Target Information

Target General Infomation
Target ID
T60606
Former ID
TTDS00452
Target Name
Thyrotropin receptor
Gene Name
TSHR
Synonyms
TSH receptor; TSH-R; Thyroid stimulating hormone receptor; TSHR
Target Type
Successful
Disease Diagnostic test to differentiate primary and secondary hypothyroidism [ICD10: W88]
Thyroid cancer [ICD9: 140-229, 193; ICD10: C73]
Thyroid cancer diagnosis [ICD9: 193; ICD10: C73]
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).
BioChemical Class
GPCR rhodopsin
UniProt ID
P16473
Sequence
MRPADLLQLVLLLDLPRDLGGMGCSSPPCECHQEEDFRVTCKDIQRIPSLPPSTQTLKLI
ETHLRTIPSHAFSNLPNISRIYVSIDVTLQQLESHSFYNLSKVTHIEIRNTRNLTYIDPD
ALKELPLLKFLGIFNTGLKMFPDLTKVYSTDIFFILEITDNPYMTSIPVNAFQGLCNETL
TLKLYNNGFTSVQGYAFNGTKLDAVYLNKNKYLTVIDKDAFGGVYSGPSLLDVSQTSVTA
LPSKGLEHLKELIARNTWTLKKLPLSLSFLHLTRADLSYPSHCCAFKNQKKIRGILESLM
CNESSMQSLRQRKSVNALNSPLHQEYEENLGDSIVGYKEKSKFQDTHNNAHYYVFFEEQE
DEIIGFGQELKNPQEETLQAFDSHYDYTICGDSEDMVCTPKSDEFNPCEDIMGYKFLRIV
VWFVSLLALLGNVFVLLILLTSHYKLNVPRFLMCNLAFADFCMGMYLLLIASVDLYTHSE
YYNHAIDWQTGPGCNTAGFFTVFASELSVYTLTVITLERWYAITFAMRLDRKIRLRHACA
IMVGGWVCCFLLALLPLVGISSYAKVSICLPMDTETPLALAYIVFVLTLNIVAFVIVCCC
YVKIYITVRNPQYNPGDKDTKIAKRMAVLIFTDFICMAPISFYALSAILNKPLITVSNSK
ILLVLFYPLNSCANPFLYAIFTKAFQRDVFILLSKFGICKRQAQAYRGQRVPPKNSTDIQ
VQKVTHDMRQGLHNMEDVYELIENSHLTPKKQGQISEEYMQTVL
Drugs and Mode of Action
Drug(s) Thyrotropin Drug Info Approved Diagnostic test to differentiate primary and secondary hypothyroidism [551871]
Thyrotropin Alfa Drug Info Approved Thyroid cancer diagnosis [538556]
Agonist Labeled TSH superagonists Drug Info [543645]
Recombinant TSH superagonists Drug Info [543645]
Modulator Thyrotropin Drug Info [556264]
Binder Thyrotropin Alfa Drug Info [536852], [537604]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway cAMP signaling pathway
Neuroactive ligand-receptor interaction
Thyroid hormone synthesis
Autoimmune thyroid disease
NetPath Pathway Wnt Signaling Pathway
Pathway Interaction Database Arf6 trafficking events
Arf6 signaling events
Reactome Hormone ligand-binding receptors
G alpha (s) signalling events
WikiPathways Peptide GPCRs
TSH signaling pathway
Thyroxine (Thyroid Hormone) Production
GPCR ligand binding
GPCR downstream signaling
References
Ref 538556FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 020898.
Ref 551871Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
Ref 536852Diagnosis of poorly differentiated thyroid cancer with radioiodine scanning after thyrotropin alfa stimulation. N Engl J Med. 2008 Sep 18;359(12):1295-7.
Ref 537604Pharmacological 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 543645(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).
Ref 556264Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.

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