General Information of the Protein
Protein ID |
PT01019
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Protein Name |
5-hydroxytryptamine receptor 2B
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Secondarily Protein Name |
Serotonin receptor 2B
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Gene Name |
HTR2B
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Sequence |
MALSYRVSELQSTIPEHILQSTFVHVISSNWSGLQTESIPEEMKQIVEEQGNKLHWAALLILMVIIPTIGGNTLVILAVSLEKKLQYATNYFLMSLAVADLLVGLFVMPIALLTIMFEAMWPLPLVLCPAWLFLDVLFSTASIMHLCAISVDRYIAIKKPIQANQYNSRATAFIKITVVWLISIGIAIPVPIKGIETDVDNPNNITCVLTKERFGDFMLFGSLAAFFTPLAIMIVTYFLTIHALQKKAYLVKNKPPQRLTWLTVSTVFQRDETPCSSPEKVAMLDGSRKDKALPNSGDETLMRRTSTIGKKSVQTISNEQRASKVLGIVFFLFLLMWCPFFITNITLVLCDSCNQTTLQMLLEIFVWIGYVSSGVNPLVYTLFNKTFRDAFGRYITCNYRATKSVKTLRKRSSKIYFRNPMAENSKFFKKHGIRNGINPAMYQSPMRLRSSTIQSSSIILLDTLLLTENEGDKTEEQVSYV
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Organism |
Homo sapiens, Human
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Protein Classification |
Membrane receptor
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Family A G protein-coupled receptor
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Small molecule receptor (family A GPCR)
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Monoamine receptor
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Serotonin receptor
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Function |
G-protein coupled receptor for 5-hydroxytryptamine (serotonin) (PubMed:8143856, PubMed:7926008, PubMed:8078486, PubMed:8882600, PubMed:18703043, PubMed:23519210). Also functions as a receptor for various ergot alkaloid derivatives and psychoactive substances (PubMed:8143856, PubMed:7926008, PubMed:8078486, PubMed:12970106, PubMed:18703043, PubMed:23519210, PubMed:23519215, PubMed:24357322, PubMed:28129538). Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors (PubMed:8143856, PubMed:8078486, PubMed:8882600, PubMed:23519215, PubMed:28129538). Beta-arrestin family members inhibit signaling via G proteins and mediate activation of alternative signaling pathways (PubMed:23519215, PubMed:28129538). Signaling activates a phosphatidylinositol-calcium second messenger system that modulates the activity of phosphatidylinositol 3-kinase and down-stream signaling cascades and promotes the release of Ca(2+) ions from intracellular stores (PubMed:8143856, PubMed:8078486, PubMed:8882600, PubMed:18703043, PubMed:23519215, PubMed:28129538). Plays a role in the regulation of dopamine and 5-hydroxytryptamine release, 5-hydroxytryptamine uptake and in the regulation of extracellular dopamine and 5-hydroxytryptamine levels, and thereby affects neural activity. May play a role in the perception of pain (By similarity). Plays a role in the regulation of behavior, including impulsive behavior (PubMed:21179162). Required for normal proliferation of embryonic cardiac myocytes and normal heart development. Protects cardiomyocytes against apoptosis. Plays a role in the adaptation of pulmonary arteries to chronic hypoxia. Plays a role in vasoconstriction. Required for normal osteoblast function and proliferation, and for maintaining normal bone density. Required for normal proliferation of the interstitial cells of Cajal in the intestine (By similarity).
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Uniprot ID |
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Subcellular Location |
Cell membrane
Synapse
Synaptosome
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Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein Protein Cell Line Compound Bioactivity Value: <= 0.1 μM > 0.1 μM and <= 10 μM > 10 μM Imprecise Activity |
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Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000901 , 661W
Cell Line ID: CL000011 , CHO
Cell Line ID: CL000026 , CHO-K1
Cell Line ID: CL000088 , Flp-In-293
Cell Line ID: CL000460 , Flp-In-T-REx-293
Cell Line ID: CL000025 , HEK-293T
Cell Line ID: CL000006 , HEK293
Cell Line ID: CL000065 , HEK293-EBNA
Cell Line ID: CL000017 , HeLa
Cell Line ID: CL000035 , NIH 3T3
Cell Line ID: CL000013 , Sf9
Cell Line ID: CL000004 , SH-SY5Y
Biochemical Assays
Clinical Information about the Protein
Target 1 ( 5-HT 2B receptor (HTR2B) )
Target Type | Successful Target | ||||
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Disease | 7 Target-related Diseases | 7 | |||
1 | Hyperprolactinaemia [ICD-11: 5A60.1] | ||||
2 | Depression [ICD-11: 6A70-6A7Z] | ||||
3 | Psychotic disorder [ICD-11: 6A20-6A25] | ||||
4 | Pulmonary arterial hypertension [ICD-11: BB01.0] | ||||
5 | Coronary artery disease [ICD-11: BA80] | ||||
6 | Anxiety disorder [ICD-11: 6B00-6B0Z] | ||||
7 | Migraine [ICD-11: 8A80] | ||||
Approved Drug(s) | 3 Approved Drugs | 3 | |||
1 | Metergolin | Approved | |||
2 | Minaprine | Approved | |||
3 | Triflupromazine | Approved | |||
Clinical Trial Drug(s) | 2 Clinical Trial Drugs | 2 | |||
1 | PRX-08066 | Phase 2 | |||
2 | Vabicaserin | Phase 2 | |||
Discontinued Drug(s) | 3 Discontinued Drugs | 3 | |||
1 | FENDILINE | Withdrawn from market | |||
2 | Ritanserin | Discontinued in Phase 3 | |||
3 | MT-500 | Discontinued in Phase 1 |