More information on this family may be found on the IUPHAR-DB family and introduction pages.
Thyroid hormone receptors (TRs, nomenclature as agreed by NC-IUPHAR Committee on Nuclear Receptors, [3]) are nuclear hormone receptors of the NR1A family, with diverse roles regulating macronutrient metabolism, cognition and cardiovascular homeostasis. TRs are activated by thyroxine (T4) and thyroid hormone (T3). Once activated by a ligand, the receptor acts as a transcription factor either as a monomer, homodimer or heterodimer with members of the retinoid X receptor family.
Unless otherwise stated all data refer to the human proteins. Gene information is provided for human (Hs), mouse (Mm) and rat (Rn).
Receptors 
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Thyroid hormone receptor-α Show »« Hide
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Thyroid hormone receptor-β Show »« Hide
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Baxter, JD; Webb, P. (2009) Thyroid hormone mimetics: potential applications in atherosclerosis, obesity and type 2 diabetes. Nat Rev Drug Discov, 8 (4): 308-20. [PMID:19337272]
Bernal, J. (2007) Thyroid hormone receptors in brain development and function. Nat Clin Pract Endocrinol Metab, 3 (3): 249-59. [PMID:17315033]
Cheng, SY; Leonard, JL; Davis, PJ. (2010) Molecular aspects of thyroid hormone actions. Endocr. Rev., 31 (2): 139-70. [PMID:20051527]
Davis, PJ; Davis, FB; Mousa, SA; Luidens, MK; Lin, HY. (2011) Membrane receptor for thyroid hormone: physiologic and pharmacologic implications. Annu. Rev. Pharmacol. Toxicol., 51: 99-115. [PMID:20868274]
Davis, PJ; Zhou, M; Davis, FB; Lansing, L; Mousa, SA; Lin, HY. (2010) Mini-review: Cell surface receptor for thyroid hormone and nongenomic regulation of ion fluxes in excitable cells. Physiol. Behav., 99 (2): 237-9. [PMID:19248795]
Flamant, F; Baxter, JD; Forrest, D; Refetoff, S; Samuels, H; Scanlan, TS; Vennström, B; Samarut, J. (2006) International Union of Pharmacology. LIX. The pharmacology and classification of the nuclear receptor superfamily: thyroid hormone receptors. Pharmacol. Rev., 58 (4): 705-11. [PMID:17132849]
Furuya, F; Lu, C; Guigon, CJ; Cheng, SY. (2009) Nongenomic activation of phosphatidylinositol 3-kinase signaling by thyroid hormone receptors. Steroids, 74 (7): 628-34. [PMID:19014961]
Grover, GJ; Mellström, K; Malm, J. (2007) Therapeutic potential for thyroid hormone receptor-beta selective agonists for treating obesity, hyperlipidemia and diabetes. Curr Vasc Pharmacol, 5 (2): 141-54. [PMID:17430219]
Liu, YY; Brent, GA. (2010) Thyroid hormone crosstalk with nuclear receptor signaling in metabolic regulation. Trends Endocrinol. Metab., 21 (3): 166-73. [PMID:20015660]
Pramfalk, C; Pedrelli, M; Parini, P. (2011) Role of thyroid receptor β in lipid metabolism. Biochim. Biophys. Acta, 1812 (8): 929-37. [PMID:21194564]
Visser, WE; Friesema, EC; Jansen, J; Visser, TJ. (2008) Thyroid hormone transport in and out of cells. Trends Endocrinol. Metab., 19 (2): 50-6. [PMID:18291666]
Yen, PM; Ando, S; Feng, X; Liu, Y; Maruvada, P; Xia, X. (2006) Thyroid hormone action at the cellular, genomic and target gene levels. Mol. Cell. Endocrinol., 246 (1-2): 121-7. [PMID:16442701]
1. Bergh, JJ; Lin, HY; Lansing, L; Mohamed, SN; Davis, FB; Mousa, S; Davis, PJ. (2005) Integrin alphaVbeta3 contains a cell surface receptor site for thyroid hormone that is linked to activation of mitogen-activated protein kinase and induction of angiogenesis. Endocrinology, 146 (7): 2864-71. [PMID:15802494]
2. Chiellini, G; Apriletti, JW; Yoshihara, HA; Baxter, JD; Ribeiro, RC; Scanlan, TS. (1998) A high-affinity subtype-selective agonist ligand for the thyroid hormone receptor. Chem. Biol., 5 (6): 299-306. [PMID:9653548]
3. Flamant, F; Baxter, JD; Forrest, D; Refetoff, S; Samuels, H; Scanlan, TS; Vennström, B; Samarut, J. (2006) International Union of Pharmacology. LIX. The pharmacology and classification of the nuclear receptor superfamily: thyroid hormone receptors. Pharmacol. Rev., 58 (4): 705-11. [PMID:17132849]
4. Nguyen, NH; Apriletti, JW; Cunha Lima, ST; Webb, P; Baxter, JD; Scanlan, TS. (2002) Rational design and synthesis of a novel thyroid hormone antagonist that blocks coactivator recruitment. J. Med. Chem., 45 (15): 3310-20. [PMID:12109914]
5. Sharma, S. K., Klee, W. A. and Nirenberg, M. (1977) Opiate-dependent modulation of adenylate cyclase. Proc Natl Acad Sci U S A, 74: 3365-3369. [PMID:269396]
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An interaction with integrin αVβ3 has been suggested to underlie plasma membrane localization of TRs and non-genomic signalling [1].One splice variant, TRα2, lacks a functional DNA-binding domain and appears to act as a transcription suppressor.
Although radioligand binding assays have been described for these receptors, the radioligands are not commercially available. NH-3 has been described as an antagonist at TRs with modest selectivity for TRβ [4].