Recombinant Human Prostacyclin receptor (PTGIR)

1. these studies are not only the first to identify alpha4 helix of Rab11a as a protein binding domain on the GTPase but also reveal novel mechanistic insights into the intracellular trafficking of the human prostacyclin receptor (hIP), and potentially of other members of the GPCR superfamily, involving Rab11-dependent mechanisms. PMID: 28739266
2. role of IP-PPARdelta signal transduction pathway in the production of sAPPalpha in cerebral microvasculature. PMID: 26661245
3. Data (including data from studies using transgenic mice, an murine experimental model of diabetes, and mouse/human cell lines) suggest prostaglandin I2 receptor (PTGIR) is involved in insulin secretion in pancreatic beta-cells and in permselectivity in glomerular podocytes; the mechanism appears to involve regulation of post-translational phosphorylation of nephrin. PMID: 26868296
4. The human prostacyclin receptor gene is under the transcriptional regulation of dihydrotestosterone, where this regulation is further influenced by serum-cholesterol levels. PMID: 27365208
5. cPGI2 generates via its cognate cell-surface receptor IP-R, converting white adipocytes to brite adipocytes. PMID: 26775637
6. these findings suggest that reduced IPR expression in DM2 platelets may contribute to platelet hyperactivity in humans with type 2 diabetes. PMID: 25617843
7. A total of 38 non-synonymous mutations were identified within the coding region of the hIP receptor, mapping to 36 distinct residues, including several mutations previously reported to affect the signaling of the hIP receptor. PMID: 24886841
8. Prostaglandin I2- Prostaglandin I2 receptor signaling regulates human Th17 and Treg cell differentiation. PMID: 24035274
9. The present report is the first to show an association between the A984C polymorphism of the IP gene and platelet activation in Japanese subjects. PMID: 23628440
10. these data provide critical insights into the transcriptional regulation of the human prostacyclin receptor gene within the vasculature, including during megakaryocytic differentiation PMID: 22381139
11. IP receptor heteridimerization with thromboxane receptor facilitates receptor trafficking to membrane lipid rafts. PMID: 23162015
12. Prostacyclin receptor-dependent inhibition of human erythroleukemia cell differentiation is STAT3-dependent PMID: 22336225
13. IKEPP was also found to be expressed in vascular endothelial cells where it co-localizes and complexes with the hIP PMID: 22884631
14. the IP receptor was expressed in blood vessels of renal cell carcinoma specimens, but not in glomerular vessels of normal renal tissue; findings suggest the IP receptor might maintain an angiogenic switch in the "on" state in tumor endothelial cells (TEC); suggest that the IP receptor is a TEC-specific marker and might be a useful therapeutic target PMID: 22380928
15. VDAC is the ATP conduit in the IP receptor-mediated signaling pathway in human erythrocytes. PMID: 22159995
16. Human prostacyclin receptor interacts with the PDZ adapter protein PDZK1; this interaction plays important role in endothelial cell migration and angiogenesis. PMID: 21653824
17. study identified a novel 8 residue ER export motif within the functionally important alpha-H8 of the hIP. PMID: 21223948
18. decreased maternal plasma levels in severe preeclamptic pregnant women PMID: 20482519
19. of 18 non-synonymous mutations, all with frequencies less than 2% in our study cohort, eight of the 18 had defects in binding, activation, and/or protein stability/folding PMID: 21189259
20. IP(R212C) exerts a dominant action on the wild-type IP and thromboxane receptor through dimerization. This likely contributes to accelerated cardiovascular disease in individuals carrying 1 copy of the variant allele. PMID: 20522800
21. The human IP gene is directly regulated by estrogen that largely occurs through an ERalpha-dependent transcriptional mechanism. PMID: 20070947
22. Impaired receptor binding and activation associated with polymorphism PMID: 11854299
23. role in protein isoprenylation PMID: 11895442
24. Data show that prostacyclin receptor mediated increases in cAMP play a role in enhancing LPS/IFN-gamma-induced iNOS expression in human monocytes/macrophages and may contribute to the increased production of NO during peritonitis. PMID: 12119468
25. identification of a unique ligand-binding pocket by site-directed mutagenesis and molecular modeling PMID: 12446735
26. current state of knowledge of the prostacyclin receptor, its signaling and regulation, and its biological role in vivo [review] PMID: 12481546
27. activation-dependent internalization of this receptor PMID: 12664600
28. the presence of a free heavy chain IgG in the circulation from spinal cord-injured subjects blocked insulin receptor binding sites and also blocked the prostacyclin receptor interaction in platelets; insulin-induced NO synthesis was markedly impaired. PMID: 12850828
29. Iloprost stimulation (1 microM, 2 h) of IP prostanoid receptor expressed in HEK293 cells resulted in specific decrease of endogenous G(s)alpha protein in detergent-insensitive, caveolin-enriched, membrane domains PMID: 15053924
30. elucidated the molecular requirements for receptor activation within the region of the ligand-binding pocket, identifying transmembrane residues affecting potency PMID: 15248755
31. The -CSLC motif of the IP is a direct target for inhibition by the FTI SCH66336, and in the presence of strong farnesyltransferase inhibition, the IP does not undergo compensatory geranylgeranylation. PMID: 15469414
32. prostacyclin and thromboxane receptor dimerization facilitates thromboxane receptor-mediated cAMP generation PMID: 15471868
33. results demonstrate for the first time that prostacyclin receptor activation by cicaprost can lead to STAT1 and STAT3 phosphorylations via signaling pathways involving pertussis toxin-insensitive G proteins, ERK and JNK PMID: 15979846
34. The first intracellular loop of human prostacyclin receptor (IP) was proposed to be involved in signaling via its interaction with the Galphas protein. PMID: 16114876
35. PGI-IP interaction within glandular epithelial cells can promote the expression of proangiogenic genes in human endometrium via cross talk with the EGFR. PMID: 16373414
36. These data suggest that iloprost modulates VSMC phenotype via G(s) activation of the cAMP/PKA pathway. PMID: 16399867
37. AC6 overexpression in endothelial cells may have use as a means to enhance prostacyclin function and reduce endothelial barrier permeability. PMID: 16885208
38. results indicate that the three residues (E392-L394) of the Galphas protein predicted from NMR peptide studies, and the IP iLP1 and iLP3 play important roles in the Galphas-mediated IP receptor signaling in the cells. PMID: 16942748
39. analysis of roles of cysteine residues in human prostacyclin receptor structure and function PMID: 17015447
40. Three Arg-targeted changes at the same 212 position within the third cytoplasmic loop of the human prostacyclin (hIP) receptor were detected. PMID: 17481829
41. The charged residues and the presence of naturally occurring mutations in prostacyclin receptor have important implications in the rational design of prostacyclin agonists for treating cardiovascular disease. PMID: 17704830
42. Prostaglandin I(2) receptor (IP) was more specifically expressed in hair cuticle layer and outer root sheath (ORS) basal layer. PMID: 18005048
43. A profile of the residues in the second extracellular loop that are critical for ligand recognition of human prostacyclin receptor PMID: 18042246
44. IP-receptor agonists may limit the mitogenic actions of thrombin in human SMC by downregulating PAR-1 via modulation of cAMP-/PKA- and Rac1-dependent signaling pathways. PMID: 18162607
45. diminished prostacyclin receptor signaling may contribute, in part, to the underlying adverse cardiovascular outcomes observed with cyclooxygenase-2 inhibition. PMID: 18323528
46. A propensity of enhanced platelet activation in deep vein thrombosis patients with PTGIR polymorphisms V53V/S328S; A dysfunctional PTGIR polymorphism (R212C) associated with intimal hyperplasia. PMID: 18551041
47. Co-stimulation of G(s) and G(q) can result in the fine-tuning of STAT3 activation status, and this may provide the basis for cell type-specific responses following activation of hIP. PMID: 18755267
48. The prostacyclin receptor plays a central role in regulating its recycling following agonist activation by rab11 protein binding domain within its C-tail domain. PMID: 18832025
49. These data provide critical insights into the transcriptional regulation of the IP gene in human megakaryocytic and endothelial cells, identifying Sp1, PU.1 and Oct-1 as the critical factors involved in its basal regulation in humans. PMID: 19118563

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HGNC: 9602

OMIM: 600022

KEGG: hsa:5739

STRING: 9606.ENSP00000291294

UniGene: Hs.458324