Abstract：
:The interaction of cell surface hormone receptors with heterotrimeric G proteins is crucial for hormonal actions. The domains of the receptor, which interact with and activate G protein, have been extensively studied. However, precise molecular mechanisms underlying regulation of the receptor-induced G protein activation are still poorly understood. Prostaglandin E(2) (PGE(2)) receptors comprise of four subtypes, EP1, EP2, EP3 and EP4. Among them, EP2 and EP4 couple to Gs and EP3 to Gi. To assess the functional domains essential for Gs activation in prostanoid receptors, EP2, EP3beta and each intracellular loop- (IC-) interchanged EP2/EP3 chimeras were tested for agonist binding and functional responses. In EP2 receptor, substitution of IC1 or IC3 resulted in loss of binding activity, while substitution of IC2, N- (IC2N) or C-terminal half region of IC2 (IC2C) had no effects on the binding activity. Wild-type EP2 and IC2C-substituted EP2 showed agonist-induced Gs activity, but IC2- and IC2N-substituted EP2 failed to elicit Gs activity upon agonist stimulation. On the other hand, in EP3 receptor substitution of IC1 resulted in loss of PGE(2) binding, while substitution of IC2, IC3, IC2N or IC2C had no effects on binding activity. Wild-type EP3beta, IC3- or IC2C-substituted EP3 failed to show Gs activity upon agonist stimulation, but IC2- or IC2N-substituted EP3 chimera showed agonist-dependent Gs activity. These results indicated that the second intracellular loop of the EP2 plays an essential role in activation of Gs.
journal_name
Life Scijournal_title
Life sciencesauthors
Sugimoto Y,Nakato T,Kita A,Hatae N,Tabata H,Tanaka S,Ichikawa Adoi
10.1016/j.lfs.2003.09.002subject
Has Abstractpub_date
2003-12-05 00:00:00pages
135-41issue
2-3eissn
0024-3205issn
1879-0631pii
S0024320503008191journal_volume
74pub_type
杂志文章相关文献
LIFE SCIENCES文献大全abstract：:Decreased heart rate variability (HRV) and heart rate turbulence (HRT) are independent predictors of mortality after acute myocardial infarction (AMI). There are no previous studies on the relationship between warm-up phenomenon and cardiac autonomic control in stable coronary artery disease (CAD). We investigated the...
journal_title：Life sciences
pub_type： 临床试验,杂志文章
doi：10.1016/j.lfs.2004.06.033
更新日期：2005-03-25 00:00:00
abstract：:The relative affinities of nortriptyline (NT) and its 10-hydroxymetabolites to rat brain muscarinic acetylcholine receptors have been determined by competition with 3H-quinuclidinyl benzilate binding. It is shown that the major NT metabolite, E-10-OH-NT, has only 1/18 the affinity of NT for the muscarinic receptor. Si...
journal_title：Life sciences
pub_type： 杂志文章
doi：10.1016/0024-3205(84)90395-3
更新日期：1984-09-24 00:00:00
abstract：:Catalase, glutathione peroxidase and superoxide dismutase enzymes were determined after administering dexamethasone. Catalase increased its activity over six times (0.388 U/mg DNA) the normal rate, while glutathione peroxidase caused 3 times an increase one hour after dexamethasone injection. Superoxide dismutase incr...
journal_title：Life sciences
pub_type： 杂志文章
doi：10.1016/s0024-3205(97)00193-8
更新日期：1997-01-01 00:00:00
abstract：:This experiment was designed to assess the role of the septo-hippocampal cholinergic (ACh) system in the deleterious effects produced by systemic benzodiazepine injection on learning processes in rats. Retention of a step through passive avoidance task was analysed after systemic injection of increasing doses of eithe...
journal_title：Life sciences
pub_type： 杂志文章
doi：10.1016/s0024-3205(99)00092-2
更新日期：1999-01-01 00:00:00
abstract：:Certain pharmacological properties of methyl beta-carboline-3-carboxylate (beta-CCM), a benzodiazepine receptor ligand, have been investigated in chicks. Although beta-CCM has been established previously as an "inverse agonist" of benzodiazepine receptors in rodents, having effects opposite to those of benzodiazepines...
journal_title：Life sciences
pub_type： 杂志文章
doi：10.1016/0024-3205(86)90201-8
更新日期：1986-09-22 00:00:00
abstract：:The aim of the present study was to determine the role of adrenals in gonadal activity in the male toad during the breeding season. Exogenous administration of corticosterone or metapyrone for 6 days inhibited adrenal delta5-3beta(delta 5-3 beta) hydroxysteroid (delta5-3beta-HSD) and testicular 17beta (17 beta) hydrox...
journal_title：Life sciences
pub_type： 杂志文章
doi：10.1016/s0024-3205(00)00433-1
更新日期：2000-02-18 00:00:00
abstract：:In the course of investigating the binding of imipramine to soluble cellular fractions from brain and leukocytes using equilibrium dialysis, an artifactual binding component was produced. On Scatchard and double-reciprocal plots of the data, the component appeared as a homogenous population of sites displaying a bindi...
journal_title：Life sciences
pub_type： 杂志文章
doi：10.1016/0024-3205(83)90405-8
更新日期：1983-07-11 00:00:00
abstract：:The patterns of prolactin release after bilateral ECT and after 0.4 mg TRH i.v. were studied in 11 female melancholic patients in a 5-min sampling protocol. Mean prolactin peaking times were 10.2 min after ECT and 20.5 min after TRH. The elimination rate coefficients were significantly lower--and the corresponding hal...
journal_title：Life sciences
pub_type： 杂志文章
doi：10.1016/0024-3205(87)90206-2
更新日期：1987-09-07 00:00:00
abstract：:Secreted frizzled-related protein 5 (Sfrp5) primarily acts in combination with wingless-type family member 5a (Wnt5a), to inhibits chronic inflammation and repress atherosclerosis and other metabolic disorders. Epicardial adipose tissue (EAT), surrounding the heart and coronary arteries, has been found to be highly re...
journal_title：Life sciences
pub_type： 杂志文章
doi：10.1016/j.lfs.2020.117338
更新日期：2020-03-15 00:00:00
abstract：:Free radicals induced by cerebral ischemia-reperfusion injury can trigger lipid peroxidation, leading to the production of malondialdehyde (MDA) and 4-hydroxy-2(E)-nonenal (4-HNE). Post-ischemia electroacupuncture (EA) therapy was able to reduce extent of lipid peroxidation. However, the effect of pre-ischemic EA ther...
journal_title：Life sciences
pub_type： 杂志文章
doi：10.1016/j.lfs.2004.02.025
更新日期：2004-07-30 00:00:00
abstract：:In this study, we evaluated whether butein can inhibit the effects of tumor necrosis factor alpha (TNF-alpha), an inflammatory mediator, in intestinal epithelial HT-29 cells. Butein significantly inhibited TNF-alpha-induced interleukin 8 (IL-8) secretion and mRNA expression. Moreover, butein suppressed the expression ...
journal_title：Life sciences
pub_type： 杂志文章
doi：10.1016/j.lfs.2007.09.024
更新日期：2007-11-10 00:00:00
abstract：:We studied effects of tyrphostin A23 (an inhibitor of protein tyrosine kinase; PTK) and tyrphostin A63 (an inactive analog of tyrphostin A23) on forskolin-activated cystic fibrosis transmembrane conductance regulator (CFTR) Cl(-) channels and Cl(-) secretion in renal epithelial A6 cells. Tyrphostin A23 and A63 had no ...
journal_title：Life sciences
pub_type： 杂志文章
doi：10.1016/s0024-3205(02)01824-6
更新日期：2002-07-26 00:00:00
abstract：:Dietary guidelines published in the past two decades have acknowledged the beneficial effects of myricetin, an important and common type of herbal flavonoid, against several human diseases such as inflammation, cardiovascular pathologies, and cancer. An increasing number of studies have shown the beneficial effects of...
journal_title：Life sciences
pub_type： 杂志文章,评审
doi：10.1016/j.lfs.2015.10.004
更新日期：2015-12-01 00:00:00
abstract：:The effects of erythropoietin (EPO) on cytosolic free calcium concentration ([Ca2+]i) in platelets of 20 essential hypertensive patients (HT) and of 25 normotensive subjects (NT) were investigated using the fura2 technique. In resting platelets [Ca2+]i were not significantly higher in HT compared to NT (74.3 +/- 7.8 n...
journal_title：Life sciences
pub_type： 杂志文章
doi：10.1016/0024-3205(92)90010-m
更新日期：1992-01-01 00:00:00
abstract：:Ovine fetal renal responses to ANF decrease during the last third of gestation, although circulating fetal plasma atrial natriuretic factor (ANF) levels are higher than in the maternal circulation, and do not change with gestation. This study examined whether previously reported maturational changes in fetal renal res...
journal_title：Life sciences
pub_type： 杂志文章
doi：10.1016/0024-3205(94)00420-x
更新日期：1994-01-01 00:00:00
abstract：:Quetiapine, a new atypical antipsychotic drug, has beneficial effects on cognitive impairment and neuropathological changes in treating chronic neurodegenerative diseases. Our previous studies have demonstrated that quetiapine may have neuroprotective properties. In the present study, we investigated the effects of a ...
journal_title：Life sciences
pub_type： 杂志文章
doi：10.1016/j.lfs.2007.05.020
更新日期：2007-07-12 00:00:00
abstract：:The effect of thapsigargin, a specific inhibitor of intracellular Ca(2+)-ATPases, on endothelium-dependent relaxation was studied in the guinea pig thoracic aorta. Thapsigargin (1 nM-1 microM) produced a concentration-dependent relaxation of aortic strips precontracted by phenylephrine (0.1 microM) in the presence and...
journal_title：Life sciences
pub_type： 杂志文章
doi：10.1016/0024-3205(93)90244-w
更新日期：1993-01-01 00:00:00
abstract：:Increase of intracellular reactive oxygen species (ROS) has been proposed to cause endothelial injury, and oxidized LDL (oxLDL) actions are associated with an early increase of ROS. Estrogen protects vascular cells partly via its antioxidant effects and by preventing lipid peroxidation. However, whether it can inhibit...
journal_title：Life sciences
pub_type： 杂志文章
doi：10.1016/s0024-3205(01)01486-2
更新日期：2001-12-14 00:00:00
abstract：AIMS:Smooth muscle cells (SMCs) play a role in medial vascular calcification, which can be stimulated by high levels of serum phosphate and inflammatory mediators. The aim of this study was to investigate whether mitogen-activated protein kinases (MAPKs) (p38 MAPK, ERK1/2, and JNK) and protein kinase A (PKA) can partic...
journal_title：Life sciences
pub_type： 杂志文章
doi：10.1016/j.lfs.2018.08.051
更新日期：2018-09-15 00:00:00
abstract：:The temporal relationship of changes in cAMP and cGMP to oocyte maturation was examined in proestrous hamsters (day 4). The first series of experiments showed, in normal cycling hamsters, an increase in cAMP and a decrease in cGMP at 1400 h shortly after the rise in LH with oocyte maturation beginning at 1800 h. When ...
journal_title：Life sciences
pub_type： 杂志文章
doi：10.1016/0024-3205(83)90726-9
更新日期：1983-10-24 00:00:00
abstract：:This study is aimed to investigate the effect of the prolonged intake of conspicuous amounts of licorice (LE), or its natural constituent glycyrrhizin (G) on murine liver CYP-catalyzed drug metabolism. For this purpose the modulation of the regio- and stereo-selective hydroxylation of testosterone, together with the u...
journal_title：Life sciences
pub_type： 杂志文章
doi：10.1016/s0024-3205(97)01154-5
更新日期：1998-01-01 00:00:00
abstract：:Pretreatment of pancreatic acini with 5-hydroxytryptamine (5-HT) reduced the binding of the labeled somatostatin (SS) analogue 125I-Tyr3-SMS to pancreatic acinar membranes. This effect was dependent of the dose of 5-HT used and length of pretreatment. This inhibitory effect of 5-HT was abolished when pancreatic acini ...
journal_title：Life sciences
pub_type： 杂志文章
doi：10.1016/s0024-3205(97)00161-6
更新日期：1997-01-01 00:00:00
abstract：:The rate of oxidation of sparteine by the 9000 x g supernatant fraction of a human liver was measured in the presence of various drugs which exert cardiovascular effects. Hexamethonium, ouabain, caffeine and isoproterenol had no effect on this rate, while alprenolol, metoprolol, oxprenolol, propranolol, timolol, pindo...
journal_title：Life sciences
pub_type： 杂志文章
doi：10.1016/0024-3205(84)90332-1
更新日期：1984-01-02 00:00:00
abstract：:The acute dose-dependent effects of epinephrine and cocaine on heart rate and coronary flow rate (CFR) were examined in isolated, perfused (Langendorff) rat hearts from animals: i) pretreated with daily cocaine injections (20 mg/kg/day) for 8 weeks; ii) after 2-day withdrawal from 8-week cocaine pretreatment; iii) veh...
journal_title：Life sciences
pub_type： 杂志文章
doi：10.1016/0024-3205(90)90390-d
更新日期：1990-01-01 00:00:00
abstract：:The retina contains three catecholamine neurotransmitters: dopamine (DA); norepinephrine (NE); and epinephrine (EPI). DA and EPI appear to be associated with separate amacrine neurons that directly participate in the visual process. NE, in contrast, appears to be associated primarily with the sympathetic nerves that i...
journal_title：Life sciences
pub_type： 杂志文章,评审
doi：10.1016/0024-3205(84)90184-x
更新日期：1984-09-10 00:00:00
abstract：:We reported previously that acetylcholine (ACh)-induced endothelium-dependent relaxation of rat mesenteric microvessels depended both on nitric oxide (NO) and on a charybdotoxin (CTX)-sensitive endothelium-derived hyperpolarizing vasodilator. Cytochrome P450 (CYP)-dependent arachidonic acid metabolites act in some sys...
journal_title：Life sciences
pub_type： 杂志文章
doi：10.1016/s0024-3205(00)00413-6
更新日期：2000-02-11 00:00:00
abstract：:Unconjugated bilirubin (UCB), like trifluoperazine (TFP), dibucaine (DBC) and praziquantel (PZQ), induces erythrocyte morphological changes, lysis and lipid exfoliation. In the present study we determined whether TFP, DBC and PZQ toxicity to erythrocytes was potentiated or reverted by UCB. Human erythrocytes were eith...
journal_title：Life sciences
pub_type： 杂志文章
doi：10.1016/s0024-3205(01)01171-7
更新日期：2001-07-13 00:00:00
abstract：:Rats were made sensitive to the effects of the opioid antagonist naltrexone by treating them once weekly with cumulative doses of the drug (1, 3, 10, 30 and 100 mg/kg). Sensitization was monitored by measuring salivation following naltrexone administration. During the first week of treatment, no salivation was noted f...
journal_title：Life sciences
pub_type： 杂志文章
doi：10.1016/0024-3205(92)90341-l
更新日期：1992-01-01 00:00:00
abstract：:The purpose of this research is to elucidate the pharmacological mechanism mediating vesicating effects of sulfur mustard (HD) and identify an antidote to its action. HD causes blisters because epithelial cells lose their attachments. Epithelial cell adhesion is under control of the local cytotransmitter acetylcholine...
journal_title：Life sciences
pub_type： 杂志文章
doi：10.1016/s0024-3205(03)00074-2
更新日期：2003-03-28 00:00:00
abstract：AIMS:This study's purpose was to evaluate the effect of ultrasound in air at a frequency of 0.04MHz and an intensity of 50mW/cm2 on neural differentiation of hBM-MSCs in vitro and on neurogenesis in an ischemic stroke model. MATERIALS AND METHODS:hBM-MSCs were exposed to 0.04MHz ultrasound and then compared with no ex...
journal_title：Life sciences
pub_type： 杂志文章
doi：10.1016/j.lfs.2016.08.029
更新日期：2016-11-15 00:00:00
