Thyroid hormone receptor alpha

Thyroid hormone receptor, alpha

PDB rendering based on 1nav.

Available structures

Ortholog search: PDBe, RCSB

List of PDB id codes
1NAV, 2H77, 2H79, 3HZF, 3ILZ, 3JZB, 4LNW, 4LNX

Identifiers

Symbols

THRA ; AR7; CHNG6; EAR7; ERB-T-1; ERBA; ERBA1; NR1A1; THRA1; THRA2; c-ERBA-1

External IDs

OMIM: 190120 MGI: 98742 HomoloGene: 37747 IUPHAR: 588 ChEMBL: 1860 GeneCards: THRA Gene

Gene ontology
Molecular function	• steroid receptor RNA activator RNA binding • transcription factor activity, sequence-specific DNA binding • transcription factor activity, RNA polymerase II distal enhancer sequence-specific binding • steroid hormone receptor activity • thyroid hormone receptor activity • protein binding • transcription factor binding • zinc ion binding • TBP-class protein binding • protein domain specific binding • chromatin DNA binding • protein complex binding • protein homodimerization activity • sequence-specific DNA binding • transcription regulatory region DNA binding • intronic transcription regulatory region DNA binding • protein heterodimerization activity • thyroid hormone binding
Cellular component	• nucleus • nucleoplasm • mitochondrion • cytosol
Biological process	• cartilage condensation • ossification • kidney development • liver development • regulation of thyroid hormone mediated signaling pathway • regulation of transcription from RNA polymerase II promoter • transcription from RNA polymerase II promoter • transcription initiation from RNA polymerase II promoter • brain development • learning or memory • regulation of heart contraction • female courtship behavior • response to cold • hormone-mediated signaling pathway • gene expression • positive regulation of myotube differentiation • negative regulation of RNA polymerase II transcriptional preinitiation complex assembly • erythrocyte differentiation • adrenal gland development • intracellular receptor signaling pathway • thyroid gland development • response to nutrient levels • regulation of myeloid cell apoptotic process • response to drug • cytoplasmic sequestering of transcription factor • steroid hormone mediated signaling pathway • negative regulation of sequence-specific DNA binding transcription factor activity • negative regulation of transcription, DNA-templated • positive regulation of female receptivity • positive regulation of transcription from RNA polymerase II promoter • digestive tract development • embryonic organ development • regulation of lipid catabolic process • Type I pneumocyte differentiation • negative regulation of DNA-templated transcription, initiation
Sources: Amigo / QuickGO

RNA expression pattern

More reference expression data

Orthologs

Species

Human

Mouse

RefSeq (mRNA)

RefSeq (protein)

Location (UCSC)

Chr 17:
40.06 – 40.09 Mb

Chr 11:
98.74 – 98.77 Mb

PubMed search

Thyroid hormone receptor alpha (TR-alpha) also known as nuclear receptor subfamily 1, group A, member 1 (NR1A1), is a nuclear receptor protein that in humans is encoded by the THRA gene.^[1]^[2]^[3]

Function

The protein encoded by this gene is a nuclear hormone receptor for triiodothyronine. It is one of the several receptors for thyroid hormone, and has been shown to mediate the biological activities of thyroid hormone. Knockout studies in mice suggest that the different receptors, while having certain extent of redundancy, may mediate different functions of thyroid hormone. Alternatively spliced transcript variants encoding distinct isoforms have been reported.^[1]

Interactions

THR1 has been shown to interact with:

References

1 2 "Entrez Gene: THRA thyroid hormone receptor, alpha (erythroblastic leukemia viral (v-erb-a) oncogene homolog, avian)".
↑ Spurr NK, Solomon E, Jansson M, Sheer D, Goodfellow PN, Bodmer WF, Vennstrom B (Jan 1984). "Chromosomal localisation of the human homologues to the oncogenes erbA and B". The EMBO Journal 3 (1): 159–63. PMC 557313. PMID 6323162.
↑ Dayton AI, Selden JR, Laws G, Dorney DJ, Finan J, Tripputi P, Emanuel BS, Rovera G, Nowell PC, Croce CM (Jul 1984). "A human c-erbA oncogene homologue is closely proximal to the chromosome 17 breakpoint in acute promyelocytic leukemia". Proceedings of the National Academy of Sciences of the United States of America 81 (14): 4495–9. doi:10.1073/pnas.81.14.4495. PMC 345617. PMID 6589608.
↑ Dressel U, Thormeyer D, Altincicek B, Paululat A, Eggert M, Schneider S, Tenbaum SP, Renkawitz R, Baniahmad A (May 1999). "Alien, a highly conserved protein with characteristics of a corepressor for members of the nuclear hormone receptor superfamily". Molecular and Cellular Biology 19 (5): 3383–94. doi:10.1128/mcb.19.5.3383. PMC 84131. PMID 10207062.
1 2 De Luca A, Severino A, De Paolis P, Cottone G, De Luca L, De Falco M, Porcellini A, Volpe M, Condorelli G (Feb 2003). "p300/cAMP-response-element-binding-protein ('CREB')-binding protein (CBP) modulates co-operation between myocyte enhancer factor 2A (MEF2A) and thyroid hormone receptor-retinoid X receptor". The Biochemical Journal 369 (Pt 3): 477–84. doi:10.1042/BJ20020057. PMC 1223100. PMID 12371907.
↑ Li D, Wang F, Samuels HH (Dec 2001). "Domain structure of the NRIF3 family of coregulators suggests potential dual roles in transcriptional regulation". Molecular and Cellular Biology 21 (24): 8371–84. doi:10.1128/MCB.21.24.8371-8384.2001. PMC 100002. PMID 11713274.
↑ Li D, Desai-Yajnik V, Lo E, Schapira M, Abagyan R, Samuels HH (Oct 1999). "NRIF3 is a novel coactivator mediating functional specificity of nuclear hormone receptors". Molecular and Cellular Biology 19 (10): 7191–202. doi:10.1128/mcb.19.10.7191. PMC 84712. PMID 10490654.
↑ Yuan CX, Ito M, Fondell JD, Fu ZY, Roeder RG (Jul 1998). "The TRAP220 component of a thyroid hormone receptor- associated protein (TRAP) coactivator complex interacts directly with nuclear receptors in a ligand-dependent fashion". Proceedings of the National Academy of Sciences of the United States of America 95 (14): 7939–44. doi:10.1073/pnas.95.14.7939. PMC 20908. PMID 9653119.
1 2 3 Ito M, Yuan CX, Malik S, Gu W, Fondell JD, Yamamura S, Fu ZY, Zhang X, Qin J, Roeder RG (Mar 1999). "Identity between TRAP and SMCC complexes indicates novel pathways for the function of nuclear receptors and diverse mammalian activators". Molecular Cell 3 (3): 361–70. doi:10.1016/S1097-2765(00)80463-3. PMID 10198638.
↑ Lee SK, Anzick SL, Choi JE, Bubendorf L, Guan XY, Jung YK, Kallioniemi OP, Kononen J, Trent JM, Azorsa D, Jhun BH, Cheong JH, Lee YC, Meltzer PS, Lee JW (Nov 1999). "A nuclear factor, ASC-2, as a cancer-amplified transcriptional coactivator essential for ligand-dependent transactivation by nuclear receptors in vivo". The Journal of Biological Chemistry 274 (48): 34283–93. doi:10.1074/jbc.274.48.34283. PMID 10567404.
↑ Lee SK, Na SY, Jung SY, Choi JE, Jhun BH, Cheong J, Meltzer PS, Lee YC, Lee JW (Jun 2000). "Activating protein-1, nuclear factor-kappaB, and serum response factor as novel target molecules of the cancer-amplified transcription coactivator ASC-2". Molecular Endocrinology 14 (6): 915–25. doi:10.1210/mend.14.6.0471. PMID 10847592.
↑ Chang KH, Chen Y, Chen TT, Chou WH, Chen PL, Ma YY, Yang-Feng TL, Leng X, Tsai MJ, O'Malley BW, Lee WH (Aug 1997). "A thyroid hormone receptor coactivator negatively regulated by the retinoblastoma protein". Proceedings of the National Academy of Sciences of the United States of America 94 (17): 9040–5. doi:10.1073/pnas.94.17.9040. PMC 23019. PMID 9256431.
↑ Tan F, Lu L, Cai Y, Wang J, Xie Y, Wang L, Gong Y, Xu BE, Wu J, Luo Y, Qiang B, Yuan J, Sun X, Peng X (Jul 2008). "Proteomic analysis of ubiquitinated proteins in normal hepatocyte cell line Chang liver cells". Proteomics 8 (14): 2885–96. doi:10.1002/pmic.200700887. PMID 18655026.

Forrest D, Reh TA, Rüsch A (Feb 2002). "Neurodevelopmental control by thyroid hormone receptors". Current Opinion in Neurobiology 12 (1): 49–56. doi:10.1016/S0959-4388(02)00289-1. PMID 11861164.
Sakurai A, Bell GI, DeGroot LJ (Oct 1992). "Dinucleotide repeat polymorphism in the human thyroid hormone receptor alpha gene (THRA1) on chromosome 17". Human Molecular Genetics 1 (7): 553. doi:10.1093/hmg/1.7.553-a. PMID 1307263.
Berrodin TJ, Marks MS, Ozato K, Linney E, Lazar MA (Sep 1992). "Heterodimerization among thyroid hormone receptor, retinoic acid receptor, retinoid X receptor, chicken ovalbumin upstream promoter transcription factor, and an endogenous liver protein". Molecular Endocrinology 6 (9): 1468–78. doi:10.1210/me.6.9.1468. PMID 1331778.
Schmidt ED, Schmidt ED, van der Gaag R, Ganpat R, Broersma L, de Boer PA, Moorman AF, Lamers WH, Wiersinga WM, Koornneef L (Apr 1992). "Distribution of the nuclear thyroid-hormone receptor in extraocular and skeletal muscles". The Journal of Endocrinology 133 (1): 67–74. doi:10.1677/joe.0.1330067. PMID 1517709.
Yen PM, Sunday ME, Darling DS, Chin WW (Mar 1992). "Isoform-specific thyroid hormone receptor antibodies detect multiple thyroid hormone receptors in rat and human pituitaries". Endocrinology 130 (3): 1539–46. doi:10.1210/en.130.3.1539. PMID 1537303.
Laudet V, Begue A, Henry-Duthoit C, Joubel A, Martin P, Stehelin D, Saule S (Mar 1991). "Genomic organization of the human thyroid hormone receptor alpha (c-erbA-1) gene". Nucleic Acids Research 19 (5): 1105–12. doi:10.1093/nar/19.5.1105. PMC 333788. PMID 1850510.
Nakai A, Sakurai A, Bell GI, DeGroot LJ (Nov 1988). "Characterization of a third human thyroid hormone receptor coexpressed with other thyroid hormone receptors in several tissues". Molecular Endocrinology 2 (11): 1087–92. doi:10.1210/mend-2-11-1087. PMID 2464749.
Miyajima N, Horiuchi R, Shibuya Y, Fukushige S, Matsubara K, Toyoshima K, Yamamoto T (Apr 1989). "Two erbA homologs encoding proteins with different T3 binding capacities are transcribed from opposite DNA strands of the same genetic locus". Cell 57 (1): 31–9. doi:10.1016/0092-8674(89)90169-4. PMID 2539258.
Sakurai A, Nakai A, DeGroot LJ (Feb 1989). "Expression of three forms of thyroid hormone receptor in human tissues". Molecular Endocrinology 3 (2): 392–9. doi:10.1210/mend-3-2-392. PMID 2710139.
Sap J, Muñoz A, Damm K, Goldberg Y, Ghysdael J, Leutz A, Beug H, Vennström B (1987). "The c-erb-A protein is a high-affinity receptor for thyroid hormone". Nature 324 (6098): 635–40. doi:10.1038/324635a0. PMID 2879242.
Nakai A, Seino S, Sakurai A, Szilak I, Bell GI, DeGroot LJ (Apr 1988). "Characterization of a thyroid hormone receptor expressed in human kidney and other tissues". Proceedings of the National Academy of Sciences of the United States of America 85 (8): 2781–5. doi:10.1073/pnas.85.8.2781. PMC 280083. PMID 3357890.
Mitelman F, Manolov G, Manolova Y, Billström R, Heim S, Kristoffersson U, Mandahl N, Ferro MT, San Roman C (Jun 1986). "High resolution chromosome analysis of constitutional and acquired t(15;17) maps c-erbA to subband 17q11.2". Cancer Genetics and Cytogenetics 22 (2): 95–8. doi:10.1016/0165-4608(86)90168-8. PMID 3458521.
Benbrook D, Pfahl M (Nov 1987). "A novel thyroid hormone receptor encoded by a cDNA clone from a human testis library". Science 238 (4828): 788–91. doi:10.1126/science.3672126. PMID 3672126.
Pfahl M, Benbrook D (Nov 1987). "Nucleotide sequence of cDNA encoding a novel human thyroid hormone receptor". Nucleic Acids Research 15 (22): 9613. doi:10.1093/nar/15.22.9613. PMC 306505. PMID 3684612.
Chen JD, Evans RM (Oct 1995). "A transcriptional co-repressor that interacts with nuclear hormone receptors". Nature 377 (6548): 454–7. doi:10.1038/377454a0. PMID 7566127.
Desai-Yajnik V, Hadzic E, Modlinger P, Malhotra S, Gechlik G, Samuels HH (Aug 1995). "Interactions of thyroid hormone receptor with the human immunodeficiency virus type 1 (HIV-1) long terminal repeat and the HIV-1 Tat transactivator". Journal of Virology 69 (8): 5103–12. PMC 189328. PMID 7609079.
Lee JW, Choi HS, Gyuris J, Brent R, Moore DD (Feb 1995). "Two classes of proteins dependent on either the presence or absence of thyroid hormone for interaction with the thyroid hormone receptor". Molecular Endocrinology 9 (2): 243–54. doi:10.1210/me.9.2.243. PMID 7776974.
Desai-Yajnik V, Samuels HH (1994). "Regulation of the human immunodeficiency virus type 1 long terminal repeat: interactions of thyroid hormone receptor with retinoid-X receptor, nuclear factor kappa B, Sp1, and Tat". Transactions of the Association of American Physicians 106: 13–32. PMID 8036737.

This article incorporates text from the United States National Library of Medicine, which is in the public domain.

PDB gallery

1nav: Thyroid Receptor Alpha in complex with an agonist selective for Thyroid Receptor Beta1

2h77: Crystal structure of human TR alpha bound T3 in monoclinic space group

2h79: Crystal Structure of human TR alpha bound T3 in orthorhombic space group

Transcription factors and intracellular receptors

(1) Basic domains

(1.1) Basic leucine zipper (bZIP)	Activating transcription factor AATF 1 2 3 4 5 6 7 AP-1 c-Fos FOSB FOSL1 FOSL2 JDP2 c-Jun JUNB JunD BACH 1 2 BATF BLZF1 C/EBP α β γ δ ε ζ CREB 1 3 L1 CREM DBP DDIT3 GABPA HLF MAF B F G K NFE 2 L1 L2 L3 NFIL3 NRL NRF 1 2 3 XBP1

(1.2) Basic helix-loop-helix (bHLH)	ATOH1 AhR AHRR ARNT ASCL1 BHLH 2 3 9 ARNTL ARNTL ARNTL2 CLOCK EPAS1 FIGLA HAND 1 2 HES 5 6 HEY 1 2 L HES1 HIF 1A 3A ID 1 2 3 4 LYL1 MESP2 MXD4 MYCL1 MYCN Myogenic regulatory factors MyoD Myogenin MYF5 MYF6 Neurogenins 1 2 3 NeuroD 1 2 NPAS 1 2 3 OLIG 1 2 Pho4 Scleraxis SIM 1 2 TAL 1 2 Twist USF1

(1.3) bHLH-ZIP	AP-4 MAX MXD3 MITF MNT MLX MXI1 Myc SREBP 1 2

(1.4) NF-1	NFI A B C X SMAD R-SMAD 1 2 3 5 9 I-SMAD 6 7 4)

(1.5) RF-X	RFX 1 2 3 4 5 6 ANK

(1.6) Basic helix-span-helix (bHSH)	AP-2 α β γ δ ε

(2) Zinc finger DNA-binding domains

(2.1) Nuclear receptor (Cys₄)

subfamily 1	Thyroid hormone α β CAR FXR LXR α β PPAR α β/δ γ PXR RAR α β γ ROR α β γ Rev-ErbA α β VDR

subfamily 2	COUP-TF (I II Ear-2 HNF4 α γ PNR RXR α β γ Testicular receptor 2 4 TLX

subfamily 3	Steroid hormone Androgen Estrogen α β Glucocorticoid Mineralocorticoid Progesterone Estrogen related α β γ

subfamily 4	NUR NGFIB NOR1 NURR1

subfamily 5	LRH-1 SF1

subfamily 6	GCNF

subfamily 0	DAX1 SHP

(2.2) Other Cys₄

GATA
- 1
- 2
- 3
- 4
- 5
- 6
MTA
- 1
- 2
- 3
TRPS1

(2.3) Cys₂His₂

General transcription factors
- TFIIA
- TFIIB
- TFIID
- TFIIE
  - 1
  - 2
- TFIIF
- 1
- 2
  - TFIIH
  - 1
  - 2
  - 4
  - 2I
  - 3A
  - 3C1
  - 3C2

ATBF1
BCL
- 6
- 11A
- 11B
CTCF
E4F1
EGR
- 1
- 2
- 3
- 4
ERV3
GFI1
GLI-Krüppel family
- 1
- 2
- 3
- REST
- S1
- S2
- YY1
HIC
- 1
- 2
HIVEP
- 1
- 2
- 3
IKZF
- 1
- 2
- 3
ILF
- 2
- 3
KLF
- 1
- 2
- 3
- 4
- 5
- 6
- 7
- 8
- 9
- 10
- 11
- 12
- 13
- 14
- 15
- 17
MTF1
MYT1
OSR1
PRDM9
SALL
- 1
- 2
- 3
- 4
SP
- 1
- 2
- 4
- 7
- 8
TSHZ3
WT1
Zbtb7
- 7A
- 7B
ZBTB
- 11
- 16
- 17
- 20
- 32
- 33
- 40
zinc finger
- 3
- 7
- 9
- 10
- 19
- 22
- 24
- 33B
- 34
- 35
- 41
- 43
- 44
- 51
- 74
- 143
- 146
- 148
- 165
- 202
- 217
- 219
- 238
- 239
- 259
- 267
- 268
- 281
- 295
- 300
- 318
- 330
- 346
- 350
- 365
- 366
- 384
- 423
- 451
- 452
- 471
- 593
- 638
- 644
- 649
- 655

(2.4) Cys₆

HIVEP1

(2.5) Alternating composition

AIRE
DIDO1
GRLF1
ING
- 1
- 2
- 4
JARID
- 1A
- 1B
- 1C
- 1D
- 2
JMJD1B

(2.6) WRKY

WRKY

(3) Helix-turn-helix domains

(3.1) Homeodomain	ARX CDX 1 2 CRX CUTL1 DBX 1 2 DLX 3 4 5 EMX 1 2 EN 1 2 FHL 1 2 3 HESX1 HHEX HLX Homeobox A1 A2 A3 A4 A5 A7 A9 A10 A11 A13 B1 B2 B3 B4 B5 B6 B7 B8 B9 B13 C4 C5 C6 C8 C9 C10 C11 C12 C13 D1 D3 D4 D8 D9 D10 D11 D12 D13 HOPX IRX 1 2 3 4 5 6 MKX LMX 1A 1B MEIS 1 2 MEOX2 MNX1 MSX 1 2 NANOG NKX 2-1 2-2 2-3 2-5 3-1 3-2 6-1 6-2 NOBOX PBX 1 2 3 PHF 1 3 6 8 10 16 17 20 21A PHOX 2A 2B PITX 1 2 3 POU domain PIT-1 BRN-3: A B C Octamer transcription factor: 1 2 3/4 6 7 11 OTX 1 2 PDX1 SATB2 SHOX2 SIX 1 2 3 4 5 VAX1 ZEB 1 2

(3.2) Paired box	PAX 1 2 3 4 5 6 7 8 9 PRRX 1 2 RAX

(3.3) Fork head / winged helix	E2F 1 2 3 4 5 FOX proteins A1 A2 A3 C1 C2 D3 D4 E1 E3 F1 G1 H1 I1 J1 J2 K1 K2 L2 M1 N1 N3 O1 O3 O4 P1 P2 P3 P4

(3.4) Heat shock factors	HSF 1 2 4

(3.5) Tryptophan clusters	ELF 2 4 5 EGF ELK 1 3 4 ERF ETS 1 2 ERG SPIB ETV 1 4 5 6 FLI1 Interferon regulatory factors 1 2 3 4 5 6 7 8 MYB MYBL2

(3.6) TEA domain	transcriptional enhancer factor 1 2 3 4

(4) β-Scaffold factors with minor groove contacts

(4.1) Rel homology region	NF-κB NFKB1 NFKB2 REL RELA RELB NFAT C1 C2 C3 C4 5

(4.2) STAT	STAT 1 2 3 4 5 6

(4.3) p53	p53 TBX 1 2 3 5 19 21 22 TBR1 TBR2 TFT MYRF TP63

(4.4) MADS box	Mef2 A B C D SRF

(4.6) TATA-binding proteins	TBP TBPL1

(4.7) High-mobility group	BBX HMGB 1 2 3 4 HMGN 1 2 3 4 HNF 1A 1B LEF1 SOX 1 2 3 4 5 6 8 9 10 11 12 13 14 15 18 21 SRY SSRP1 TCF 3 4 TOX 1 2 3 4

(4.9) Grainyhead	TFCP2

(4.10) Cold-shock domain	CSDA YBX1

(4.11) Runt	CBF CBFA2T2 CBFA2T3 RUNX1 RUNX2 RUNX3 RUNX1T1

(0) Other transcription factors

(0.2) HMGI(Y)	HMGA 1 2 HBP1

(0.3) Pocket domain	Rb RBL1 RBL2

(0.5) AP-2/EREBP-related factors	Apetala 2 EREBP B3

(0.6) Miscellaneous	ARID 1A 1B 2 3A 3B 4A CAP IFI 16 35 MLL 2 3 T1 MNDA NFY A B C Rho/Sigma

see also transcription factor/coregulator deficiencies

Nuclear receptor ligands

CAR

Agonists	5β-Dihydroprogesterone 6,7-Dimethylesculetin Amiodarone Artemisinin Benfuracarb Carbamazepine Carvedilol Chlorpromazine Chrysin CITCO Clotrimazole Cyclophosphamide Cypermethrin DHEA Efavirenz Ellagic acid Griseofulvin Methoxychlor Mifepristone Nefazodone Nevirapine Nicardipine Octicizer Permethrin Phenobarbital Phenytoin Reserpine TCPOBOP Telmisartan Tolnaftate Troglitazone Valproic acid

Antagonists	3,17β-Estradiol 3α-Androstanol 3α-Androstenol 3β-Androstanol 17-Androstanol AITC Ethinyl estradiol Meclizine Nigramide J Okadaic acid PK-11195 S-07662 T-0901317

ERR

ERRα

Agonists	6,3′,4′-Trihydroxyflavone Biochanin A Cholesterol Daidzein Genistein

Antagonists	XCT-790

ERRβ

Agonists	DY-131 GSK-4716

Antagonists	4-Hydroxytamoxifen (afimoxifene) Diethylstilbestrol

ERRγ

Agonists	Bisphenol A DY-131 GSK-4716

Antagonists	4-Hydroxytamoxifen (afimoxifene) Diethylstilbestrol

FXR

Agonists	Bile acids Cafestol Chenodeoxycholic acid Fexaramine GW-4064 Obeticholic acid

Antagonists	Guggulsterone

LXR

Agonists	22R-Hydroxycholesterol 24S-Hydroxycholesterol 27-Hydroxycholesterol Cholestenoic acid DMHCA GW-3965 Hypocholamide T-0901317

PPAR

PPARα

Agonists	15-HETE 15-HpETE Aleglitazar Aluminium clofibrate Arachidonic acid Bezafibrate Clofibrate CP-775146 Daidzein DHEA Elafibranor Fenofibrate Genistein Gemfibrozil GW-7647 Leukotriene B₄ LG-101506 LG-100754 Lobeglitazone Muraglitazar Oleylethanolamide Palmitoylethanolamide Pemafibrate Perfluorononanoic acid Perfluorooctanoic acid Pioglitazone Saroglitazar Sodelglitazar Tesaglitazar Tetradecylthioacetic acid Troglitazone WY-14643

Antagonists	GW-6471 MK-886

PPARδ

Agonists	15-HETE 15-HpETE Arachidonic acid Bezafibrate Daidzein Elafibranor Genistein GW-0742 GW-501516 L-165,041 LG-101506 MBX-8025 Sodelglitazar Tetradecylthioacetic acid

Antagonists	FH-535 GSK-0660 GSK-3787

PPARγ

Agonists	5-Oxo-ETE 5-Oxo-15-hydroxy-ETE 15-Deoxy-Δ^12,14-prostaglandin J₂ 15-HETE 15-HpETE Aleglitazar Arachidonic acid Berberine Bezafibrate Ciglitazone Daidzein Darglitazone Edaglitazone Etalocib Genistein GW-1929 Ibuprofen LG-100268 LG-100754 LG-101506 Lobeglitazone Muraglitazar nTZDpa Perfluorononanoic acid Pioglitazone Prostaglandin J₂ Rosiglitazone RS5444 Saroglitazar Sodelglitazar Telmisartan Tesaglitazar Troglitazone

SPPARMs	BADGE EPI-001 INT-131 MK-0533 S26948

Antagonists	FH-535 GW-9662 SR-202 T-0070907

Unknown	SR-1664

Unselective

Agonists	Ciprofibrate Clinofibrate Clofibride Englitazone Etofibrate Farglitazar Netoglitazone Ronifibrate Rivoglitazone Simfibrate

PXR

Agonists	5α-Dihydroprogesterone 5β-Dihydroprogesterone 17α-Hydroxypregnenolone 17α-Hydroxyprogesterone Δ⁴-Androstenedione Δ⁵-Androstenediol Δ⁵-Androstenedione AA-861 Allopregnanolone Alpha-Lipoic acid Ambrisentan AMI-193 Amlodipine besylate Antimycotics Artemisinin Aurothioglucose Bile acids Bithionol Bosentan Bumecaine Cafestol Cephaloridine Cephradine Chlorpromazine Ciglitazone Clindamycin Clofenvinfos Chloroxine Clotrimazole Colforsin Corticosterone Cyclophosphamide Cyproterone acetate Demecolcine Dexamethasone DHEA DHEA-S Dibunate sodium Diclazuril Dicloxacillin Dimercaprol Dinaline Docetaxel Docusate calcium Dodecylbenzenesulfonic acid Dronabinol Droxidopa Eburnamonine Ecopipam Enzacamene Epothilone B Erythromycin Famprofazone Febantel Felodipine Fenbendazole Fentanyl Flucloxacillin Fluorometholone Griseofulvin Haloprogin Hetacillin potassium Hyperforin (Hypericum perforatum) Indinavir sulfate Lasalocid sodium Levothyroxine Linolenic acid LOE-908 Loratadine Lovastatin Meclizine Methacycline Methylprednisolone Metyrapone Mevastatin Mifepristone Nafcillin Nicardipine Nicotine Nifedipine Nilvadipine Nisoldipine Norelgestromin Omeprazole Orlistat Oxatomide Paclitaxel Phenobarbital Piperine Plicamycin Prednisolone Pregnanolone Pregnenolone Pregnenolone 16α-carbonitrile Proadifen Progesterone Reserpine Reverse triiodothyronine Rifampicin Rifaximin Rimexolone Riodipine Ritonavir Simvastatin Sirolimus Spironolactone Spiroxatrine SR-12813 Suberoylanilide Sulfisoxazole Suramin Tacrolimus Tenylidone Terconazole Testosterone isocaproate Tetracycline Thiamylal sodium Thiothixene Thonzonium bromide Tianeptine Troglitazone Troleandomycin Tropanyl 3,5-dimethulbenzoate Zafirlukast Zearalanol

Antagonists	Ketoconazole

RAR

Agonists	9CDHRA 9-cis-Retinoic acid (alitretinoin) AC-261066 AC-55649 Acitretin Adapalene all-trans-Retinoic acid (tretinoin) AM-580 BMS-493 BMS-753 BMS-961 CD-1530 CD-2314 CD-437 Ch-55 EC 23 Etretinate Fenretinide Isotretinoin Palovarotene Retinoic acid Retinol (vitamin A) Tamibarotene Tazarotene Tazarotenic acid TTNPB

Antagonists	BMS-195614 BMS-493 CD-2665 ER-50891 LE-135 MM-11253

RXR

Agonists	9CDHRA 9-cis-Retinoic acid (alitretinoin) all-trans-Retinoic acid (tretinoin) Bexarotene CD 3254 Docosahexaenoic acid Fluorobexarotene Isotretinoin LG-100268 LG-101506 LG-100754 Retinoic acid Retinol (vitamin A) SR-11237

Antagonists	HX-531 HX-630 LG-100754 PA-452 UVI-3003

SHR

See here instead.

VDR

Agonists	7-Dehydrocholesterol 22-Oxacalcitriol 25-Hydroxyergocalciferol Alfacalcidol Calcifediol Calciferol Calcipotriol Calcitriol Cholecalciferol (vitamin D₃) Dihydrotachysterol Doxercalciferol EB-1089 Eldecalcitol Ercalcidiol Ercalcitriol Ergocalciferol (vitamin D₂) Lithocholic acid Paricalcitol Tacalcitol

Agonists	Dextrothyroxine GC-1 Levothyroxine Liothyronine Thyroxine Tiratricol Triiodothyronine

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Thyroid hormone receptor alpha

Function

Interactions

References

Further reading