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P2Y2 receptor

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https://www.readbyqxmd.com/read/29682007/possible-neuroprotective-role-of-p2x2-in-the-retina-of-diabetic-rats
#1
Jorge E Mancini, Gustavo Ortiz, Constanza Potilinstki, Juan P Salica, Emiliano S Lopez, J Oscar Croxatto, Juan E Gallo
Background: Purinergic receptors are expressed in different tissues including the retina. These receptors are involved in processes like cell growth, proliferation, activation and survival. ATP is the major activator of P2 receptors. In diabetes, there is a constant ATP production and this rise of ATP leads to a persistent activation of purinergic receptors. Antagonists of these receptors are used to evaluate their inhibition effects. Recently, the P2X2 has been reported to have a neuroprotective role...
2018: Diabetology & Metabolic Syndrome
https://www.readbyqxmd.com/read/29681152/highly-selective-and-potent-ecto-nucleotide-pyro%C3%A2-phosphatase-1-npp1-inhibitors-based-on-uridine-5-p%C3%AE-%C3%AE-dithiophosphate-analogues
#2
Vadim Zelikman, Julie Pelletier, Luba Simhaev, Aviad Sela, Fernand-Pierre Gendron, Guillaume Arguin, Hanoch Senderowitz, Jean Sévigny, Bilha Fischer
Ecto-nucleotide pyro¬phosphatase/phosphodiesterase-1 (NPP1) hydrolyzes phospho¬diester bonds of nucleotides such as ATP, resulting mainly in the formation of AMP and pyrophosphate. NPP1 activity plays a deleterious function in calcified aortic valve disease and calcium pyrophosphate deposition disease. Thus, inhibitors of NPP1 represent a medical need. We developed novel NPP1 inhibitors based on uridine 5'-Pα,α-di-thiophosphate analogues, 9-12. All these analogues potently inhibited hNPP1 (80-100% inhibition) at 100 µM, with no, or minimal, inhibition of NPP3 and other ectonucleotidases (NTPDase1,2,3,8)...
April 22, 2018: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29673908/mechanism-underlying-the-contractile-activity-of-utp-in-the-mammalian-heart
#3
Ulrich Gergs, Daniel Rothkirch, Britt Hofmann, Hendrik Treede, Bernard Robaye, Andreas Simm, Christa E Müller, Joachim Neumann
We previously reported that uridine 5'-triphosphate (UTP), a pyrimidine nucleoside triphosphate produced a concentration- and time-dependent increase in the contraction force in isolated right atrial preparations from patients undergoing cardiac bypass surgery due to angina pectoris. The stimulation of the force of contraction was sustained rather than transient. In the present study, we tried to elucidate the underlying receptor and signal transduction for this effect of UTP. Therefore, we measured the effect of UTP on force of contraction, phosphorylation of p38 and ERK1/2, in human atrial preparations, atrial preparations from genetically modified mice, cardiomyocytes from adult mice and cardiomyocytes from neonatal rats...
April 16, 2018: European Journal of Pharmacology
https://www.readbyqxmd.com/read/29660366/tools-and-drugs-for-uracil-nucleotide-activated-p2y-receptors
#4
REVIEW
Muhammad Rafehi, Christa E Müller
P2Y receptors (P2YRs) are a family of G protein-coupled receptors activated by extracellular nucleotides. Physiological P2YR agonists include purine and pyrimidine nucleoside di- and triphosphates, such as ATP, ADP, UTP, UDP, nucleotide sugars, and dinucleotides. Eight subtypes exist, P2Y1 , P2Y2 , P2Y4 , P2Y6 , P2Y11 , P2Y12 , P2Y13 , and P2Y14 , which represent current or potential future drug targets. Here we provide a comprehensive overview of ligands for the subgroup of the P2YR family that is activated by uracil nucleotides: P2Y2 (UTP, also ATP and dinucleotides), P2Y4 (UTP), P2Y6 (UDP), and P2Y14 (UDP, UDP-glucose, UDP-galactose)...
April 13, 2018: Pharmacology & Therapeutics
https://www.readbyqxmd.com/read/29652806/excessive-extracellular-atp-desensitizes-p2y2-and-p2x4-atp-receptors-provoking-surfactant-impairment-ending-in-ventilation-induced-lung-injury
#5
REVIEW
Djo Hasan, Joshua Satalin, Philip van der Zee, Michaela Kollisch-Singule, Paul Blankman, Atsuko Shono, Peter Somhorst, Corstiaan den Uil, Han Meeder, Toru Kotani, Gary F Nieman
Stretching the alveolar epithelial type I (AT I) cells controls the intercellular signaling for the exocytosis of surfactant by the AT II cells through the extracellular release of adenosine triphosphate (ATP) (purinergic signaling). Extracellular ATP is cleared by extracellular ATPases, maintaining its homeostasis and enabling the lung to adapt the exocytosis of surfactant to the demand. Vigorous deformation of the AT I cells by high mechanical power ventilation causes a massive release of extracellular ATP beyond the clearance capacity of the extracellular ATPases...
April 13, 2018: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/29626161/extracellular-atp-activates-hyaluronan-synthase-2-has2-in-epidermal-keratinocytes-via-p2y-2-ca-2-signaling-and-mapk-pathways
#6
Leena Rauhala, Tiina Jokela, Riikka Kärnä, Geneviève Bart, Piia Takabe, Sanna Oikari, Markku I Tammi, Sanna Pasonen-Seppänen, Raija H Tammi
Extracellular nucleotides are used as signaling molecules by several cell types. In epidermis, their release is triggered by insults such as ultraviolet radiation, barrier disruption and wounding and by specific nerve terminals firing. Increased synthesis of hyaluronan, a ubiquitous extracellular matrix glycosaminoglycan, also occurs in response to stress, leading to the attractive hypothesis that nucleotide signaling and hyaluronan synthesis could also be linked. In HaCaT keratinocytes ATP caused a rapid and strong but transient activation of hyaluronan synthase 2 ( HAS2 ) expression via PKC-, CaMKII-, MAPK- and CREB-dependent pathways by activating the purinergic P2Y2 receptor...
April 6, 2018: Biochemical Journal
https://www.readbyqxmd.com/read/29604959/coupling-of-p2y-receptors-to-ca-2-mobilization-in-mesenchymal-stromal-cells-from-the-human-adipose-tissue
#7
Polina D Kotova, Marina F Bystrova, Olga A Rogachevskaja, Alexander A Khokhlov, Veronika Yu Sysoeva, Vsevolod A Tkachuk, Stanislav S Kolesnikov
The purinergic transduction was examined in mesenchymal stromal cells (MSCs) from the human adipose tissue, and several nucleotides, including ATP, UTP, and ADP, were found to mobilize cytosolic Ca2+ . Transcripts for multiple purinoreceptors were detected in MSC preparations, including A1 , A2A , A2B , P2Y1 , P2Y2 , P2Y4 , P2Y6 , P2Y11 , P2Y13 , P2Y14 , P2X2 , P2X4 , and P2X7 . Cellular responses to nucleotides were insignificantly sensitive to bath Ca2+ , pointing at a minor contribution of Ca2+ entry, and were suppressed by U73122 and 2-APB, implicating the phosphoinositide cascade in coupling P2Y receptors to Ca2+ release...
May 2018: Cell Calcium
https://www.readbyqxmd.com/read/29596864/effect-of-low-androgen-status-on-the-expression-of-p2y-receptors-in-the-corpus-cavernosum-of-rats
#8
Pan Liu, Jun Jiang, Jiyi Xia, Rui Jiang
OBJECTIVE: To determine whether low androgen status impacts erectile function by regulating the expression of the G protein-coupled P2Y receptors (P2Y1, P2Y2, P2Y4, and P2Y6) in the corpus cavernosum penis of rats. METHODS: A total of 36 healthy, 8-week-old, male Sprague-Dawley (SD) rats were randomly allocated into 6 groups: 4 weeks of androgen replacement therapy post castration (group A); 4 weeks post castration (group B); 4 weeks post sham operation (group C); 8 weeks of androgen replacement therapy post castration (group D); 8 weeks post castration (group E); and 8 weeks post sham operation (group F)...
March 26, 2018: Urology
https://www.readbyqxmd.com/read/29558126/synthesis-and-evaluation-of-the-first-fluorescent-antagonists-of-the-human-p2y-2-receptor-based-on-ar-c118925
#9
Sean Conroy, Nicholas D Kindon, Jacqueline Glenn, Leigh A Stoddart, Richard James Lewis, Stephen J Hill, Barrie Kellam, Michael John Stocks
The human P2Y2 receptor (hP2Y2R) is a G protein-coupled receptor that shows promise as a therapeutic target for many important conditions including anti-metastatic cancer therapy and more recently for the treatment of idiopathic pulmonary fibrosis. As such, there is a need for new hP2Y2R antagonists and molecular probes to study this receptor. Herein, we report the development of a new series of non-nucleotide hP2Y2R antagonists leading to the discovery of a series of fluorescent ligands containing different linkers and fluorophores based on the known, non-nucleotide hP2Y2R antagonist AR-C118925 (1)...
March 20, 2018: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29541027/p2y-6-receptors-regulate-cxcl10-expression-and-secretion-in-mouse-intestinal-epithelial-cells
#10
Mabrouka Salem, Alain Tremblay, Julie Pelletier, Bernard Robaye, Jean Sévigny
In this study, we investigated the role of extracellular nucleotides in chemokine (KC, MIP-2, MCP-1, and CXCL10) expression and secretion by murine primary intestinal epithelial cells (IECs) with a focus on P2Y6 receptors. qRT-PCR experiments showed that P2Y6 was the dominant nucleotide receptor expressed in mouse IEC. In addition, the P2Y6 ligand UDP induced expression and secretion of CXCL10. For the other studies, we took advantage of mice deficient in P2Y6 ( P2ry6 -/- ). Similar expression levels of P2Y1 , P2Y2 , P2X2, P2X4, and A2A were detected in P2ry6 -/- and WT IEC...
2018: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/29432865/functional-characterization-of-purinergic-p2y-2-and-p2y-12-receptors-involved-in-japanese-flounder-paralichthys-olivaceus-innate-immune-responses
#11
Shuo Li, Gaixiang Hao, Yaqi Xu, Nan Wang, Jiafang Li, Xuyun Geng, Jinsheng Sun
G-protein-coupled P2Y receptors activated by extracellular nucleotides play important roles under different physiological and pathophysiological conditions in mammals. To investigate the immunological relevance of P2Y receptors in fish, we identified and characterized the P2Y2 and P2Y12 receptors in Japanese flounder Paralichthys olivaceus. The P. olivaceus P2Y2 and P2Y12 receptors harbor seven transmembrane domains but share only 24% sequence identity. Real-time PCR analysis revealed the constitutive but unequal mRNA expression pattern of P2Y2 R and P2Y12 R in normal Japanese flounder tissues with the dominant expression of P2Y2 R in head kidney and blood and P2Y12 R in hepatopancreas...
April 2018: Fish & Shellfish Immunology
https://www.readbyqxmd.com/read/29361137/homodimer-formation-by-the-atp-utp-receptor-p2y2-via-disulfide-bridges
#12
Maya Abe, Kanae Watanabe, Yoshiyuki Kuroda, Tetsuto Nakagawa, Hideyoshi Higashi
Many class C GPCRs function as homo- or heterodimers and several class A GPCRs have also been shown to form a homodimer. We expressed human P2Y2 receptor (P2Y2R) in cultured cells and compared SDS-PAGE patterns under reducing and nonreducing conditions. Under nonreducing conditions, approximately half of the P2Y2Rs were electrophoresed as a dimer. We then produced Cys to Ser mutants at four sites (Cys25, Cys106, Cys183, Cys278) in the extracellular domains of P2Y2R and examined the effect on dimer formation and receptor activity...
January 18, 2018: Journal of Biochemistry
https://www.readbyqxmd.com/read/29335300/extracellular-atp-activates-store-operated-ca-2-entry-in-white-adipocytes-functional-evidence-for-stim1-and-orai1
#13
Mickaël F El Hachmane, Anna Ermund, Cecilia Brännmark, Charlotta S Olofsson
In the present study, we have applied ratiometric measurements of intracellular Ca2+ concentrations ([Ca2+ ]i ) to show that extracellularly applied ATP (adenosine triphosphate) (100 µM) stimulates store-operated Ca2+ entry (SOCE) in 3T3-L1 adipocytes. ATP produced a rapid increase in [Ca2+ ]i consisting of an initial transient elevation followed by a sustained elevated phase that could be observed only in the presence of extracellular Ca2+ Gene expression data and [Ca2+ ]i recordings with uridine-5'-triphosphate or with the phospholipase C (PLC) inhibitor U73122 demonstrated the involvement of purinergic P2Y2 receptors and the PLC/inositol trisphosphate pathway...
February 14, 2018: Biochemical Journal
https://www.readbyqxmd.com/read/29297959/p2y-2-r-deletion-ameliorates-sialadenitis-in-il-14%C3%AE-transgenic-mice
#14
L T Woods, J M Camden, M G Khalafalla, M J Petris, L Erb, J L Ambrus, G A Weisman
OBJECTIVE: Interleukin-14α-transgenic (IL-14αTG) mice develop an autoimmune exocrinopathy with characteristics similar to Sjögren's syndrome, including sialadenitis and hyposalivation. The P2Y2 receptor (P2Y2 R) for extracellular ATP and UTP is upregulated during salivary gland inflammation (i.e., sialadenitis) where it regulates numerous inflammatory responses. This study investigated the role of P2Y2 Rs in autoimmune sialadenitis in the IL-14αTG mouse model of Sjögren's syndrome...
January 3, 2018: Oral Diseases
https://www.readbyqxmd.com/read/29279307/intraneural-injection-of-atp-stimulates-regeneration-of-primary-sensory-axons-in-the-spinal-cord
#15
Dongsheng Wu, Sena Lee, Juan Luo, Haijian Xia, Svetlana Gushchina, Peter M Richardson, John Yeh, Ute Krügel, Heike Franke, Yi Zhang, Xuenong Bo
Injury to the peripheral axons of sensory neurons strongly enhances the regeneration of their central axons in the spinal cord. It remains unclear on what molecules that initiate such conditioning effect. Because ATP is released extracellularly by nerve and other tissue injury, we hypothesize that injection of ATP into a peripheral nerve might mimic the stimulatory effect of nerve injury on the regenerative state of the primary sensory neurons. We found that a single injection of 6 μl of 150 μm ATP into female rat sciatic nerve quadrupled the number of axons growing into a lesion epicenter in spinal cord after a concomitant dorsal column transection...
February 7, 2018: Journal of Neuroscience: the Official Journal of the Society for Neuroscience
https://www.readbyqxmd.com/read/29199560/lion-s-mane-medicinal-mushroom-hericium-erinaceus-agaricomycetes-modulates-purinoceptor-coupled-calcium-signaling-and-murine-nociceptive-behavior
#16
Pei-Shan Liu, Sheau-Huei Chueh, Chin-Chu Chen, Li-Ya Lee, Li-Yen Shiu
Hericium erinaceus is well known for the neurotrophic effect it confers by promoting nerve growth factor biosynthesis. We discovered a novel bioactivity of H. erinaceus in its ability to suppress adenosine triphosphate (ATP)-induced calcium signaling in neuronal PC12 cells. ATP, known primarily as a neurotransmitter, also acts on purinoceptors (P2 purinergic receptor [P2R]) to generate the cellular calcium signaling and secretion that mediate P2R physiological manifestations, including pain. Chronic pain reduces quality of life...
2017: International Journal of Medicinal Mushrooms
https://www.readbyqxmd.com/read/29122954/pregnancy-adapted-uterine-artery-endothelial-cell-ca2-signaling-and-its-relationship-with-membrane-potential
#17
Roxanne E Alvarez, Derek S Boeldt, Bikash R Pattnaik, Hannah L Friedman, Ian M Bird
Pregnancy-derived uterine artery endothelial cells (P-UAEC) express P2Y2 receptors and at high cell density show sustained and synchronous [Ca2+]i burst responses in response to ATP Bursts in turn require coupling of transient receptor potential canonical type3 channel (TRPC3) and inositol 1,4,5-triphosphate receptor type 2 (IP3R2), which is upregulated in P-UAEC in a manner dependent on connexin 43 (Cx43) gap junctions. While there is no known direct interaction of TRPC3 with Cx43, early descriptions of TRPC3 function showed it may also be influenced by altered membrane potential ( V m )...
November 2017: Physiological Reports
https://www.readbyqxmd.com/read/29115551/p2y2-receptor-promotes-the-migration-and-invasion-of-breast-cancer-cells-via-emt-related-genes-snail-and-e-cadherin
#18
Ying Qiu, Yan Liu, Wei-Hua Li, Hong-Quan Zhang, Xin-Xia Tian, Wei-Gang Fang
Adenosine 5'-triphosphate (ATP) is one of the most abundant biochemical constituents within the tumor microenvironment and is postulated to play critical roles in the progression of a number of types of tumors via interaction with the P2Y2 receptor. In the present study, we demonstrated that the P2Y2 receptor was highly expressed in MCF7 and Hs578T breast cancer cells. Downregulation of the P2Y2 receptor by small interfering RNA (siRNA) significantly attenuated ATP- or UTP-driven migration and invasion of the breast cancer cells as well as expression of EMT-related genes Snail and E-cadherin...
January 2018: Oncology Reports
https://www.readbyqxmd.com/read/29031899/synapse-formation-in-the-brain-can-be-enhanced-by-co-administering-three-specific-nutrients
#19
Richard J Wurtman
The memory impairments of early Alzheimer's disease [AD] are thought to result from a deficiency in synapses within the hippocampus and related brain regions. This deficiency could result from an acceleration in synapse turnover - perhaps caused by an endogenous neurotoxin like A-beta oligomers - or from a decrease in the production of the synaptic membrane needed to form new synapses. An AD-associated decrease in synaptogenesis almost certainly does occur, inasmuch as major decreases are also observed in the numbers of hippocampal dendritic spines, the immediate cytologic precursor of glutamatergic synapses...
December 15, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28993732/purinergic-signalling-therapeutic-developments
#20
REVIEW
Geoffrey Burnstock
Purinergic signalling, i.e., the role of nucleotides as extracellular signalling molecules, was proposed in 1972. However, this concept was not well accepted until the early 1990's when receptor subtypes for purines and pyrimidines were cloned and characterised, which includes four subtypes of the P1 (adenosine) receptor, seven subtypes of P2X ion channel receptors and 8 subtypes of the P2Y G protein-coupled receptor. Early studies were largely concerned with the physiology, pharmacology and biochemistry of purinergic signalling...
2017: Frontiers in Pharmacology
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