. (Pubitemid 41233556)
    • (2005) Biophysical Journal , vol.89 , Issue.3 , pp. 2011-2023
    • Martinez, L.1    Sonoda, M.T.2    Webb, P.3    Baxter, J.D.4    Skaf, M.S.5    Polikarpov, I.6
  • 27
    • 18044365802 scopus 로고    scopus 로고
    • Conformational adaptation of nuclear receptor ligand binding domains to agonists: Potential for novel approaches to ligand design
    • Togashi, M.; Borngraeber, S.; Sandler, B.; Fletterick, R.J.; Webb, P.; Baxter, J.D. Conformational adaptation of nuclear receptor ligand binding domains to agonists: potential for novel approaches to ligand design. J. Steroid Biochem. Mol. Biol., 2005, 93, 127-137.
    • (2005) J. Steroid Biochem. Mol. Biol. , vol.93 , pp. 127-137
    • Togashi, M.1    Borngraeber, S.2    Sandler, B.3    Fletterick, R.J.4    Webb, P.5    Baxter, J.D.6
  • 28
    • 51849109110 scopus 로고    scopus 로고
    • Only subtle protein conformational adaptations are required for ligand binding to thyroid hormone receptors: Simulations using a novel multipoint steered molecular dynamics approach
    • Martínez, L.; Polikarpov, I.; Skaf, M.S. Only subtle protein conformational adaptations are required for ligand binding to thyroid hormone receptors: simulations using a novel multipoint steered molecular dynamics approach. J. Phys. Chem. B., 2008, 112, 10741-10751.
    • (2008) J. Phys. Chem. B , vol.112 , pp. 10741-10751
    • Martínez, L.1    Polikarpov, I.2    Skaf, M.S.3
  • 29
    • 14544296973 scopus 로고    scopus 로고
    • Antithyroid drugs
    • Cooper, D.S. Antithyroid drugs N. Engl. J. Med., 2005, 352, 905-917.
    • (2005) N. Engl. J. Med. , vol.352 , pp. 905-917
    • Cooper, D.S.1
  • 30
  • 31
    • 0028775261 scopus 로고
    • The management of hyperthyroidism
    • Franklyn, J.A. The management of hyperthyroidism. N. Engl. J. Med., 1994, 330, 1731-1738.
    • (1994) N. Engl. J. Med. , vol.330 , pp. 1731-1738
    • Franklyn, J.A.1
  • 35
    • 0024578703 scopus 로고
    • A proton and fluorine-19 nuclear magnetic resonance and fluorescence study of the binding of some natural and synthetic thyromimetics to prealbumin (transthyretin)
    • Reid, D.G.; Maclachlan, L.K.; Voyle, M.; Leeson, P.D. A proton and fluorine-19 nuclear magnetic resonance and fluorescence study of the binding of some natural and synthetic thyromimetics to prealbumin (transthyretin). J. Biol. Chem., 1989, 264, 2013-2023.
    • (1989) J. Biol. Chem. , vol.264 , pp. 2013-2023
    • Reid, D.G.1    Maclachlan, L.K.2    Voyle, M.3    Leeson, P.D.4
  • 36
    • 0024273897 scopus 로고
    • Thyroid hormone analog inhibition of hepatic 5'-iodothyronine deiodinase activity
    • Shulkin, B.L.; Bolger, M.B.; Utiger, R.D. Thyroid hormone analog inhibition of hepatic 5'-iodothyronine deiodinase activity. J. Endocrinol. Invest., 1988, 11, 657-661.
    • (1988) J. Endocrinol. Invest. , vol.11 , pp. 657-661
    • Shulkin, B.L.1    Bolger, M.B.2    Utiger, R.D.3
  • 37
    • 0022967239 scopus 로고
    • Rat liver iodothyronine monodeiodinase. Evaluation of the iodothyronine ligand-binding site
    • Koehrle, J.; Auf'mkolk, M.; Rokos, H.; Hesch, R.D.; Cody, V. Rat liver iodothyronine monodeiodinase. Evaluation of the iodothyronine ligand-binding site. J. Biol. Chem., 1986, 261, 11613-11622.
    • (1986) J. Biol. Chem. , vol.261 , pp. 11613-11622
    • Koehrle, J.1    Auf'mkolk, M.2    Rokos, H.3    Hesch, R.D.4    Cody, V.5
  • 38
    • 0021404848 scopus 로고
    • Configuration and properties of a binding site for thyroid hormones on a specific receptor
    • Tropsha, A.E.; Rakhmaninova, A.B.; Iaguzhinskii, L.S. Configuration and properties of a binding site for thyroid hormones on a specific receptor Bioorg. Khim., 1984, 10, 483-492.
    • (1984) Bioorg. Khim. , vol.10 , pp. 483-492
    • Tropsha, A.E.1    Rakhmaninova, A.B.2    Iaguzhinskii, L.S.3
  • 39
    • 0019134825 scopus 로고
    • Molecular interactions between thyroid hormone analogs and the rat liver nuclear receptor. Partitioning of equilibrium binding free energy changes into substituent group interactions
    • Bolger, M.B.; Jorgensen, E.C. Molecular interactions between thyroid hormone analogs and the rat liver nuclear receptor. Partitioning of equilibrium binding free energy changes into substituent group interactions. J. Biol. Chem., 1980, 255, 10271-10278.
    • (1980) J. Biol. Chem. , vol.255 , pp. 10271-10278
    • Bolger, M.B.1    Jorgensen, E.C.2
  • 40
    • 0017644831 scopus 로고
    • Thyroxine analogues. 23. Quantitative structure-activity correlation studies of in vivo and in vitro thyromimetic activities
    • Dietrich, S.W.; Bolger, M.B.; Kollman, P.A.; Jorgensen, E.C. Thyroxine analogues. 23. Quantitative structure-activity correlation studies of in vivo and in vitro thyromimetic activities. J. Med. Chem., 1977, 20, 863-880.
    • (1977) J. Med. Chem. , vol.20 , pp. 863-880
    • Dietrich, S.W.1    Bolger, M.B.2    Kollman, P.A.3    Jorgensen, E.C.4
  • 41
    • 0016753057 scopus 로고
    • Binding of selected iodothyronine analogues to receptor sites of isolated rat hepatic nuclei. High correlation between structural requirements for nuclear binding and biological activity
    • Koerner, D.; Schwartz. H.L.; Surks, M.L.; Oppenheimer, J.H. Binding of selected iodothyronine analogues to receptor sites of isolated rat hepatic nuclei. High correlation between structural requirements for nuclear binding and biological activity. J. Biol. Chem., 1975, 250, 6417-6423.
    • (1975) J. Biol. Chem. , vol.250 , pp. 6417-6423
    • Koerner, D.1    Schwartz, H.L.2    Surks, M.L.3    Oppenheimer, J.H.4
  • 44
    • 0036132531 scopus 로고    scopus 로고
    • Synthesis and biological activity of novel thyroid hormone analogues: 5′-aryl substituted GC-1 derivatives
    • Chiellini, G.; Nguyen, N. H.; Apriletti, J.W.; Baxter, J.D.; Scanlan, T.S. Synthesis and biological activity of novel thyroid hormone analogues: 5′-aryl substituted GC-1 derivatives. Bioorg. Med. Chem. Lett., 2002, 10, 333-346.
    • (2002) Bioorg. Med. Chem. Lett. , vol.10 , pp. 333-346
    • Chiellini, G.1    Nguyen, N.H.2    Apriletti, J.W.3    Baxter, J.D.4    Scanlan, T.S.5
  • 45
    • 0037130243 scopus 로고    scopus 로고
    • Rational design and synthesis of a novel thyroid hormone antagonist that blocks coactivator recruitment
    • Nguyen, N.H.; Apriletti, J.W.; Lima, S.T.C.; Webb, P.; Baxter, J.D.; Scanlan, T.S. Rational design and synthesis of a novel thyroid hormone antagonist that blocks coactivator recruitment. J. Med. Chem., 2002, 45, 3310-3320.
    • (2002) J. Med. Chem. , vol.45 , pp. 3310-3320
    • Nguyen, N.H.1    Apriletti, J.W.2    Lima, S.T.C.3    Webb, P.4    Baxter, J.D.5    Scanlan, T.S.6
  • 46
    • 0037144443 scopus 로고    scopus 로고
    • A thyroid hormone antagonist that inhibits thyroid hormone action in vivo
    • DOI 10.1074/jbc.M205608200
    • Lim, W.; Nguyen, N.H.; Yang, H.Y.; Scanlan, T.S.; Furlow, J.D. A thyroid hormone antagonist that inhibits thyroid hormone action in vivo. J. Biol. Chem., 2002, 277, 35664-35670. (Pubitemid 35052476)
    • (2002) Journal of Biological Chemistry , vol.277 , Issue.38 , pp. 35664-35670
    • Lim, W.1    Nguyen, N.-H.2    Yang, H.Y.3    Scanlan, T.S.4    David Furlow, J.5
  • 50
    • 70450136929 scopus 로고    scopus 로고
    • note
    • While this type of antagonism has been referred to as "passive", we prefer the term "indirect" to avoid confusion with active vs. competitive or "passive" antagonism that has been used to describe antagonism of e.g. the glucocorticoid (GR) receptor. The rationale for making this distinction has been outlined in reference [54].
  • 52
    • 0034121290 scopus 로고    scopus 로고
    • Androgen receptor antagonists (antiandrogens): Structure-activity relationships
    • Singh, S.M.; Gauthier, S.; Labrie, F. Androgen receptor antagonists (antiandrogens): structure-activity relationships. Curr. Med. Chem., 2000, 7, 211-247. (Pubitemid 30396447)
    • (2000) Current Medicinal Chemistry , vol.7 , Issue.2 , pp. 211-247
    • Singh, S.M.1    Gauthier, S.2    Labrie, F.3
  • 53
    • 0028892751 scopus 로고
    • The mineralocorticoid activity of progesterone derivatives depends on the nature of the C18 substituent
    • Souque, A.; Fagart, J.; Couette, B.; Davioud, E.; Sobrio, F.; Marquet A.; Rafestin-Oblin, M.E. The mineralocorticoid activity of progesterone derivatives depends on the nature of the C18 substituent. Endocrinology, 1995, 136, 5651-5658.
    • (1995) Endocrinology , vol.136 , pp. 5651-5658
    • Souque, A.1    Fagart, J.2    Couette, B.3    Davioud, E.4    Sobrio, F.5    Marquet, A.6    Rafestin-Oblin, M.E.7
  • 54
    • 18244365116 scopus 로고    scopus 로고
    • Thyroid receptor ligands. 3. Design and synthesis of 3,5-dihalo-4- Alkoxyphenylalkanoic acids as indirect antagonists of the thyroid hormone receptor
    • DOI 10.1021/jm050004k
    • Hedfors, Å.; Appelqvist, T.; Carlsson, B.; Bladh, L.-B.; Litten, C.; Agback, P.; Grynfarb, M.; Koehler, K.F.; Malm, J. Thyroid receptor ligands. 3. Design and synthesis of 3,5-dihalo-4-alkoxyphenylalkanoic acids as indirect antagonists of the thyroid hormone receptor. J. Med. Chem., 2005, 48, 3114-3117. (Pubitemid 40628029)
    • (2005) Journal of Medicinal Chemistry , vol.48 , Issue.9 , pp. 3114-3117
    • Hedfors, A.1    Appelqvist, T.2    Carlsson, B.3    Bladh, L.-G.4    Litten, C.5    Agback, P.6    Grynfarb, M.7    Koehler, K.F.8    Malm, J.9
  • 55
    • 33847777160 scopus 로고    scopus 로고
    • Thyroid receptor ligands. Part 7: Indirect antagonists of the thyroid hormone receptor with improved affinity
    • DOI 10.1016/j.bmcl.2007.01.009, PII S0960894X07000455
    • Malm, J.; Gordon, S.; Brandt, P.; Carlsson, B.; Agback, P.; Bäckbro Saeidi, A.; Sandberg, J. Thyroid receptor ligands. Part 7: Indirect antagonists of the thyroid hormone receptor with improved affinity. Bioorg. Med. Chem. Lett., 2007, 17, 2018-2021. (Pubitemid 46389581)
    • (2007) Bioorganic and Medicinal Chemistry Letters , vol.17 , Issue.7 , pp. 2018-2021
    • Malm, J.1    Gordon, S.2    Brandt, P.3    Carlsson, B.4    Agback, P.5    Backbro Saeidi, A.6    Sandberg, J.7
  • 56
    • 0014829352 scopus 로고
    • The effect of amiodarone, a new anti-anginal drug, on cardiac muscle
    • Singh, B.N.; Vaughan Williams, E.M. The effect of amiodarone, a new anti-anginal drug, on cardiac muscle. Br. J. Pharmacol., 1970, 39, 657-667.
    • (1970) Br. J. Pharmacol. , vol.39 , pp. 657-667
    • Singh, B.N.1    Vaughan Williams, E.M.2
  • 57
    • 0008336594 scopus 로고
    • Interaction of amiodarone and desethylamiodarone with solubilized nuclear thyroid hormone receptors
    • Latham, K.R.; Selitti, D.F.; Goldstein, R.E. Interaction of amiodarone and desethylamiodarone with solubilized nuclear thyroid hormone receptors. J. Am. Coll. Cardiol., 1987, 7, 472-476.
    • (1987) J. Am. Coll. Cardiol. , vol.7 , pp. 472-476
    • Latham, K.R.1    Selitti, D.F.2    Goldstein, R.E.3
  • 58
    • 0024552154 scopus 로고
    • Antagonism of thyroid hormone action by amiodarone in rat pituitary tumor cells
    • Norman, M.F.; Lavin, T.A. Competition of thyroid hormone action by amiodarone in rat pituitary tumor cells. J. Clin. Invest., 1989, 83, 306-313. (Pubitemid 19048437)
    • (1989) Journal of Clinical Investigation , vol.83 , Issue.1 , pp. 306-313
    • Norman, M.F.1    Lavin, T.N.2
  • 59
    • 0032893049 scopus 로고    scopus 로고
    • Electrophysiologic effects of chronic amiodarone therapy and hypothyroidism, alone and in combination, on guinea pig ventricular myocytes
    • Bosch, R.F.; Li, G-R.; Gaspo, R.; Nattel, S. Electrophysiologic effects of chronic amiodarone therapy and hypothyroidism, alone and in combination, on guinea pig ventricular myocytes. J. Pharmacol. Exp. Ther., 1999, 289,156-165. (Pubitemid 29156024)
    • (1999) Journal of Pharmacology and Experimental Therapeutics , vol.289 , Issue.1 , pp. 156-165
    • Bosch, R.F.1    Li, G.-R.2    Gaspo, R.3    Nattel, S.4
  • 60
    • 0029801247 scopus 로고    scopus 로고
    • Antiarrhythmic actions of amiodarone: A profile of a paradoxical agent
    • Singh, B.N. Antiarrhythmic actions of amiodarone: A profile of a paradoxical agent. Am. J. Cardiol., 1996, 78, 41-53.
    • (1996) Am. J. Cardiol. , vol.78 , pp. 41-53
    • Singh, B.N.1
  • 61
    • 0030773253 scopus 로고    scopus 로고
    • Cellular electropharmacology of amiodarone
    • Kodama, I.; Kamiya, K.; Toyama, J. Cellular electropharmacology of amiodarone. Cardiovasc. Res., 1997, 35, 13-29.
    • (1997) Cardiovasc. Res. , vol.35 , pp. 13-29
    • Kodama, I.1    Kamiya, K.2    Toyama, J.3
  • 62
    • 0029100396 scopus 로고
    • Amiodarone is a dose-dependent noncompetitive and competitive inhibitor of T3 binding to thyroid hormone receptor subtype beta 1, whereas disopyramide, lignocaine, propafenone, metoprolol, dl-sotalol, and verapamil have no inhibitory effect
    • Drvota, V.; Carlsson, B.; Häggblad, J.; Sylven, C. Amiodarone is a dose-dependent noncompetitive and competitive inhibitor of T3 binding to thyroid hormone receptor subtype beta 1, whereas disopyramide, lignocaine, propafenone, metoprolol, dl-sotalol, and verapamil have no inhibitory effect. J. Cardiovasc. Pharmacol., 1995, 26, 222-226.
    • (1995) J. Cardiovasc. Pharmacol. , vol.26 , pp. 222-226
    • Drvota, V.1    Carlsson, B.2    Häggblad, J.3    Sylven, C.4
  • 63
    • 0029047556 scopus 로고
    • Desethylamiodarone is a competitive inhibitor of the binding of thyroid hormone to the thyroid hormone alpha 1-receptor protein
    • van Beeren, H.C.; Bakker, O.; Wiersinga, W.M. Desethylamiodarone is a competitive inhibitor of the binding of thyroid hormone to the thyroid hormone alpha 1-receptor protein. Mol. Cell. Endocrinol., 1995, 112, 15-19.
    • (1995) Mol. Cell. Endocrinol. , vol.112 , pp. 15-19
    • Van Beeren, H.C.1    Bakker, O.2    Wiersinga, W.M.3
  • 64
    • 0028180732 scopus 로고
    • 1-receptor protein
    • DOI 10.1210/en.134.4.1665
    • Bakker, O.; van Beeren, H.C.; Wiersinga, W.M. Desethylamiodarone is a noncompetitive inhibitor of the binding of thyroid hormone to the thyroid hormone beta 1-receptor protein. Endocrinology, 1994, 134, 1665-1670. (Pubitemid 24110721)
    • (1994) Endocrinology , vol.134 , Issue.4 , pp. 1665-1670
    • Bakker, O.1    Van Beeren, H.C.2    Wiersinga, W.M.3
  • 65
    • 0037320339 scopus 로고    scopus 로고
    • Dronerarone acts as a selective inhibitor of 3,5,3′- triiodothyronine binding to thyroid hormone receptor-alpha1: In vitro and in vivo evidence
    • van Beeren, H.C.; Jong, W.M.; Kaptein, E.; Visser, T.J.; Bakker, O.; Wiersinga, W.M. Dronerarone acts as a selective inhibitor of 3,5,3′-triiodothyronine binding to thyroid hormone receptor-alpha1: in vitro and in vivo evidence. Endocrinology, 2003, 144, 552-558.
    • (2003) Endocrinology , vol.144 , pp. 552-558
    • Van Beeren, H.C.1    Jong, W.M.2    Kaptein, E.3    Visser, T.J.4    Bakker, O.5    Wiersinga, W.M.6
  • 66
    • 0037203995 scopus 로고    scopus 로고
    • Synthesis and preliminary characterization of a novel antiarrhythmic compound (KB130015) with an improved toxicity profile compared with amiodarone
    • Carlsson, B.; Singh, B.N.; Temciuc, M.; Nilsson, S.; Li, Y.L.; Mellin, C.; Malm, J. Synthesis and preliminary characterization of a novel antiarrhythmic compound (KB130015) with an improved toxicity profile compared with amiodarone. J. Med. Chem., 2002, 45, 623-630.
    • (2002) J. Med. Chem. , vol.45 , pp. 623-630
    • Carlsson, B.1    Singh, B.N.2    Temciuc, M.3    Nilsson, S.4    Li, Y.L.5    Mellin, C.6    Malm, J.7
  • 67
    • 0029953792 scopus 로고    scopus 로고
    • 1-Thyroid Hormone Receptor by Amiodarone Analogs
    • van Beeren, H.C.; Bakker, O.; Wiersinga, W.M. Structure-function relationship of the inhibition of the 3,5,3′-triiodothyronine binding to the alpha1- and beta1-thyroid hormone receptor by amiodarone analogs. Endocrinology, 1996, 137, 2807-2814. (Pubitemid 126425496)
    • (1996) Endocrinology , vol.137 , Issue.7 , pp. 2807-2814
    • Van Beeren, H.C.1    Barker, O.2    Wiersinga, W.M.3
  • 69
    • 0034038927 scopus 로고    scopus 로고
    • Structure effect relationships of amiodarone analogues on the inhibition of thyroxine deiodination
    • Ha, H.R.; Stieger, B.; Grassi, G.; Altorfer, H.R.; Follath, F. Structure-effect relationships of amiodarone analogues on the inhibition of thyroxine deiodination. Eur. J. Clin. Pharmacol., 2000, 55, 807-814. (Pubitemid 30201762)
    • (2000) European Journal of Clinical Pharmacology , vol.55 , Issue.11-12 , pp. 807-814
    • Ha, H.R.1    Stieger, B.2    Grassi, G.3    Altorfer, H.R.4    Follath, F.5
  • 70
    • 0024995158 scopus 로고
    • Thyroxine, 3,5,3'-triiodothyronine, and 3,3',5-triiodothyronine concentrations in several tissues of the rat: Effects of amiodarone and desethylamiodarone on thyroid hormone metabolism
    • Schröder-van der Elst, J.P.; van der Heide, D. Thyroxine, 3,5,3′-triiodothyronine, and 3,3′,5′-triiodothyronine concentrations in several tissues of the rat: effects of amiodarone and desethylamiodarone on thyroid hormone metabolism. Endocrinology, 1990, 127, 1656-1664. (Erratum in Endocrinology, 1991, 128, 393) (Pubitemid 20315223)
    • (1990) Endocrinology , vol.127 , Issue.4 , pp. 1656-1664
    • Schroder-Van Der Elst, J.P.1    Van Der Heide, D.2
  • 71
    • 0024552154 scopus 로고
    • Antagonism of thyroid hormone action by amiodarone in rat pituitary tumor cells
    • Norman, M.F.; Lavin, T.N. Antagonism of thyroid hormone action by amiodarone in rat pituitary tumor cells. J. Clin. Invest., 1989, 83, 306-313. (Pubitemid 19048437)
    • (1989) Journal of Clinical Investigation , vol.83 , Issue.1 , pp. 306-313
    • Norman, M.F.1    Lavin, T.N.2
  • 75
    • 0035925134 scopus 로고    scopus 로고
    • An inhibitor of the interaction of thyroid hormone receptor beta and glucocorticoid interacting protein 1
    • Geistlinger, T.R.; Guy, R.K. An inhibitor of the interaction of thyroid hormone receptor beta and glucocorticoid interacting protein 1. J. Am. Chem. Soc., 2001, 123, 1525-1526.
    • (2001) J. Am. Chem. Soc. , vol.123 , pp. 1525-1526
    • Geistlinger, T.R.1    Guy, R.K.2
  • 76
    • 0037939789 scopus 로고    scopus 로고
    • Novel selective inhibitors of the interaction of individual nuclear hormone receptors with a mutually shared steroid receptor coactivator 2
    • Geistlinger, T.R.; Guy, R.K. Novel selective inhibitors of the interaction of individual nuclear hormone receptors with a mutually shared steroid receptor coactivator 2. J. Am. Chem. Soc., 2003, 125, 6852-6853.
    • (2003) J. Am. Chem. Soc. , vol.125 , pp. 6852-6853
    • Geistlinger, T.R.1    Guy, R.K.2
  • 79
    • 35848969820 scopus 로고    scopus 로고
    • Inhibitors of the interaction of a thyroid hormone receptor and coactivators: Preliminary structure-activity relationships
    • DOI 10.1021/jm070556y
    • Arnold, L.A.; Kosinski, A.; Estébanez-Perpiñá, E.; Fletterick, R.J.; Guy, R.K. Inhibitors of the interaction of a thyroid hormone receptor and coactivators: preliminary structure-activity relationships. J. Med. Chem., 2007, 50, 5269-5280. (Pubitemid 350057839)
    • (2007) Journal of Medicinal Chemistry , vol.50 , Issue.22 , pp. 5269-5280
    • Arnold, L.A.1    Kosinski, A.2    Estebanez-Perpina, E.3    Fletterick, R.J.4    Guy, R.K.5


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