促甲状腺激素受体

Thyroid stimulating hormone receptor
促甲状腺激素受体
Thyroid stimulating hormone receptor; 促甲状腺激素受体
	Rendering based on PDB 1XUM.
有效结构
PDB	直系同源检索：PDBe, RCSB
PDB查询代码列表
	2XWT, 3G04
标识
代号	TSHR; CHNG1; LGR3; hTSHR-I
扩展标识	遗传学：603372 鼠基因：98849 同源基因：315 IUPHAR: TSH ChEMBL: 1963 GeneCards: TSHR Gene
基因本体论描述
分子功能	· thyroid-stimulating hormone receptor activity; · protein binding;
细胞成分	· plasma membrane; · integral to plasma membrane;
生物过程	· G-protein coupled receptor signaling pathway; · G-protein coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger; · cell-cell signaling; · positive regulation of cell proliferation;
	Sources: Amigo / QuickGO
RNA表达模式
	更多表达数据
直系同源体
物种	人类
Entrez	7253
Ensembl	ENSG00000165409
UniProt	P16473
mRNA序列	NM_000369
蛋白序列	NP_000360
基因位置	Chr 14:; 81.42 – 81.61 Mb
PubMed查询	[1]
	查; 论; 编;

促甲状腺激素受体（英语：thyrotropin receptor，TSH receptor，TSHR）又称甲促素受体，是一种接受促甲状腺激素（甲促素，thyrotropin）信号，刺激细胞生成甲状腺激素（T4）和三碘甲状腺激素（T3）的跨膜受体。TSHR是整合膜蛋白中G蛋白偶联受体超家族的一员^[1]，与G_s蛋白偶合^[2]。

该受体主要出现在甲状腺上皮细胞（英语：thyroid epithelial cell）的表面。

功能

在结合血循的TSH后，G蛋白信号级联反应会激活腺苷酸环化酶（adenylyl cyclase）进而使胞内环腺苷酸（cAMP）浓度升高。环腺苷酸可活化甲状腺细胞各功能层面，包括：碘泵运，甲状腺球蛋白的合成、碘化、胞吞和蛋白酶解，甲状腺过氧化物酶活性，以及甲状腺激素释放。

另见

弥漫性毒性甲状腺肿

参考文献

^ Farid NR, Szkudlinski MW. Minireview: structural and functional evolution of the thyrotropin receptor. Endocrinology. 2004, 145 (9): 4048–57. PMID 15231707. doi:10.1210/en.2004-0437.
^ Calebiro D, Nikolaev VO, Lohse MJ. Imaging of persistent cAMP signaling by internalized G protein-coupled receptors. J. Mol. Endocrinol. July 2010, 45 (1): 1–8. PMID 20378719. doi:10.1677/JME-10-0014.

延伸阅读

Führer D, Wonerow P, Willgerodt H, Paschke R. Identification of a new thyrotropin receptor germline mutation (Leu629Phe) in a family with neonatal onset of autosomal dominant nonautoimmune hyperthyroidism.. J. Clin. Endocrinol. Metab. 1998, 82 (12): 4234–8. PMID 9398746. doi:10.1210/jc.82.12.4234.
Farid NR, Kascur V, Balazs C. The human thyrotropin receptor is highly mutable: a review of gain-of-function mutations.. Eur. J. Endocrinol. 2000, 143 (1): 25–30. PMID 10870027. doi:10.1530/eje.0.1430025.
Szkudlinski MW, Fremont V, Ronin C, Weintraub BD. Thyroid-stimulating hormone and thyroid-stimulating hormone receptor structure-function relationships.. Physiol. Rev. 2002, 82 (2): 473–502. PMID 11917095. doi:10.1152/physrev.00031.2001.
Tonacchera M, Vitti P, De Servi M; et al. Gain of function TSH receptor mutations and iodine deficiency: implications in iodine prophylaxis.. J. Endocrinol. Invest. 2004, 26 (2 Suppl): 2–6. PMID 12762632.
Arturi F, Scarpelli D, Coco A; et al. Thyrotropin receptor mutations and thyroid hyperfunctioning adenomas ten years after their first discovery: unresolved questions.. Thyroid. 2004, 13 (4): 341–3. PMID 12804102. doi:10.1089/105072503321669811.
Vaidya B, Campbell V, Tripp JH; et al. Premature birth and low birth weight associated with nonautoimmune hyperthyroidism due to an activating thyrotropin receptor gene mutation.. Clin. Endocrinol. (Oxf). 2004, 60 (6): 711–8. PMID 15163335. doi:10.1111/j.1365-2265.2004.02040.x.
Takeshita A, Nagayama Y, Fujiyama K; et al. Molecular cloning and sequencing of an alternatively spliced form of the human thyrotropin receptor transcript.. Biochem. Biophys. Res. Commun. 1992, 188 (3): 1214–9. PMID 1445355. doi:10.1016/0006-291X(92)91360-3.
Graves PN, Tomer Y, Davies TF. Cloning and sequencing of a 1.3 KB variant of human thyrotropin receptor mRNA lacking the transmembrane domain.. Biochem. Biophys. Res. Commun. 1992, 187 (2): 1135–43. PMID 1530609. doi:10.1016/0006-291X(92)91315-H.
Loosfelt H, Pichon C, Jolivet A; et al. Two-subunit structure of the human thyrotropin receptor. Proc. Natl. Acad. Sci. U.S.A. 1992, 89 (9): 3765–9. PMC 525571 . PMID 1570295. doi:10.1073/pnas.89.9.3765.
Nagayama Y, Russo D, Wadsworth HL; et al. Eleven amino acids (Lys-201 to Lys-211) and 9 amino acids (Gly-222 to Leu-230) in the human thyrotropin receptor are involved in ligand binding. J. Biol. Chem. 1991, 266 (23): 14926–30. PMID 1651314.
Murakami M, Mori M. Identification of immunogenic regions in human thyrotropin receptor for immunoglobulin G of patients with Graves' disease. Biochem. Biophys. Res. Commun. 1990, 171 (1): 512–8. PMID 1697467. doi:10.1016/0006-291X(90)91423-P.
Heldin NE, Gustavsson B, Westermark K, Westermark B. A somatic point mutation in a putative ligand binding domain of the TSH receptor in a patient with autoimmune hyperthyroidism. J. Clin. Endocrinol. Metab. 1992, 73 (6): 1374–6. PMID 1955520. doi:10.1210/jcem-73-6-1374.
Libert F, Passage E, Lefort A; et al. Localization of human thyrotropin receptor gene to chromosome region 14q3 by in situ hybridization. Cytogenet. Cell Genet. 1991, 54 (1–2): 82–3. PMID 2249482. doi:10.1159/000132964.
Frazier AL, Robbins LS, Stork PJ; et al. Isolation of TSH and LH/CG receptor cDNAs from human thyroid: regulation by tissue specific splicing. Mol. Endocrinol. 1991, 4 (8): 1264–76. PMID 2293030. doi:10.1210/mend-4-8-1264.
Misrahi M, Loosfelt H, Atger M; et al. Cloning, sequencing and expression of human TSH receptor. Biochem. Biophys. Res. Commun. 1990, 166 (1): 394–403. PMID 2302212. doi:10.1016/0006-291X(90)91958-U.
Nagayama Y, Kaufman KD, Seto P, Rapoport B. Molecular cloning, sequence and functional expression of the cDNA for the human thyrotropin receptor. Biochem. Biophys. Res. Commun. 1990, 165 (3): 1184–90. PMID 2558651. doi:10.1016/0006-291X(89)92727-7.
Libert F, Lefort A, Gerard C; et al. Cloning, sequencing and expression of the human thyrotropin (TSH) receptor: evidence for binding of autoantibodies. Biochem. Biophys. Res. Commun. 1990, 165 (3): 1250–5. PMID 2610690. doi:10.1016/0006-291X(89)92736-8.
Cuddihy RM, Bryant WP, Bahn RS. Normal function in vivo of a homozygotic polymorphism in the human thyrotropin receptor. Thyroid. 1996, 5 (4): 255–7. PMID 7488864. doi:10.1089/thy.1995.5.255.
Bahn RS, Dutton CM, Heufelder AE, Sarkar G. A genomic point mutation in the extracellular domain of the thyrotropin receptor in patients with Graves' ophthalmopathy. J. Clin. Endocrinol. Metab. 1994, 78 (2): 256–60. PMID 7508946. doi:10.1210/jc.78.2.256.
Sunthornthepvarakui T, Gottschalk ME, Hayashi Y, Refetoff S. Brief report: resistance to thyrotropin caused by mutations in the thyrotropin-receptor gene. N. Engl. J. Med. 1995, 332 (3): 155–60. PMID 7528344. doi:10.1056/NEJM199501193320305.

外部链接

Glycoprotein Hormone Receptors: TSH. IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology. （原始内容存档于2013-11-01）.
医学主题词表（MeSH）：Thyrotropin+Receptors
GRIS: Glycoprotein-hormone Receptor Information System

[pmid15231707-1] Farid NR, Szkudlinski MW. Minireview: structural and functional evolution of the thyrotropin receptor. Endocrinology. 2004, 145 (9): 4048–57. PMID 15231707. doi:10.1210/en.2004-0437.

[pmid20378719-2] Calebiro D, Nikolaev VO, Lohse MJ. Imaging of persistent cAMP signaling by internalized G protein-coupled receptors. J. Mol. Endocrinol. July 2010, 45 (1): 1–8. PMID 20378719. doi:10.1677/JME-10-0014.

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