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https://www.readbyqxmd.com/read/29145453/the-antiviral-drug-tenofovir-an-inhibitor-of-pannexin-1-mediated-atp-release-prevents-liver-and-skin-fibrosis-by-downregulating-adenosine-levels-in-the-liver-and-skin
#1
Jessica L Feig, Aranzazu Mediero, Carmen Corciulo, Hailing Liu, Jin Zhang, Miguel Perez-Aso, Laura Picard, Tuere Wilder, Bruce Cronstein
BACKGROUND: Fibrosing diseases are a leading cause of morbidity and mortality worldwide and, therefore, there is a need for safe and effective antifibrotic therapies. Adenosine, generated extracellularly by the dephosphorylation of adenine nucleotides, ligates specific receptors which play a critical role in development of hepatic and dermal fibrosis. Results of recent clinical trials indicate that tenofovir, a widely used antiviral agent, reverses hepatic fibrosis/cirrhosis in patients with chronic hepatitis B infection...
2017: PloS One
https://www.readbyqxmd.com/read/29129783/hypoxia-induced-mir-214-expression-promotes-tumour-cell-proliferation-and-migration-by-enhancing-the-warburg-effect-in-gastric-carcinoma-cells
#2
Liuqing Yang, Weijie Zhang, Yanbo Wang, Tianhui Zou, Bin Zhang, Yuanyuan Xu, Taohong Pang, Qingqing Hu, Min Chen, Lei Wang, Ying Lv, Kai Yin, Hongwei Liang, Xi Chen, Guifang Xu, Xiaoping Zou
miR-214 is an important oncomiRNA and is upregulated in various types of cancer, including gastric cancer. However, the molecular mechanism underlying the ectopic expression and function of miR-214 in gastric cancer is largely undefined. In this study, we found that miR-214 induces the Warburg effect and promotes the migration and proliferation of human gastric cancer cells. According to the mechanistic analysis, miR-214 expression is induced by environmental hypoxia, and miR-214 mediates hypoxia-induced functions...
November 9, 2017: Cancer Letters
https://www.readbyqxmd.com/read/29126977/enhancement-of-inosine-mediated-a2ar-signaling-through-positive-allosteric-modulation
#3
Ajith A Welihinda, Manmeet Kaur, Kaviya S Raveendran, Edward P Amento
Inosine is an endogenous nucleoside that is produced by metabolic deamination of adenosine. Inosine is metabolically more stable (half-life 15h) than adenosine (half-life <10s). Inosine exerts anti-inflammatory and immunomodulatory effects similar to those observed with adenosine. These effects are mediated in part through the adenosine A2A receptor (A2AR). Relative to adenosine inosine exhibits a lower affinity towards the A2AR. Therefore, it is generally believed that inosine is incapable of activating the A2AR through direct engagement, but indirectly activates the A2AR upon metabolic conversion to higher affinity adenosine...
November 8, 2017: Cellular Signalling
https://www.readbyqxmd.com/read/29079454/the-adenosine-a2a-receptor-agonist-t1-11-ameliorates-neurovisceral-symptoms-and-extends-the-lifespan-of-a-mouse-model-of-niemann-pick-type-c-disease
#4
Antonella Ferrante, Antonella Pezzola, Andrea Matteucci, Antonella Di Biase, Lucilla Attorri, Monica Armida, Alberto Martire, Yijuang Chern, Patrizia Popoli
Niemann-Pick C is a fatal neurovisceral disorder caused, in 95% of cases, by mutation of NPC1 gene. Therapeutic options are extremely limited and new "druggable" targets are highly warranted. We previously demonstrated that the stimulation of the adenosine A2A receptor (A2AR) normalized the pathological phenotype of cellular models of NPC1. Since the validation of A2ARs as a therapeutic target for NPC1 can be obtained only conducting studies in in vivo models of the disease, in the present paper, the effects of two agonists of A2ARs were evaluated in the mouse model Balb/c Npc1(nih), hereafter indicated as NPC1-/-...
October 25, 2017: Neurobiology of Disease
https://www.readbyqxmd.com/read/29071996/-effect-of-electroacupuncture-on-adenosine-receptor-expression-in-white-adipose-tissue-of-diet-induced-obese-mice
#5
Yue-Xia Tang, Jian-Zhong Meng, Ya-Juan Ding, Hao Hong, Mei-Ling Yu, Xin-Yue Jing, Sheng-Feng Lu, Bing-Mei Zhu
OBJECTIVE: To investigate the effects of electroacupuncture (EA) on the expression of adenosine receptor (AR) in the white adipose tissue (WAT) of diet-induced obese (DIO) mice, so as to reveal a peripheral mechanism of EA underlying improvement of body weight. METHODS: Forty three-week-old C 57 BL/6 male mice were divided into normal diet group (n=12) and high fat diet group (n=28) randomly, and fed by normal diet and high fat diet for 12 weeks, respectively. In the high fat diet group, mice with body weight over 20% heavier than that of the normal diet group were considered as obese mice...
February 25, 2017: Zhen Ci Yan Jiu, Acupuncture Research
https://www.readbyqxmd.com/read/29064819/age-related-decline-of-the-acute-local-inflammation-response-a-mitigating-role-for-the-adenosine-a2a-receptor
#6
Cynthia Laflamme, Geneviève Bertheau Mailhot, Marc Pouliot
Aging is accompanied by an increase in markers of innate immunity. How aging affects neutrophil functions remains of debate.The adenosine A2A receptor (A2AR), essential to the resolution of inflammation, modulates neutrophil functions. We sought to determine whether or not A2AR protects against the effects of aging. We monitored neutrophil influx, viability, and activation as well as cytokine accumulation in wild-type (WT) and A2AR-knockout mice (KO) at three different ages.Several readouts decreased with aging: neutrophil counts in dorsal air pouches (by up to 55%), neutrophil viability (by up to 56%), elastase and total protein in exudates (by up to 80%), and local levels of cytokines (by up to 90%)...
October 18, 2017: Aging
https://www.readbyqxmd.com/read/29042444/development-of-novel-biosensors-to-study-receptor-mediated-activation-of-gs-and-golf
#7
Hideaki Yano, Davide Provasi, Ning Sheng Cai, Marta Filizola, Sergi Ferre, Jonathan A Javitch
Gαs (Gs) and Gαolf (Golf) are highly homologous G protein α; subunits that activate adenylate cyclase, thereby serving as crucial mediators of intracellular signaling. Owing to their dramatically different brain expression patterns, we studied similarities and differences between their activation processes with the aim of comparing their receptor coupling mechanisms. We engineered novel luciferase- and Venus-fused Gα constructs that can be used in bioluminescence resonance energy transfer (BRET) assays...
October 17, 2017: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/29022877/striatal-adenosine-a2a-receptor-neurons-control-active-period-sleep-via-parvalbumin-neurons-in-external-globus-pallidus
#8
Xiang-Shan Yuan, Lu Wang, Hui Dong, Wei-Min Qu, Su-Rong Yang, Yoan Cherasse, Michael Lazarus, Serge N Schiffmann, Alban de Kerchove d'Exaerde, Rui-Xi Li, Zhi-Li Huang
Dysfunction of the striatum is frequently associated with sleep disturbances. However, its role in sleep-wake regulation has been paid little attention even though the striatum densely expresses adenosine A2A receptors (A2ARs), which are essential for adenosine-induced sleep. Here we showed that chemogenetic activation of A2AR neurons in specific subregions of the striatum induced a remarkable increase in non-rapid eye movement (NREM) sleep. Anatomical mapping and immunoelectron microscopy revealed that striatal A2AR neurons innervated the external globus pallidus (GPe) in a topographically organized manner and preferentially formed inhibitory synapses with GPe parvalbumin (PV) neurons...
October 12, 2017: ELife
https://www.readbyqxmd.com/read/28984574/ligand-modulation-of-sidechain-dynamics-in-a-wild-type-human-gpcr
#9
Lindsay D Clark, Igor Dikiy, Karen Chapman, Karin Ej Rödström, James Aramini, Michael V LeVine, George Khelashvili, Søren Gf Rasmussen, Kevin H Gardner, Daniel M Rosenbaum
GPCRs regulate all aspects of human physiology, and biophysical studies have deepened our understanding of GPCR conformational regulation by different ligands. Yet there is no experimental evidence for how sidechain dynamics control allosteric transitions between GPCR conformations. To address this deficit, we generated samples of a wild-type GPCR (A2AR) that are deuterated apart from (1)H/(13)C NMR probes at isoleucine δ1 methyl groups, which facilitated (1)H/(13)C methyl TROSY NMR measurements with opposing ligands...
October 6, 2017: ELife
https://www.readbyqxmd.com/read/28981089/treatment-with-a2a-receptor-antagonist-kw6002-and-caffeine-intake-regulate-microglia-reactivity-and-protect-retina-against-transient-ischemic-damage
#10
Raquel Boia, Filipe Elvas, Maria H Madeira, Inês D Aires, Ana C Rodrigues-Neves, Pedro Tralhão, Eszter C Szabó, Younis Baqi, Christa E Müller, Ângelo R Tomé, Rodrigo A Cunha, António F Ambrósio, Ana R Santiago
Transient retinal ischemia is a major complication of retinal degenerative diseases and contributes to visual impairment and blindness. Evidences indicate that microglia-mediated neuroinflammation has a key role in the neurodegenerative process, prompting the hypothesis that the control of microglia reactivity may afford neuroprotection to the retina against the damage induced by ischemia-reperfusion (I-R). The available therapeutic strategies for retinal degenerative diseases have limited potential, but the blockade of adenosine A2A receptor (A2AR) emerges as candidate strategy...
October 5, 2017: Cell Death & Disease
https://www.readbyqxmd.com/read/28979687/activation-of-a2ar-attenuates-bleomycin-induced-pulmonary-fibrosis-via-the-sdf-1-cxcr4-axis-related-pathway
#11
Yanfan Chen, Xiaoming Yu, Yicheng He, Lin Zhang, Xiaoying Huang, Xiaomei Xu, Mayun Chen, Xiang Chen, Liangxing Wang
Previous studies in our lab have demonstrated that Adenosine A2a receptor (A2aR) gene-knockout mice were vulnerable to pulmonary fibrosis induced by bleomycin (BLM). Inhibition of the SDF-1/CXCR4 axis has been reported to protect the lungs from fibrogenesis in BLM-exposed mice. Little is yet known about the relationships between A2aR and the SDF-1/CXCR4 axis in idiopathic pulmonary fibrosis (IPF). This study probes the role of A2aR in the fibrotic process and explores the relationship between A2aR and the SDF-1/CXCR4 axis in BLM-induced pulmonary fibrosis in mice...
2017: American Journal of Translational Research
https://www.readbyqxmd.com/read/28978989/adenosine-a2a-receptor-mediates-hypnotic-effects-of-ethanol-in-mice
#12
Teng Fang, Hui Dong, Xin-Hong Xu, Xiang-Shan Yuan, Ze-Ka Chen, Jiang-Fan Chen, Wei-Min Qu, Zhi-Li Huang
Ethanol has extensive effects on sleep and daytime alertness, causing premature disability and death. Adenosine, as a potent sleep-promoting substance, is involved in many cellular and behavioral responses to ethanol. However, the mechanisms of hypnotic effects of ethanol remain unclear. In this study, we investigated the role of adenosine in ethanol-induced sleep using C57BL/6Slac mice, adenosine A2A receptor (A2AR) knockout mice, and their wild-type littermates. The results showed that intraperitoneal injection of ethanol (3...
October 4, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28941549/the-corticostriatal-adenosine-a2a-receptor-controls-maintenance-and-retrieval-of-spatial%C3%A2-working-memory
#13
Zhihui Li, Xingjun Chen, Tao Wang, Ying Gao, Fei Li, Long Chen, Jin Xue, Yan He, Yan Li, Wei Guo, Wu Zheng, Liping Zhang, Fenfen Ye, Xiangpeng Ren, Yue Feng, Piu Chan, Jiang-Fan Chen
BACKGROUND: Working memory (WM) taps into multiple executive processes including encoding, maintenance, and retrieval of information, but the molecular and circuit modulation of these WM processes remains undefined due to the lack of methods to control G protein-coupled receptor signaling with temporal resolution of seconds. METHODS: By coupling optogenetic control of the adenosine A2A receptor (A2AR) signaling, the Cre-loxP-mediated focal A2AR knockdown with a delayed non-match-to-place (DNMTP) task, we investigated the effect of optogenetic activation and focal knockdown of A2ARs in the dorsomedial striatum (n = 8 to 14 per group) and medial prefrontal cortex (n = 16 to 22 per group) on distinct executive processes of spatial WM...
August 1, 2017: Biological Psychiatry
https://www.readbyqxmd.com/read/28855798/abnormalities-of-dopamine-d3-receptor-signaling-in-the-diseased-brain
#14
REVIEW
G Aleph Prieto
Dopamine D3 receptors (D3R) modulate neuronal activity in several brain regions including cortex, striatum, cerebellum, and hippocampus. A growing body of evidence suggests that aberrant D3R signaling contributes to multiple brain diseases, such as Parkinson's disease, essential tremor, schizophrenia, and addiction. In line with these findings, D3R has emerged as a potential target in the treatment of neurological disorders. However, the mechanisms underlying neuronal D3R signaling are poorly understood, either in healthy or diseased brain...
2017: Journal of Central Nervous System Disease
https://www.readbyqxmd.com/read/28844595/cognitive-impairments-associated-with-alterations-in-synaptic-proteins-induced-by-the-genetic-loss-of-adenosine-a2a-receptors-in-mice
#15
Maria Moscoso-Castro, Marc López-Cano, Irene Gracia-Rubio, Francisco Ciruela, Olga Valverde
The study of psychiatric disorders usually focuses on emotional symptoms assessment. However, cognitive deficiencies frequently constitute the core symptoms, are often poorly controlled and handicap individual's quality of life. Adenosine receptors, through the control of both dopamine and glutamate systems, have been implicated in the pathophysiology of several psychiatric disorders such as schizophrenia and attention deficit/hyperactivity disorder. Indeed, clinical data indicate that poorly responsive schizophrenia patients treated with adenosine adjuvants show improved treatment outcomes...
August 26, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28842709/the-parkinson-s-disease-associated-gpr37-receptor-interacts-with-striatal-adenosine-a2a-receptor-controlling-its-cell-surface-expression-and-function-in-vivo
#16
Xavier Morató, Rafael Luján, Marc López-Cano, Jorge Gandía, Igor Stagljar, Masahiko Watanabe, Rodrigo A Cunha, Víctor Fernández-Dueñas, Francisco Ciruela
G protein-coupled receptor 37 (GPR37) is an orphan receptor associated to Parkinson's disease (PD) neuropathology. Here, we identified GPR37 as an inhibitor of adenosine A2A receptor (A2AR) cell surface expression and function in vivo. In addition, we showed that GPR37 and A2AR do oligomerize in the striatum. Thus, a close proximity of GPR37 and A2AR at the postsynaptic level of striatal synapses was observed by double-labelling post-embedding immunogold detection. Indeed, the direct receptor-receptor interaction was further substantiated by proximity ligation in situ assay...
August 25, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28807491/adenosine-a2a-receptor-signaling-affects-il-21-il-22-cytokines-and-gata3-t-bet-transcription-factor-expression-in-cd4-t-cells-from-a-btbr-t-itpr3tf-j-mouse-model-of-autism
#17
Sheikh F Ahmad, Mushtaq A Ansari, Ahmed Nadeem, Saleh A Bakheet, Mashal M Almutairi, Sabry M Attia
Autism is a complex heterogeneous neurodevelopmental disorder; previous studies have identified altered immune responses among individuals diagnosed with autism. An imbalance in the production of pro- and anti-inflammatory cytokines and transcription factors plays a role in neurodevelopmental behavioral and autism disorders. BTBR T(+) Itpr3tf/J (BTBR) mice are used as a model for autism, as they exhibit social deficits, communication deficits, and repetitive behaviors compared with C57BL/6J (B6) mice. The adenosine A2A receptor (A2AR) appears to be a potential target for the improvement of behavioral, inflammatory, immune, and neurological disorders...
October 15, 2017: Journal of Neuroimmunology
https://www.readbyqxmd.com/read/28779842/strategy-for-the-thermostabilization-of-an-agonist-bound-gpcr-coupled-to-a-g-protein
#18
Annette Strege, Byron Carpenter, Patricia C Edwards, Christopher G Tate
Structure determination of G protein-coupled receptors (GPCRs) in the inactive state bound to high-affinity antagonists has been very successful through the implementation of a number of protein engineering and crystallization strategies. However, the structure determination of GPCRs in their fully active state coupled to a G protein is still very challenging. Recently, mini-G proteins were developed, which recapitulate the coupling of a full heterotrimeric G protein to a GPCR despite being less than one-third of the size...
2017: Methods in Enzymology
https://www.readbyqxmd.com/read/28774332/baicalin-attenuates-chronic-hypoxia-induced-pulmonary-hypertension-via-adenosine-a2a-receptor-induced-sdf-1-cxcr4-pi3k-akt-signaling
#19
Xiaoying Huang, Peiliang Wu, Feifei Huang, Min Xu, Mayun Chen, Kate Huang, Guo-Ping Li, Manhuan Xu, Dan Yao, Liangxing Wang
BACKGROUND: Baicalin, an important flavonoid in Scutellaria baicalensis Georgi extracts, exerts a variety of pharmacological effects. In this study, we explored the effects of baicalin on chronic hypoxia-induced pulmonary arterial hypertension (PAH) and investigated the mechanism underlying these effects. Moreover, we examined whether the inflammatory response was mediated by the A2A receptor (A2AR) and stromal cell-derived factor-1 (SDF-1)/C-X-C chemokine receptor type 4 (CXCR4)-induced phosphatidyl inositol-3-kinase (PI3K) signaling in vivo...
August 3, 2017: Journal of Biomedical Science
https://www.readbyqxmd.com/read/28758541/cobra-neurotoxin-produces-central-analgesic-and-hyperalgesic-actions-via-adenosine-a1-and-a2a-receptors
#20
Chuang Zhao, Jun Zhao, Qian Yang, Yong Ye
Cobra neurotoxin, a short-chain peptide isolated from snake venom of Naja naja atra, showed both a central analgesic effect and a hyperalgesic effect in mice tests. In order to explore mechanisms, a hypothesis is put forward that cobra neurotoxin takes effect through adenosine receptor pathway. The central effects of cobra neurotoxin were evaluated using the hot plate test (a model of acute pain) and the spinal cord injury (a model of central pain) in mice and using A1 receptor antagonist (DPCPX) and A2A receptor antagonist (ZM241385); behaviors were scored and signal molecules such as reactive oxygen species and adenosine triphosphate levels and mitogen-activated protein kinases/extracellular signal-regulated protein kinase expression were measured...
January 2017: Molecular Pain
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