Tclin 5-hydroxytryptamine receptor 2B

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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).

This gene encodes one of the several different receptors for 5-hydroxytryptamine (serotonin) that belongs to the G-protein coupled receptor 1 family. Serotonin is a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. Serotonin receptors mediate many of the central and peripheral physiologic functions of serotonin, including regulation of cardiovascular functions and impulsive behavior. Population and family-based analyses of a minor allele (glutamine-to-stop substitution, designated Q20*) which blocks expression of this protein, and knockout studies in mice, suggest a role for this gene in impulsivity. However, other factors, such as elevated testosterone levels, may also be involved. Alternatively spliced transcript variants have been found for this gene. [provided by RefSeq, Mar 2016]

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Property Summary

Ligand Count	554
NCBI Gene PubMed Count	69
PubMed Score	486.27

PubTator Score	175.63

Knowledge Summary

Patent (8,933)

TINX Plot

Disease (6)

Disease	Target Count	Z-score	Confidence
Hypertension	396	3.601	1.8
Cardiomegaly	116	0.0	0.0
Drug-Related Side Effects and Adverse Reactions	62	0.0	0.0
Heart Valve Diseases	25	0.0	0.0
Heart failure	162	0.0	0.0
Hypertension, Pulmonary	37	0.0	0.0

Disease	Target Count
Adverse reaction to drug	61
Heart valve disease	39
Hypertensive disease	292
Pulmonary hypertension	85

Disease	Target Count
Migraine	83
Acromegaly	51
Amenorrhea	58
Chronic thromboembolic pulmonary hypertension	4
Major Depressive Disorder	301
Migraine Prevention	23
pulmonary arterial hypertension	75

Disease	Target Count	P-value
malignant mesothelioma	3232	1.1e-05
psoriasis	6694	1.1e-05
adrenocortical carcinoma	1428	1.3e-05
osteosarcoma	7950	1.1e-04
invasive ductal carcinoma	2951	1.3e-02
non diabetic and post-ischemic heart failure	200	4.4e-02

Disease	Target Count	Z-score	Confidence
Carcinoma	11493	0.0	0.7

Disease	Target Count	Z-score	Confidence
Heart disease	306	3.935	2.0
Irritable bowel syndrome	60	3.787	1.9
Schizophrenia	1160	3.432	1.7
Hypoactive sexual desire disorder	8	3.307	1.7
Obesity	678	3.015	1.5

Differential Expression (6)

Disease	log2 FC	p
adrenocortical carcinoma	-3.234	1.3e-05
invasive ductal carcinoma	-1.300	1.3e-02
malignant mesothelioma	1.600	1.1e-05
non diabetic and post-ischemic heart fai...	1.200	4.4e-02
osteosarcoma	-3.617	1.1e-04
psoriasis	-4.000	1.1e-05

Uterus 17,618

Adrenal Gland 18,071

Colon - Sigmoid 18,089

Artery - Coronary 17,949

Stomach 17,879

Thyroid 18,024

Artery - Aorta 17,896

Esophagus - Muscularis 18,017

Heart - Atrial Appendage 17,896

Esophagus - Gastroesophageal Junction 18,000

Artery - Tibial 17,631

Adipose - Subcutaneous 18,110

Vagina 17,834

Adipose - Visceral (Omentum) 17,937

Cells - Transformed fibroblasts 17,577

Spleen 17,614

Breast - Mammary Tissue 18,103

Ovary 17,971

Small Intestine - Terminal Ileum 17,954

Kidney - Cortex 17,329

Prostate 18,213

Lung 18,057

Pituitary 18,147

Cells - EBV-transformed lymphocytes 18,186

Nerve - Tibial 18,007

Minor Salivary Gland 18,005

Liver 18,071

Testis 18,518

Colon - Transverse 17,825

Heart - Left Ventricle 18,006

Skin - Not Sun Exposed (Suprapubic) 18,081

Brain - Spinal cord (cervical c-1) 17,973

Esophagus - Mucosa 18,076

Skin - Sun Exposed (Lower leg) 17,968

Brain - Cerebellum 17,983

Brain - Cerebellar Hemisphere 18,015

Brain - Caudate (basal ganglia) 18,001

Brain - Putamen (basal ganglia) 17,863

Brain - Hypothalamus 18,169

Brain - Hippocampus 18,011

Brain - Cortex 18,039

Brain - Substantia nigra 17,981

Brain - Frontal Cortex (BA9) 18,069

Brain - Anterior cingulate cortex (BA24) 17,989

Brain - Nucleus accumbens (basal ganglia... 18,024

Brain - Amygdala 18,006

Pancreas 18,123

Muscle - Skeletal 17,778

Whole Blood 17,439

adipose tissue 15,837

adrenal gland 15,963

appendix 16,247

bone marrow 14,571

breast 16,063

cerebral cortex 16,630

cervix, uterine 15,871

colon 15,959

duodenum 15,975

endometrium 16,349

epididymis 15,863

esophagus 15,898

fallopian tube 16,245

gallbladder 16,333

heart muscle 14,972

kidney 15,917

liver 14,587

lung 16,312

lymph node 15,833

ovary 15,408

parathyroid gland 14,769

placenta 15,937

prostate 16,460

rectum 15,705

salivary gland 14,981

seminal vesicle 15,918

skin 16,206

small intestine 16,154

smooth muscle 15,857

spleen 15,972

stomach 16,099

testis 17,936

thyroid gland 15,959

tonsil 15,400

urinary bladder 15,814

Liver and Pancreas 16,750

Digestive Tract 17,369

Urinary Tract 16,678

Endocrine System 18,159

Blood and immune system 16,909

Respiratory system 16,393

Female tissues 17,400

Male tissues 17,142

Skin and soft tissues 17,230

Nervous System 16,725

Cardiovascular System 15,192

Brain 7,346

Colon 1,063

Skin 1,556

Uterus 1,493

See source...

Brain 1,516

Artery 356

Nerve 290

Muscle 1,170

Heart 914

Stomach 185

Ganglion 334

Interstitial cell 21

Blood 1,962

Spinal cord 549

See source...

Synonym

Accession	P41595 B2R9D5 Q53TI1 Q62221 Q6P523 5-HT-2B
Symbols	5-HT2B 5-HT-2B 5-HT(2B)

Gene

HTR2B

PANTHER Protein Class (2)

receptor 400

G-protein coupled receptor 221

Ortholog (14)

Species	Source	Disease
Chimp 14,136	OMA EggNOG
Macaque 12,758	Inparanoid OMA EggNOG
Mouse 16,567	Inparanoid OMA EggNOG
Rat 15,112	Inparanoid OMA EggNOG
Dog 15,069	OMA EggNOG
Horse 14,249	Inparanoid OMA EggNOG
Cow 15,316	Inparanoid OMA EggNOG
Pig 10,164	OMA EggNOG
Opossum 12,223	Inparanoid OMA EggNOG
Platypus 5,699	OMA EggNOG
Chicken 7,823	OMA EggNOG
Anole lizard 10,585	Inparanoid OMA EggNOG
Xenopus 10,463	OMA EggNOG
Zebrafish 9,725	Inparanoid OMA

UniProt Keyword (19)

Complete proteome 20,231

Polymorphism 12,194

Reference proteome 20,231

Cell membrane 3,390

Disulfide bond 3,599

G-protein coupled receptor 830

Glycoprotein 4,623

Membrane 7,361

Receptor 1,502

Transducer 887

See all...

GO Function (6)

G-protein coupled serotonin receptor act... 24

neurotransmitter receptor activity 25

serotonin binding 11

GTPase activator activity 281

drug binding 75

G-protein alpha-subunit binding 19

GO Component (6)

cytoplasm 4,094

plasma membrane 4,414

integral component of plasma membrane 1,418

neuron projection 235

cell junction 502

synapse 172

GO Process (38)

G-protein coupled receptor signaling pat... 1,053

positive regulation of cell proliferatio... 470

negative regulation of apoptotic process 479

activation of phospholipase C activity 25

calcium-mediated signaling 49

response to drug 303

phospholipase C-activating G-protein cou... 64

positive regulation of ERK1 and ERK2 cas... 194

positive regulation of MAP kinase activi... 58

positive regulation of I-kappaB kinase-N... 164

See all...

Compartment GO Term (33)

Cation channel complex 231

Cell 16,178

Cell junction 960

Cell part 16,177

Cell periphery 5,382

Cell projection 1,541

Cytoplasm 10,983

Intracellular 14,108

Intracellular membrane-bounded organelle 10,341

Intracellular organelle 12,025

Intracellular organelle lumen 5,090

Intracellular organelle part 8,784

Intracellular part 13,972

Macromolecular complex 5,475

Membrane 8,531

See all...

IMPC Phenotype (3)

preweaning lethality, complete penetranc... 979

increased total body fat amount 134

decreased lean body mass 135

MGI Phenotype (9)

growth-size-body region phenotype 4,157

cellular phenotype 3,637

cardiovascular system phenotype 2,660

reproductive system phenotype 1,999

mortality-aging 5,018

embryo phenotype 1,827

muscle phenotype 1,479

adipose tissue phenotype 992

normal phenotype 1,999

HCA RNA Cell Line (52)

A-431 16,131

A549 15,174

AF22 16,160

AN3-CA 15,648

ASC TERT1 14,842

BEWO 16,726

BJ 15,448

BJ hTERT+ 15,353

BJ hTERT+ SV40 Large T+ 15,609

BJ hTERT+ SV40 Large T+ RasG12V 15,493

See all...

CSPA Cell Line (2)

Melanoma NSph 305

RD 277

Pathway (18)

Serotonergic synapse 114

Neuroactive ligand-receptor interaction 276

Gap junction 90

Inflammatory mediator regulation of TRP ... 99

Calcium signaling pathway 183

http://identifiers.org/panther.pathway/P... 149

http://identifiers.org/panther.pathway/P... 46

Signal Transduction 2,657

Amine ligand-binding receptors 41

Class A/1 (Rhodopsin-like receptors) 322

See all...

PDB (4)

...
More...

Drug (38)

terguride
pKi 8.20

lisuride
pKi 8.49

mianserin
pKi 8.12

methysergide
pKi 9.34

alosetron
pIC50 7.00

guanabenz
pIC50 7.01

doxepin
pIC50 7.05

thioridazine
pKi 7.09

chlorpromazine
pKi 7.10

cisapride
pKi 7.16

raloxifene
pKi 7.16

promethazine
pIC50 7.17

prochlorperazine
pKi 7.19

sorafenib
pKi 7.25

ketotifen
pIC50 7.34

desloratadine
pIC50 7.37

fluphenazine
pIC50 7.41

clemastine
pIC50 7.44

methysergide
pKi 8.12

Lysergide
- 8.43

See all 38 drugs...

Ligand (513)

CHEMBL55472
pKi 7.00

CHEMBL12420
pKi 7.00

CHEMBL432217
pKi 7.00

CHEMBL278685
pKi 7.00

CHEMBL3813796
pIC50 7.00

CHEMBL234738
pKi 7.00

CHEMBL234533
pKi 7.00

CHEMBL1910139
pKi 7.00

CHEMBL2058415
pKi 7.00

CHEMBL293937
pKi 7.00

CHEMBL301409
pKi 7.00

CHEMBL14460
pKi 7.00

CHEMBL14563
pKi 7.00

CHEMBL53152
pKi 7.00

CHEMBL2337106
pEC50 7.00

CHEMBL3770225
pEC50 7.00

CHEMBL3764335
pKi 7.00

CHEMBL262862
pKi 7.00

CHEMBL597002
pKi 7.00

CHEMBL481153
pKi 7.00

See all 513 ligands...

Gene RIF (38)

AA Sequence

MALSYRVSELQSTIPEHILQSTFVHVISSNWSGLQTESIPEEMKQIVEEQGNKLHWAALLILMVIIPTIG      1 - 70
GNTLVILAVSLEKKLQYATNYFLMSLAVADLLVGLFVMPIALLTIMFEAMWPLPLVLCPAWLFLDVLFST     71 - 140
ASIMHLCAISVDRYIAIKKPIQANQYNSRATAFIKITVVWLISIGIAIPVPIKGIETDVDNPNNITCVLT    141 - 210
KERFGDFMLFGSLAAFFTPLAIMIVTYFLTIHALQKKAYLVKNKPPQRLTWLTVSTVFQRDETPCSSPEK    211 - 280
VAMLDGSRKDKALPNSGDETLMRRTSTIGKKSVQTISNEQRASKVLGIVFFLFLLMWCPFFITNITLVLC    281 - 350
DSCNQTTLQMLLEIFVWIGYVSSGVNPLVYTLFNKTFRDAFGRYITCNYRATKSVKTLRKRSSKIYFRNP    351 - 420
MAENSKFFKKHGIRNGINPAMYQSPMRLRSSTIQSSSIILLDTLLLTENEGDKTEEQVSYV             421 - 481
//

Text Mined References (74)

Summary
Details

	PMID	Year	Title

Tclin 5-hydroxytryptamine receptor 2B Add to cart View Collections Empty Collection

Property Summary

Knowledge Summary

Patent (8,933)

TINX Plot

Disease (6)

Expression

Differential Expression (6)

Synonym

Gene

PANTHER Protein Class (2)

Ortholog (14)

UniProt Keyword (19)

GO Function (6)

GO Component (6)

GO Process (38)

Compartment GO Term (33)

IMPC Phenotype (3)

MGI Phenotype (9)

HCA RNA Cell Line (52)

CSPA Cell Line (2)

Pathway (18)

PDB (4)

Drug (38)

Ligand (513)

Gene RIF (38)

AA Sequence

Text Mined References (74)

Tclin 5-hydroxytryptamine receptor 2B

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