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Ep3 receptor

Timothy D Bryson, Xiaosong Gu, Remonda M Khalil, Safa Khan, Liping Zhu, Jiang Xu, Edward Peterson, Xiao-Ping Yang, Pamela Harding
BACKGROUND: Prostaglandin E2 (PGE2 ) signals through 4 separate G-protein coupled receptor sub-types to elicit a variety of physiologic and pathophysiological effects. We recently reported that PGE2 via its EP3 receptor could reduce cardiac contractility of isolated myocytes and the working heart preparation. We thus hypothesized that there is an imbalance in the EP3/EP4 ratio towards EP3 in the failing heart and that overexpression of EP4 in a mouse model of heart failure would improve cardiac function...
March 6, 2018: Journal of Molecular and Cellular Cardiology
Jing-Yu Xiao, Bing-Rui Xiong, Wen Zhang, Wen-Chang Zhou, Hui Yang, Feng Gao, Hong-Bing Xiang, Anne Manyande, Xue-Bi Tian, Yu-Ke Tian
AIM: Multifactors contribute to the development of postoperative cognitive dysfunction (POCD), of which the most important mechanism is neuroinflammation. Prostaglandin E2 (PGE2) is a key neuroinflammatory molecule and could modulate hippocampal synaptic transmission and plasticity. This study was designed to investigate whether PGE2 and its receptors signaling pathway were involved in the pathophysiology of POCD. METHODS: Sixteen-month old male C57BL/6J mice were exposed to laparotomy...
February 27, 2018: CNS Neuroscience & Therapeutics
Junyan Zhu, Fabian Trillsch, Doris Mayr, Christina Kuhn, Martina Rahmeh, Simone Hofmann, Marianne Vogel, Sven Mahner, Udo Jeschke, Viktoria von Schönfeldt
Background: Prostaglandin E2 (PGE2) receptor 3 (EP3) regulates tumor cell proliferation, migration, and invasion in numerous cancers. The role of EP3 as a prognostic biomarker in endometrial cancer remains unclear. The primary aim of this study was to analyze the prognostic significance of EP3 expression in endometrial cancer. Methods: We analyzed the EP3 expression of 140 endometrial carcinoma patients by immunohistochemistry. RL95-2 endometrial cancer cell line was chosen from four endometrial cancer cell lines (RL95-2, Ishikawa, HEC-1-A, and HEC-1-B) according to EP3 expression level...
January 2, 2018: Oncotarget
Leonard F Lebender, Laura Prünte, Nowshin N Rumzhum, Alaina J Ammit
Arachidonic acid is metabolized by cyclooxygenases (COX-1 and COX-2) into various prostanoids which exert different functions in mammalian physiology. One of these prostanoids, prostaglandin E2 (PGE2 ), interacts with four different G protein-coupled receptors, named EP1 , EP2 , EP3 and EP4 , to initiate different downstream signalling pathways. Prostanoid receptors are diversely expressed throughout different tissues all over the body and PGE2 is responsible for a large variety of beneficial and disadvantageous effects...
January 30, 2018: Pulmonary Pharmacology & Therapeutics
Yan Zhang, Yanfang Liu, Lehao Wu, Chao Fan, Zhiwei Wang, Xiuli Zhang, Amal Alachkar, Xinmiao Liang, Olivier Civelli
Bombesin receptor subtype 3 (BRS-3) is a GPCR that is expressed in the CNS, peripheral tissues, and tumors. Our understanding of BRS-3's role in physiology and pathophysiology is limited because its natural ligand is unknown. In an attempt to identify this ligand, we screened toad skin ( Bufo bufo gargarizans Cantor) extracts and identified prostaglandins as putative ligands. In BRS-3-transfected human embryonic kidney (HEK) cells, we found that prostaglandins, with prostaglandin E2 (PGE2) being the most potent, fulfill the pharmacologic criteria of affinity, selectivity, and specificity to be considered as agonists to the BRS-3 receptor...
January 22, 2018: FASEB Journal: Official Publication of the Federation of American Societies for Experimental Biology
W Ma, B St-Jacques
BACKGROUND: Prostaglandin E2 (PGE2) enriched in inflamed tissues contributes to chronic pain by sensitizing nociceptive dorsal root ganglion (DRG) neurons (nociceptors). Of four PGE2 receptors (EP1-4), EP4 plays a major role in PGE2-induced nociceptor sensitization. We have previously reported that PGE2 or EP4 agonists stimulated EP4 externalization in cultured DRG neurons and this event contributes to nociceptor sensitization. However, the signalling transduction events governing this event remain unknown...
January 16, 2018: European Journal of Pain: EJP
Rania Nasrallah, Joseph Zimpelmann, David Eckert, Jamie Ghossein, Sean Geddes, Jean-Claude Beique, Jean-Francois Thibodeau, Chris R J Kennedy, Kevin D Burns, Richard L Hébert
PGE2 regulates glomerular hemodynamics, renin secretion, and tubular transport. This study examined the contribution of PGE2 EP1 receptors to sodium and water homeostasis. Male EP1-/- mice were bred with hypertensive TTRhRen mice (Htn) to evaluate blood pressure and kidney function at 8 weeks of age in four groups: wildtype (WT), EP1-/-, Htn, HtnEP1-/-. Blood pressure and water balance were unaffected by EP1 deletion. COX1 and mPGE2 synthase were increased and COX2 was decreased in mice lacking EP1, with increases in EP3 and reductions in EP2 and EP4 mRNA throughout the nephron...
December 18, 2017: Laboratory Investigation; a Journal of Technical Methods and Pathology
Akihiro Kinoshita, Masato Higashino, Koji Yoshida, Yoshiyuki Aratani, Akito Kakuuchi, Keisuke Hanada, Hiroyuki Takeda, Atsushi Naganawa, Hidekazu Matsuya, Kazuyuki Ohmoto
A highly potent and well-balanced dual agonist for the EP2 and EP3 receptors is described. Optimization of the lead compound was accomplished in consideration of the relative agonist activity against each EP subtype receptor and the pharmacokinetic profile. As the result, 2-[(2-{(1R,2R)-2-[(1E,4S)-5-cyclopentyl-4-hydroxy-4-methyl-1-penten-1-yl]-5-oxocyclopentyl}eth-yl)thio]-1,3-thiazole-4-carboxylic acid (10) showed excellent potency (human EC50 EP2  = 1.1 nM, EP3  = 1.0 nM) with acceptable selectivity over the EP1 and EP4 subtypes (>2000-fold)...
January 1, 2018: Bioorganic & Medicinal Chemistry
Lu Yang, Yuling Wei, Ying Luo, Qunfang Yang, Huan Li, Congli Hu, Yang Yang, Junqing Yang
To observe the characteristic changes of PGE2 -EPs pathway and divergent functions of PGE2 receptor subtypes on neuronal injury. The primary cultured rat hippocampus neuron injury model was established via aluminum maltolate (100 μM). The aluminum-overload neurons were treated with the agonists of EP1 (17-phenyl trinor Prostaglandin E2 ethyl amide), EP2 (Butaprost), EP3 (Sulprostone) and EP4 (CAY10598) and antagonists of EP1 (SC-19220), EP2 (AH6809) and EP4 (L-161982) at different concentrations, respectively...
November 3, 2017: Oncotarget
Akihito Okazaki, Johsuke Hara, Noriyuki Ohkura, Masaki Fujimura, Tamami Sakai, Miki Abo, Nobuyuki Katayama, Kazuo Kasahara, Shinji Nakao
A feature of cough variant asthma is a heightened cough response to bronchoconstriction. The mediators of this response are unknown. This study was designed to elucidate the role of lipid mediators in bronchoconstriction-triggered cough response in an experimental animal model. We examined the influence of bronchoconstriction on cell components and mediators including prostaglandin E2 (PGE2) in bronchoalveolar lavage fluid (BALF). We studied the cough response to bronchoconstriction (CRB) by measuring the correlation between the increase in enhanced pause (Penh), an index of bronchoconstriction, and cough counts induced by methacholine (Mch) inhalation in conscious guinea pigs...
September 22, 2017: Pulmonary Pharmacology & Therapeutics
Nicolás Salinas-Parra, Cristian Reyes-Martínez, Minolfa C Prieto, Alexis A Gonzalez
BACKGROUND: Prostaglandin E2 (PGE2) regulates renin expression in renal juxtaglomerular cells. PGE2 acts through E-prostanoid (EP) receptors in the renal collecting duct (CD) to regulate sodium and water balance. CD cells express EP1 and EP4, which are linked to protein kinase C (PKC) and PKA downstream pathways, respectively. Previous studies showed that the presence of renin in the CD, and that of PKC and PKA pathways, activate its expression. The (pro)renin receptor (PRR) is also expressed in CD cells, and its activation enhances cyclooxygenase-2 (COX-2) through extracellular signal-regulated kinase (ERK)...
September 2017: American Journal of the Medical Sciences
Ankita Dillipkumar Verma, Manjit Panigrahi, Naseer Ahmad Baba, Sourabh Sulabh, Abdul Sadam, Subhashree Parida, Krishnaswamy Narayanan, Arvind A Sonwane, Bharat Bhushan
Prostaglandins (PGs) are the key mediators of several female reproductive functions, including luteolysis, ovulation, fertilization, implantation, pregnancy, and parturition. The present study was conducted in buffalo endometrial and luteal tissues between nonpregnant and two stages of pregnancy (29-38 days of pregnancy, 48-56 days of pregnancy) tissue samples. The genes involved from synthesis upto receptor level effect of PGs (PGF2α and PGE2) were studied for their relative mRNA expression. We have collected the endometrial and luteal tissues from slaughtered animals and confirmed the stages by external examination and crown vertebral rump length measurement of the foetus...
January 1, 2018: Theriogenology
Sujie Wang, Li Xie, Yanfei Zhang, Pengfei Xu, Aiguo Liu
Objectives.: To investigate the expression of prostaglandin E2 receptor subtypes, E-prostanoid (EP) 1-4 receptors, in acquired cholesteatoma and its possible role in the pathologic process of this disorder. Methods.: Specimens of human acquired cholesteatoma were obtained from 29 patients and 19 skin biopsies of normal external auditory canal were as controls. The mRNA and protein expression of EP receptors was assessed by quantitative real-time polymerase chain reaction, immunohistochemistry and Western blot...
August 26, 2017: Clinical and Experimental Otorhinolaryngology
Bin Liu, Mengyi Zhan, Yingzhan Zhang, Hui Li, Xiangzhong Wu, Fengfeng Zhuang, Wenhong Luo, Yingbi Zhou
This study aimed to determine whether E prostanoid receptor-3 (EP3) is involved in prostacyclin (PGI2 )-evoked vasoconstrictor activity of resistance arteries and if so, how it changes under hypertensive conditions. Mesenteric resistance arteries from Wistar-Kyoto rats (WKYs) and spontaneously hypertensive rats (SHRs) were isolated for functional and biochemical studies. Here we show that in vessels from WKYs, PGI2 or the endothelial muscarinic agonist ACh (which stimulates in vitro PGI2 synthesis) evoked vasoconstrictor activity, which increased in SHRs...
August 21, 2017: Scientific Reports
H Ota, K Katanosaka, S Murase, T Furuyashiki, S Narumiya, K Mizumura
We previously demonstrated that nerve growth factor (NGF) and glial cell line-derived neurotrophic factor (GDNF) were upregulated after lengthening contractions (LC) in exercised muscle through B2 bradykinin receptor activation and cyclooxygenase (COX)-2 upregulation, respectively, and that these trophic factors sensitized nociceptors resulting in mechanical hyperalgesia (delayed-onset muscle soreness, DOMS). Here, we examined the prostaglandin receptor subtype involved in DOMS. The mechanical withdrawal threshold of the exercised muscle was measured before and after LC in rats administered prostaglandin E2 receptor (EP) antagonists before LC, or in wild-type (WT), EP2 knockout (EP2(-/-) ), and IP knockout (IP(-/-) ) mice...
July 31, 2017: Scandinavian Journal of Medicine & Science in Sports
Helene Heidegger, Sebastian Dietlmeier, Yao Ye, Christina Kuhn, Aurelia Vattai, Caroline Aberl, Udo Jeschke, Sven Mahner, Bernd Kost
We know that one of the main risk factors for cervical cancer is an infection with high-risk human papillomavirus (HR-HPV). Prostaglandins and their receptors are very important for the tumour growth and tumour-associated angiogenesis. Little is known about the expression of the Prostaglandin E receptor type 3 (EP3) or the Prostaglandin (PG)E₂-EP3 signalling in cervical cancer, so the aim of the study was to analyse the expression of the EP3 receptor in cervical cancer and find prognostic factors in relation to survival; EP3 immunohistological staining of 250 cervical cancer slides was performed and analysed with a semi-quantitative score...
July 19, 2017: International Journal of Molecular Sciences
Chenggang Li, Xiaolei Liu, Yang Liu, Erik Zhang, Kantha Medepalli, Kouhei Masuda, Na Li, Kathryn A Wikenheiser-Brokamp, Andrew Osterburg, Michael T Borchers, Elizabeth J Kopras, David R Plas, Julia Sun, David N Franz, Jamie K Capal, Maxwell Mays, Yang Sun, David J Kwiatkowski, Anya Alayev, Marina K Holz, Darcy A Krueger, Brian J Siroky, Jane J Yu
Tuberous sclerosis complex (TSC) is a tumor-suppressor syndrome affecting multiple organs, including the brain, skin, kidneys, heart, and lungs. TSC is associated with mutations in TSC1 or TSC2, resulting in hyperactivation of mTOR complex 1 (mTORC1). Clinical trials demonstrate that mTORC1 inhibitors decrease tumor volume and stabilize lung function in TSC patients; however, mTOR inhibitors are cytostatic not cytocidal, and long-term benefits and toxicities are uncertain. Previously, we identified rapamycin-insensitive upregulation of cyclooxygenase 2 (PTGS2/COX2) and prostaglandin E2 (PGE2) production in TSC2-deficient cells and postulated that the action of excess PGE2 and its cognate receptors (EP) contributes to cell survival...
October 2017: Molecular Cancer Research: MCR
Alexis A Gonzalez, Nicolas Salinas-Parra, Dan Leach, L Gabriel Navar, Minolfa C Prieto
During the early phase of ANG II-dependent hypertension, tubular PGE2 is increased. Renin synthesis and secretion in the collecting duct (CD) are upregulated by ANG II, contributing to further intratubular ANG II formation. However, what happens first and whether the triggering mechanism is independent of tubular ANG II remain unknown. PGE2 stimulates renin synthesis in juxtaglomerular cells via E-prostanoid (EP) receptors through the cAMP/cAMP-responsive element-binding (CREB) pathway. EP receptors are also expressed in the CD...
October 1, 2017: American Journal of Physiology. Renal Physiology
Yu Yu, Qian Liu, Shumin Guo, Qianqian Zhang, Juan Tang, Guizhu Liu, Deping Kong, Juanjuan Li, Shuai Yan, Ruiguo Wang, Peilong Wang, Xiaoou Su, Ying Yu
Endothelial injury or dysfunction is an early event in the pathogenesis of atherosclerosis. Epidemiological and animal studies have shown that 2, 3, 7, 8-tetrachlorodibenzo-p-dioxin (TCDD) exposure increases morbidity and mortality from chronic cardiovascular diseases, including atherosclerosis. However, whether or how TCDD exposure causes endothelial injury or dysfunction remains largely unknown. Cultured human umbilical vein endothelial cells (HUVECs) were exposed to different doses of TCDD, and cell apoptosis was examined...
December 2017: Journal of Cellular and Molecular Medicine
Erdem Dinç, Özer Dursun, Banu Yılmaz, Mustafa Vatansever, A Ayça Sarı, Özlem Yıldırım, Ufuk Adıgüzel
PURPOSE: In the present study, we aimed to evaluate the expression of EP receptors in primary and recurrent human pterygium tissues. METHODS: Pterygium samples were collected from 65 patients with primary pterygium and 16 patients with recurrent pterygium. Normal conjunctival tissues were collected from nasal interpalpebral area from 17 patients without systemic and any other ocular pathology. Expression of EP receptors was evaluated by immunohistochemistry. The median value for each receptor staining score (RSS) was determined in normal conjunctival specimens...
July 10, 2017: International Ophthalmology
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