- 関
- epoprostenol receptor、PGI2 receptor、prostaglandin I2 receptor
WordNet
- a cellular structure that is postulated to exist in order to mediate between a chemical agent that acts on nervous tissue and the physiological response
PrepTutorEJDIC
- =sense organ / 受信装置
Wikipedia preview
出典(authority):フリー百科事典『ウィキペディア(Wikipedia)』「2016/01/10 15:17:16」(JST)
[Wiki en表示]
Prostaglandin I2 (prostacyclin) receptor (IP) |
Identifiers |
Symbols |
PTGIR ; IP; PRIPR |
External IDs |
OMIM: 600022 MGI: 99535 HomoloGene: 7496 IUPHAR: 345 ChEMBL: 1995 GeneCards: PTGIR Gene |
Gene ontology |
Molecular function |
• G-protein coupled receptor activity
• guanyl-nucleotide exchange factor activity
|
Cellular component |
• cytosol
• plasma membrane
• integral component of plasma membrane
|
Biological process |
• G-protein coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger
• adenylate cyclase-activating G-protein coupled receptor signaling pathway
• cell-cell signaling
• blood coagulation
• negative regulation of platelet-derived growth factor receptor signaling pathway
• positive regulation of cAMP biosynthetic process
• response to lipopolysaccharide
• positive regulation of GTPase activity
• positive regulation of cAMP-mediated signaling
• negative regulation of smooth muscle cell proliferation
|
Sources: Amigo / QuickGO |
|
RNA expression pattern |
|
More reference expression data |
Orthologs |
Species |
Human |
Mouse |
Entrez |
5739 |
19222 |
Ensembl |
ENSG00000160013 |
ENSMUSG00000043017 |
UniProt |
P43119 |
P43252 |
RefSeq (mRNA) |
NM_000960 |
NM_008967 |
RefSeq (protein) |
NP_000951 |
NP_032993 |
Location (UCSC) |
Chr 19:
46.62 – 46.63 Mb |
Chr 7:
16.91 – 16.91 Mb |
PubMed search |
[1] |
[2] |
|
Prostacyclin receptor ( or prostaglandin I2 receptor, IP1) is a receptor for prostacyclin, encoded by the PTGIR gene.
It is a member of the G-protein coupled receptor family. Prostacyclin, the major product of cyclooxygenase in macrovascular endothelium, elicits a potent vasodilation and inhibition of platelet aggregation through binding to this receptor.[1]
There are actually two receptors for prostacyclin, the other being IP2.[citation needed]
Contents
- 1 Transduction
- 2 Gene
- 3 See also
- 4 References
- 5 External links
- 6 Further reading
Transduction
When binding a prostacyclin-molecule, the receptor changes conformation and activates Gs, with its activation of cAMP and increase in protein kinase A (PKA) activity.
In vasodilation
In vasodilation, the PKA activity causes phosphorylation of MLCK, decreasing its activity, resulting in dephosphorylation of MLC of myosin. The smooth muscle relaxation leads to vasodilation.[2]
Gene
The receptor is encoded by the human gene PTGIR.[1]
See also
References
- ^ a b "Entrez Gene: PTGIR prostaglandin I2 (prostacyclin) receptor (IP)".
- ^ Walter F., PhD. Boron (2005). Medical Physiology: A Cellular And Molecular Approaoch. Elsevier/Saunders. ISBN 1-4160-2328-3. Page 479
External links
- "Prostanoid Receptors: IP1". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology.
Further reading
- Coleman RA, Smith WL, Narumiya S (1994). "International Union of Pharmacology classification of prostanoid receptors: properties, distribution, and structure of the receptors and their subtypes". Pharmacol. Rev. 46 (2): 205–29. PMID 7938166.
- Rauvala H, Peng HB (1997). "HB-GAM (heparin-binding growth-associated molecule) and heparin-type glycans in the development and plasticity of neuron-target contacts". Prog. Neurobiol. 52 (2): 127–44. doi:10.1016/S0301-0082(97)00007-5. PMID 9185236.
- Smyth EM, FitzGerald GA (2003). "Human prostacyclin receptor". Vitam. Horm. Vitamins & Hormones 65: 149–65. doi:10.1016/S0083-6729(02)65063-0. ISBN 978-0-12-709865-4. PMID 12481546.
- Boie Y, Rushmore TH, Darmon-Goodwin A, et al. (1994). "Cloning and expression of a cDNA for the human prostanoid IP receptor". J. Biol. Chem. 269 (16): 12173–8. PMID 7512962.
- Katsuyama M, Sugimoto Y, Namba T, et al. (1994). "Cloning and expression of a cDNA for the human prostacyclin receptor". FEBS Lett. 344 (1): 74–8. doi:10.1016/0014-5793(94)00355-6. PMID 7514139.
- Ogawa Y, Tanaka I, Inoue M, et al. (1995). "Structural organization and chromosomal assignment of the human prostacyclin receptor gene". Genomics 27 (1): 142–8. doi:10.1006/geno.1995.1016. PMID 7665161.
- Duncan AM, Anderson LL, Funk CD, et al. (1995). "Chromosomal localization of the human prostanoid receptor gene family". Genomics 25 (3): 740–2. doi:10.1016/0888-7543(95)80022-E. PMID 7759114.
- Nakagawa O, Tanaka I, Usui T, et al. (1994). "Molecular cloning of human prostacyclin receptor cDNA and its gene expression in the cardiovascular system". Circulation 90 (4): 1643–7. doi:10.1161/01.cir.90.4.1643. PMID 7923647.
- Bonaldo MF, Lennon G, Soares MB (1997). "Normalization and subtraction: two approaches to facilitate gene discovery". Genome Res. 6 (9): 791–806. doi:10.1101/gr.6.9.791. PMID 8889548.
- Sasaki Y, Takahashi T, Tanaka I, et al. (1997). "Expression of prostacyclin receptor in human megakaryocytes". Blood 90 (3): 1039–46. PMID 9242534.
- Fisch A, Tobusch K, Veit K, et al. (1997). "Prostacyclin receptor desensitization is a reversible phenomenon in human platelets". Circulation 96 (3): 756–60. doi:10.1161/01.cir.96.3.756. PMID 9264479.
- Smyth EM, Li WH, FitzGerald GA (1998). "Phosphorylation of the prostacyclin receptor during homologous desensitization. A critical role for protein kinase c". J. Biol. Chem. 273 (36): 23258–66. doi:10.1074/jbc.273.36.23258. PMID 9722557.
- Kömhoff M, Lesener B, Nakao K, et al. (1999). "Localization of the prostacyclin receptor in human kidney". Kidney Int. 54 (6): 1899–908. doi:10.1046/j.1523-1755.1998.00213.x. PMID 9853255.
- Hayes JS, Lawler OA, Walsh MT, Kinsella BT (1999). "The prostacyclin receptor is isoprenylated. Isoprenylation is required for efficient receptor-effector coupling". J. Biol. Chem. 274 (34): 23707–18. doi:10.1074/jbc.274.34.23707. PMID 10446129.
- Smyth EM, Austin SC, Reilly MP, FitzGerald GA (2000). "Internalization and sequestration of the human prostacyclin receptor". J. Biol. Chem. 275 (41): 32037–45. doi:10.1074/jbc.M003873200. PMID 10889200.
- Lawler OA, Miggin SM, Kinsella BT (2001). "Protein kinase A-mediated phosphorylation of serine 357 of the mouse prostacyclin receptor regulates its coupling to G(s)-, to G(i)-, and to G(q)-coupled effector signaling". J. Biol. Chem. 276 (36): 33596–607. doi:10.1074/jbc.M104434200. PMID 11443126.
- Zhang Z, Austin SC, Smyth EM (2001). "Glycosylation of the human prostacyclin receptor: role in ligand binding and signal transduction". Mol. Pharmacol. 60 (3): 480–7. PMID 11502878.
- Fortier I, Patry C, Lora M, et al. (2001). "Immunohistochemical localization of the prostacyclin receptor (IP) human bone". Prostaglandins Leukot. Essent. Fatty Acids 65 (2): 79–83. doi:10.1054/plef.2001.0292. PMID 11545623.
This article incorporates text from the United States National Library of Medicine, which is in the public domain.
Prostanoid signaling
|
|
Receptor
(ligands) |
|
|
Enzyme
(inhibitors) |
Cyclooxygenase |
|
|
PGD2 synthase |
- Retinoids
- Selenium (selenium tetrachloride, sodium selenite, selenium disulfide)
|
|
PGE synthase |
HQL-79
|
|
PGF synthase |
Bimatoprost
|
|
PGI2 synthase |
Tranylcypromine
|
|
TXA synthase |
- Camonagrel
- Dazmegrel
- Dazoxiben
- Furegrelate
- Isbogrel
- Midazogrel
- Nafagrel
- Nicogrelate
- Ozagrel
- Picotamide
- Pirmagrel
- Ridogrel
- Rolafagrel
- Samixogrel
- Terbogrel
- U63557A
|
|
|
Others |
- Precursors: Linoleic acid
- γ-Linolenic acid (gamolenic acid)
- Dihomo-γ-linolenic acid
- Diacylglycerol
- Arachidonic acid
- Prostaglandin G2
- Prostaglandin H2
|
|
See also: Leukotrienergics
|
|
UpToDate Contents
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English Journal
- Toll-like receptor 4 contributes to blood pressure regulation and vascular contraction in spontaneously hypertensive rats.
- Bomfim GF, Dos Santos RA, Oliveira MA, Giachini FR, Akamine EH, Tostes RC, Fortes ZB, Webb RC, Carvalho MH.SourceDepartment of Pharmacology, University of Sao Paulo, Sao Paulo, SP, Brazil. gifacholi@yahoo.com.br
- Clinical science (London, England : 1979).Clin Sci (Lond).2012 Jun;122(11):535-43.
- Activation of TLRs (Toll-like receptors) induces gene expression of proteins involved in the immune system response. TLR4 has been implicated in the development and progression of CVDs (cardio-vascular diseases). Innate and adaptive immunity contribute to hypertension-associated end-organ damage, al
- PMID 22233532
- Regulation of the human prostacyclin receptor gene in megakaryocytes: Major roles for C/EBPδ and PU.1.
- Keating GL, Turner EC, Kinsella BT.AbstractThe prostanoid prostacyclin plays a central role in haemostasis and vascular repair. Recent studies investigating the regulation of the human prostacyclin receptor (hIP) gene identified an upstream repressor region (URR) within its regulatory promoter, herein termed the PrmIP. This study aimed to identify the main trans-acting factors that bind within the URR to transcriptionally repress PrmIP-directed gene expression in the megakaryoblastic human erythroleukemia (HEL) 92.1.7 cell line. Of the putative cis-acting elements examined, disruption of C/EBP and PU.1 elements within the URR substantially increased PrmIP-directed gene expression. Chromatin immunoprecipitation (ChIP) confirmed that C/EBPδ and PU.1, but not C/EBPβ, bind to the URR in vivo, while ectopic expression of C/EBPδ substantially reduced hIP mRNA levels and PrmIP-directed gene expression. Phorbol 12-myristate 13-acetate (PMA)-induced megakaryocytic differentiation increased hIP mRNA and PrmIP-directed reporter gene expression and hIP-mediated cAMP generation in HEL cells. Two PMA-responsive regions, termed PRR1 and PRR2, were identified within PrmIP. Disruption of C/EBPδ and PU.1 cis-elements within the overlapping PRR1/URR and of Sp1, PU.1 and Oct-1 cis-elements within the overlapping PRR2/core PrmIP, revealed that both PRR1 and PRR2 contribute to the PMA- induction of hIP mRNA and gene expression in HEL cells. Furthermore, ChIP analysis established that induction of PrmIP-directed gene expression during megakaryocytic differentiation is largely regulated by PMA-induced dissociation of C/EBPδ and enhanced binding of PU.1 to PRR1 in addition to increased binding of Sp1, PU.1 and Oct-1 to elements within the core promoter/PRR2 in vivo. Taken together, these data provide critical insights into the transcriptional regulation of the hIP gene within the vasculature, including during megakaryocytic differentiation.
- Biochimica et biophysica acta.Biochim Biophys Acta.2012 May;1819(5):428-45. Epub 2012 Feb 23.
- The prostanoid prostacyclin plays a central role in haemostasis and vascular repair. Recent studies investigating the regulation of the human prostacyclin receptor (hIP) gene identified an upstream repressor region (URR) within its regulatory promoter, herein termed the PrmIP. This study aimed to id
- PMID 22381139
Japanese Journal
- A New Era in Medical Management of Severe Pediatric Pulmonary Arterial Hypertension
- LVY Dunbar,SAJI Ben T
- 日本小児循環器学会雑誌 = Acta cardiologica paediatrica Japonica 26(3), 206-218, 2010-05-01
- NAID 10026282365
- Autoimmune Thyroid Disease in Children and Adolescents With Idiopathic Pulmonary Arterial Hypertension
- SATOH Mari,ASO Keiko,NAKAYAMA Tomotaka,NAOI Kazuyuki,IKEHARA Satoshi,UCHINO Yumiko,SHIMADA Hiromitsu,TAKATSUKI Shinichi,MATSUURA Hiroyuki,SAJI Tsutomu
- Circulation journal : official journal of the Japanese Circulation Society 74(2), 371-374, 2010-01-25
- … The duration after PAH onset and the prostacyclin (PGI2) treatment period were significantly longer in patients with AITD (7.6±2.1 and 7.4±2.3 years, respectively) than in patients without AITD (5.0±1.1 and 4.8±1.2 years, respectively; …
- NAID 10025942805
Related Links
- Prostacyclin receptor ( or prostaglandin I2 receptor, IP1) is a receptor for prostacyclin. It is a member of the G-protein coupled receptor family. Prostacyclin, the major product of cyclooxygenase in macrovascular endothelium, elicits a potent ...
★リンクテーブル★
[★]
- 関
- epoprostenol receptor、prostacyclin receptor、prostaglandin I2 receptor
[★]
- 関
- epoprostenol receptor、PGI2 receptor、prostacyclin receptor
[★]
- 英
- prostacyclin receptor
- 関
- エポプロステノール受容体、プロスタサイクリンレセプター、プロスタグランジンI2受容体
[★]
- 関
- PGI2 receptor、prostacyclin receptor、prostaglandin I2 receptor
[★]
- 英
- prostacyclin receptor
- 関
- プロスタサイクリン受容体
[★]
プロスタグランジンI2 PC