Target Information

Target General Infomation
Target ID
T77796
Former ID
TTDR01197
Target Name
Thyrotropin-releasing hormone receptor
Gene Name
TRHR
Synonyms
TRH-R; Thyroliberin receptor; TRHR
Target Type
Successful
Disease Cognitive disorders [ICD9: 290-294, 294.0, 780.09, 780.9, 780.93; ICD10: F01-F07, F04, F05, R41.3]
CNS stimulant [ICD code not available]
Endocrine disease [ICD10: E00-E35]
Neurodegenerative disease [ICD9: 330-337; ICD10: G30-G32]
Pain [ICD9: 338, 356.0, 356.8,780; ICD10: G64, G90.0, R52, G89]
Unspecified [ICD code not available]
Function
Receptor for thyrotropin-releasing hormone. This receptor is mediated by G proteins which activate a phosphatidylinositol-calcium second messenger system.
BioChemical Class
GPCR rhodopsin
Target Validation
T77796
UniProt ID
P34981
Sequence
MENETVSELNQTQLQPRAVVALEYQVVTILLVLIICGLGIVGNIMVVLVVMRTKHMRTPT
NCYLVSLAVADLMVLVAAGLPNITDSIYGSWVYGYVGCLCITYLQYLGINASSCSITAFT
IERYIAICHPIKAQFLCTFSRAKKIIIFVWAFTSLYCMLWFFLLDLNISTYKDAIVISCG
YKISRNYYSPIYLMDFGVFYVVPMILATVLYGFIARILFLNPIPSDPKENSKTWKNDSTH
QNTNLNVNTSNRCFNSTVSSRKQVTKMLAVVVILFALLWMPYRTLVVVNSFLSSPFQENW
FLLFCRICIYLNSAINPVIYNLMSQKFRAAFRKLCNCKQKPTEKPANYSVALNYSVIKES
DHFSTELDDITVTDTYLSATKVSFDDTCLASEVSFSQS
Drugs and Mode of Action
Drug(s) protirelin Drug Info Approved Unspecified [1559458]
Protirelin Drug Info Approved CNS stimulant [551871]
AZETIRELIN Drug Info Phase 3 Pain [544285]
MONTIRELIN TETRAHYDRATE Drug Info Discontinued in Preregistration Pain [544994]
Posatirelin Drug Info Discontinued in Phase 3 Neurodegenerative disease [545969]
JTP-2942 Drug Info Discontinued in Phase 2 Cognitive disorders [545198]
Modulator AZETIRELIN Drug Info [531635], [533643]
JTP-2942 Drug Info [533738]
MK-771 Drug Info
MONTIRELIN TETRAHYDRATE Drug Info [531635], [534144]
Posatirelin Drug Info [526454]
protirelin Drug Info
Protirelin Drug Info [556264]
Inhibitor C4X-101 Drug Info [543794]
CORYMBONE B Drug Info [529425]
Agonist MeTRH Drug Info [533507]
[3H]MeTRH Drug Info [533535]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway Calcium signaling pathway
Neuroactive ligand-receptor interaction
PANTHER Pathway Thyrotropin-releasing hormone receptor signaling pathway
Reactome Peptide ligand-binding receptors
G alpha (q) signalling events
WikiPathways GPCRs, Class A Rhodopsin-like
Gastrin-CREB signalling pathway via PKC and MAPK
Peptide GPCRs
GPCR ligand binding
GPCR downstream signaling
References
Ref 544285Developing a metagenomic view of xenobiotic metabolism. Pharmacol Res. 2013 March; 69(1): 21-31.
Ref 544994Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001824)
Ref 545198Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002435)
Ref 545969Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005568)
Ref 551871Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
Ref 1559458Company report (takeda)
Ref 526454TRH analogs at Gedeon Richter Ltd.: highlights of experimental and clinical efficacy of posatirelin. Acta Pharm Hung. 2002;72(1):62-8.
Ref 529425J Nat Prod. 2008 May;71(5):881-3. Epub 2008 Apr 16.Corymbones A and B, phloroglucinols with thyrotropin releasing hormone receptor 2 binding affinity from the flowers of Corymbia peltata.
Ref 531635Therapeutic target database update 2012: a resource for facilitating target-oriented drug discovery. Nucleic Acids Res. 2012 Jan;40(Database issue):D1128-36.
Ref 533507Synthetic TRF (thyrotropin releasing factor) analogues. II. pGlu-N3imMe-His-Pro-NH2: a synthetic analogue with specific activity greater than that of TRF2. Endocrinology. 1971 Dec;89(6):1485-8.
Ref 533535Preparation of 3H-[3-M3-His2]TRH as an improved ligand for TRH receptors. Neuroendocrinology. 1981 May;32(5):310-6.
Ref 533643Intestinal absorption of azetirelin, a new thyrotropin-releasing hormone (TRH) analogue. II. In situ and in vitro absorption characteristics of azetirelin from the rat intestine. Biol Pharm Bull. 1995 Jul;18(7):976-9.
Ref 533738Effect of JTP-2942, a novel thyrotropin-releasing hormone analogue, on pentobarbital-induced anesthesia in rats. Eur J Pharmacol. 1995 Mar 24;276(1-2):177-82.
Ref 534144Montirelin hydrate (NS-3), a TRH analog, improved the disturbance of consciousness caused by head concussion and pentobarbital in mice. Nihon Yakurigaku Zasshi. 1996 May;107(5):237-45.
Ref 543794(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: 363).
Ref 556264Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.

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