Target Information
| Target General Information | Top | |||||
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| Target ID |
T60606
(Former ID: TTDS00452)
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| Target Name |
Thyrotropin receptor (TSHR)
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| Synonyms |
Thyroid stimulating hormone receptor; TSHR; TSH-R; TSH receptor
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| Gene Name |
TSHR
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| Target Type |
Successful target
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[1] | ||||
| Disease | [+] 2 Target-related Diseases | + | ||||
| 1 | Hypo-thyroidism [ICD-11: 5A00] | |||||
| 2 | Thyroid cancer [ICD-11: 2D10] | |||||
| Function |
Receptor for thyrothropin. Plays a central role in controlling thyroid cell metabolism. The activity of this receptor is mediated by G proteins which activate adenylate cyclase. Also acts as a receptor for thyrostimulin (gpa2+gpb5).
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| BioChemical Class |
GPCR rhodopsin
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| UniProt ID | ||||||
| Sequence |
MRPADLLQLVLLLDLPRDLGGMGCSSPPCECHQEEDFRVTCKDIQRIPSLPPSTQTLKLI
ETHLRTIPSHAFSNLPNISRIYVSIDVTLQQLESHSFYNLSKVTHIEIRNTRNLTYIDPD ALKELPLLKFLGIFNTGLKMFPDLTKVYSTDIFFILEITDNPYMTSIPVNAFQGLCNETL TLKLYNNGFTSVQGYAFNGTKLDAVYLNKNKYLTVIDKDAFGGVYSGPSLLDVSQTSVTA LPSKGLEHLKELIARNTWTLKKLPLSLSFLHLTRADLSYPSHCCAFKNQKKIRGILESLM CNESSMQSLRQRKSVNALNSPLHQEYEENLGDSIVGYKEKSKFQDTHNNAHYYVFFEEQE DEIIGFGQELKNPQEETLQAFDSHYDYTICGDSEDMVCTPKSDEFNPCEDIMGYKFLRIV VWFVSLLALLGNVFVLLILLTSHYKLNVPRFLMCNLAFADFCMGMYLLLIASVDLYTHSE YYNHAIDWQTGPGCNTAGFFTVFASELSVYTLTVITLERWYAITFAMRLDRKIRLRHACA IMVGGWVCCFLLALLPLVGISSYAKVSICLPMDTETPLALAYIVFVLTLNIVAFVIVCCC YVKIYITVRNPQYNPGDKDTKIAKRMAVLIFTDFICMAPISFYALSAILNKPLITVSNSK ILLVLFYPLNSCANPFLYAIFTKAFQRDVFILLSKFGICKRQAQAYRGQRVPPKNSTDIQ VQKVTHDMRQGLHNMEDVYELIENSHLTPKKQGQISEEYMQTVL Click to Show/Hide
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| 3D Structure | Click to Show 3D Structure of This Target | AlphaFold | ||||
| HIT2.0 ID | T15YX5 | |||||
| Drugs and Modes of Action | Top | |||||
|---|---|---|---|---|---|---|
| Approved Drug(s) | [+] 2 Approved Drugs | + | ||||
| 1 | Thyrotropin | Drug Info | Approved | Hypothyroidism | [2] | |
| 2 | Thyrotropin Alfa | Drug Info | Approved | Thyroid cancer | [3] | |
| Mode of Action | [+] 3 Modes of Action | + | ||||
| Modulator | [+] 1 Modulator drugs | + | ||||
| 1 | Thyrotropin | Drug Info | [4] | |||
| Binder | [+] 1 Binder drugs | + | ||||
| 1 | Thyrotropin Alfa | Drug Info | [1], [5] | |||
| Agonist | [+] 1 Agonist drugs | + | ||||
| 1 | Recombinant TSH superagonists | Drug Info | [6] | |||
| Chemical Structure based Activity Landscape of Target | Top |
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| Target Profiles in Patients | Top | |||||
|---|---|---|---|---|---|---|
| Target Expression Profile (TEP) | ||||||
| Target Affiliated Biological Pathways | Top | |||||
|---|---|---|---|---|---|---|
| KEGG Pathway | [+] 4 KEGG Pathways | + | ||||
| 1 | cAMP signaling pathway | |||||
| 2 | Neuroactive ligand-receptor interaction | |||||
| 3 | Thyroid hormone synthesis | |||||
| 4 | Autoimmune thyroid disease | |||||
| NetPath Pathway | [+] 1 NetPath Pathways | + | ||||
| 1 | Wnt Signaling Pathway | |||||
| PID Pathway | [+] 2 PID Pathways | + | ||||
| 1 | Arf6 trafficking events | |||||
| 2 | Arf6 signaling events | |||||
| Reactome | [+] 2 Reactome Pathways | + | ||||
| 1 | Hormone ligand-binding receptors | |||||
| 2 | G alpha (s) signalling events | |||||
| WikiPathways | [+] 5 WikiPathways | + | ||||
| 1 | Peptide GPCRs | |||||
| 2 | TSH signaling pathway | |||||
| 3 | Thyroxine (Thyroid Hormone) Production | |||||
| 4 | GPCR ligand binding | |||||
| 5 | GPCR downstream signaling | |||||
| References | Top | |||||
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| REF 1 | Pharmacological profiles and clinical effects of recombinant human thyrotropin alfa (Thyrogen) Intramuscular Injection 0.9 mg). Nippon Yakurigaku Zasshi. 2009 Jul;134(1):28-34. | |||||
| REF 2 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015 | |||||
| REF 3 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 020898. | |||||
| REF 4 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. | |||||
| REF 5 | Diagnosis of poorly differentiated thyroid cancer with radioiodine scanning after thyrotropin alfa stimulation. N Engl J Med. 2008 Sep 18;359(12):1295-7. | |||||
| REF 6 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 255). | |||||
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