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adenosine a2a receptor

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https://www.readbyqxmd.com/read/27903722/adenosine-kinase-deficiency-in-the-brain-results-in-maladaptive-synaptic-plasticity
#1
Ursula S Sandau, Mariana Colino-Oliveira, Abbie Jones, Bounmy Saleumvong, Shayla Q Coffman, Long Liu, Catarina Miranda-Lourenço, Cátia Palminha, Vânia L Batalha, Yiming Xu, Yuqing Huo, Maria J Diógenes, Ana M Sebastião, Detlev Boison
: Adenosine kinase (ADK) deficiency in human patients (OMIM:614300) disrupts the methionine cycle and triggers hypermethioninemia, hepatic encephalopathy, cognitive impairment, and seizures. To identify whether this neurological phenotype is intrinsically based on ADK deficiency in the brain or if it is secondary to liver dysfunction, we generated a mouse model with a brain-wide deletion of ADK by introducing a Nestin-Cre transgene into a line of conditional ADK deficient Adk(fl/fl) mice...
November 30, 2016: Journal of Neuroscience: the Official Journal of the Society for Neuroscience
https://www.readbyqxmd.com/read/27893847/a2a-adenosine-receptor-antagonism-reverts-the-blood-brain-barrier-dysfunction-induced-by-sleep-restriction
#2
Gabriela Hurtado-Alvarado, Emilio Domínguez-Salazar, Javier Velázquez-Moctezuma, Beatriz Gómez-González
Chronic sleep restriction induces blood-brain barrier disruption and increases pro-inflammatory mediators in rodents. Those inflammatory mediators may modulate the blood-brain barrier and constitute a link between sleep loss and blood-brain barrier physiology. We propose that adenosine action on its A2A receptor may be modulating the blood-brain barrier dynamics in sleep-restricted rats. We administrated a selective A2A adenosine receptor antagonist (SCH58261) in sleep-restricted rats at the 10th day of sleep restriction and evaluated the blood-brain barrier permeability to dextrans coupled to fluorescein (FITC-dextrans) and Evans blue...
2016: PloS One
https://www.readbyqxmd.com/read/27890589/aged-mice-receiving-caffeine-since-adulthood-show-distinct-patterns-of-anxiety-related-behavior
#3
Paulo Henrique S Botton, Daniela Pochmann, Andreia S Rocha, Fernanda Nunes, Amanda S Almeida, Daniela M Marques, Lisiane O Porciúncula
Caffeine is the psychostimulant most consumed worldwide. Anxiogenic effects of caffeine have been described in adult animalswith controversial findings about its anxiogenic potential. Besides, the effects of caffeine on anxiety with aging are still poorly known. In this study, adult mice (6months old) started to receive caffeine (0.3 and 1.0mg/mL, drinking water) during 12-14months only in the light cycle and at weekdays. The open field (OF) and elevated plus maze (EPM) testing were used to determine the effects of caffeine on anxiety-related behavior in adult and aged mice (18-20months old)...
November 24, 2016: Physiology & Behavior
https://www.readbyqxmd.com/read/27889899/a1-adenosine-receptor-activation-modulates-central-nervous-system-development-and-repair
#4
REVIEW
Shirin Kashfi, Kamran Ghaedi, Hossein Baharvand, Mohammad Hossein Nasr-Esfahani, Mohammad Javan
Adenosine is an endogenous, autacoid purine nucleoside which performs many important biological roles, particularly during stressful events. Adenosine can signal through four adenosine receptor (AR) subtypes: A1, A2A, A2B, and A3. Of these, adenosine A1 receptor (A1AR) has a broad, wide distribution throughout different vertebrate cell types and the highest affinity to adenosine. The A1AR-dependent action of adenosine is well documented in reports from numerous studies that have used different selective A1AR agonists and antagonists as well as in animals that have a genetically manipulated A1AR gene...
November 26, 2016: Molecular Neurobiology
https://www.readbyqxmd.com/read/27872762/understanding-the-functional-plasticity-in-neural-networks-of-the-basal-ganglia-in-cocaine-use-disorder-a-role-for-allosteric-receptor-receptor-interactions-in-a2a-d2-heteroreceptor-complexes
#5
REVIEW
Dasiel O Borroto-Escuela, Karolina Wydra, Julia Pintsuk, Manuel Narvaez, Fidel Corrales, Magdalena Zaniewska, Luigi F Agnati, Rafael Franco, Sergio Tanganelli, Luca Ferraro, Malgorzata Filip, Kjell Fuxe
Our hypothesis is that allosteric receptor-receptor interactions in homo- and heteroreceptor complexes may form the molecular basis of learning and memory. This principle is illustrated by showing how cocaine abuse can alter the adenosine A2AR-dopamine D2R heterocomplexes and their receptor-receptor interactions and hereby induce neural plasticity in the basal ganglia. Studies with A2AR ligands using cocaine self-administration procedures indicate that antagonistic allosteric A2AR-D2R heterocomplexes of the ventral striatopallidal GABA antireward pathway play a significant role in reducing cocaine induced reward, motivation, and cocaine seeking...
2016: Neural Plasticity
https://www.readbyqxmd.com/read/27865066/newly-synthesized-camp-is-integrated-at-a-membrane-protein-complex-signalosome-to-ensure-receptor-response-specificity
#6
Raquel Guinzberg, Antonio Díaz-Cruz, Carlos Acosta-Trujillo, María Magdalena Vilchis-Landeros, Héctor Vázquez-Meza, Carlos Lozano-Flores, Natalia Chiquete-Felix, Alfredo Varela-Echavarría, Salvador Uribe-Carvajal, Héctor Riveros-Rosas, Enrique Piña
Spatiotemporal regulation of cAMP within the cell is required to achieve receptor-specific responses. The mechanism through which the cell selects a specific response to new synthesized cAMP is not fully understood. In hepatocyte plasma membranes, we identified two functional and independent cAMP-responsive signaling protein macrocomplexes that produce, use, degrade, and regulate their own non-diffusible (sequestered) cAMP pool to achieve their specific responses. Each complex responds to the stimulation of an adenosine G-protein coupled receptor (Ado-GPCR), bound to either A2A or A2B , but not simultaneously to both...
November 19, 2016: FEBS Journal
https://www.readbyqxmd.com/read/27862099/identification-of-thermostabilizing-mutations-for-a-membrane-protein-whose-three-dimensional-structure-is-unknown
#7
Yuta Kajiwara, Satoshi Yasuda, Yuuki Takamuku, Takeshi Murata, Masahiro Kinoshita
We recently developed a physics-based method for identifying thermostabilizing mutations of a membrane protein. The method uses a free-energy function F where the importance of translational entropy of hydrocarbon groups within the lipid bilayer is emphasized. All of the possible mutations can rapidly be examined. The method was illustrated for the adenosine A2a receptor (A2a R) whose three-dimensional (3D) structure experimentally determined was utilized as the wild-type structure. Nine single mutations and a double mutation predicted to be stabilizing or destabilizing were checked by referring to the experimental results: The success rate was remarkably high...
November 14, 2016: Journal of Computational Chemistry
https://www.readbyqxmd.com/read/27853423/ethanol-and-caffeine-effects-on-social-interaction-and-recognition-in-mice-involvement-of-adenosine-a2a-and-a1-receptors
#8
Laura López-Cruz, Noemí San-Miguel, Pilar Bayarri, Younis Baqi, Christa E Müller, John D Salamone, Mercé Correa
Ethanol and caffeine are frequently consumed in combination and have opposite effects on the adenosine system: ethanol metabolism leads to an increase in adenosine levels, while caffeine is a non-selective adenosine A1/A2A receptor antagonist. These receptors are highly expressed in striatum and olfactory tubercle, brain areas involved in exploration and social interaction in rodents. Ethanol modulates social interaction processes, but the role of adenosine in social behavior is still poorly understood. The present work was undertaken to study the impact of ethanol, caffeine and their combination on social behavior, and to explore the involvement of A1 and A2A receptors on those actions...
2016: Frontiers in Behavioral Neuroscience
https://www.readbyqxmd.com/read/27846189/the-plausible-association-of-mthfr-and-adora2a-polymorphisms-with-nodules-in-rheumatoid-arthritis-patients-treated-with-methotrexate
#9
Tomas Soukup, Martin Dosedel, Jana Nekvindova, Ales Antonin Kubena, Ilja Tacheci, Jurjen Duintjer Tebbens, Jiri Vlcek, Petr Bradna, Ivan Barvik, Petr Pavek
OBJECTIVE: The treatment of rheumatoid arthritis (RA) patients with methotrexate (MTX) is linked to the development or progression of rheumatoid nodules. The aim of this study was to determine whether folate and adenosine pathways-related single nucleotide polymorphisms might be predictive of increased nodule formation in RA patients treated with oral MTX. METHODS: A total of 185 Caucasian RA patients were enrolled in this cross-sectional study, all of whom fulfilled the 1987 RA criteria of the American College of Rheumatology; each patient had a history of MTX treatment...
November 14, 2016: Pharmacogenetics and Genomics
https://www.readbyqxmd.com/read/27836398/discovery-of-1-3-diethyl-7-methyl-8-phenoxymethyl-xanthine-derivatives-as-novel-adenosine-a1-and-a2a-receptor-antagonists
#10
Rozanne Harmse, Mietha M van der Walt, Jacobus P Petzer, Gisella Terre'Blanche
Based on a previous report that a series of 8-(phenoxymethyl)-xanthines may be promising leads for the design of A1 adenosine receptor antagonists, selected novel and known 1,3-diethyl-7-methyl-8-(phenoxymethyl)-xanthine and 1,3,7-trimethyl-8-(phenoxymethyl)-xanthine analogs were synthesized and evaluated for their A1 and A2A adenosine receptor affinity. Generally, the study compounds exhibited affinity for both the A1 and A2A adenosine receptors. Replacement of the 1,3-dimethyl-substition with a 1,3-diethyl-substition pattern increased A1 and A2A binding affinity...
December 15, 2016: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/27835671/an-anti-parkinson-s-disease-drug-via-targeting-adenosine-a2a-receptor-enhances-amyloid-%C3%AE-generation-and-%C3%AE-secretase-activity
#11
Jing Lu, Jin Cui, Xiaohang Li, Xin Wang, Yue Zhou, Wenjuan Yang, Ming Chen, Jian Zhao, Gang Pei
γ-secretase mediates the intramembranous proteolysis of amyloid precursor protein (APP) and determines the generation of Aβ which is associated with Alzheimer's disease (AD). Here we identified that an anti-Parkinson's disease drug, Istradefylline, could enhance Aβ generation in various cell lines and primary neuronal cells of APP/PS1 mouse. Moreover, the increased generation of Aβ42 was detected in the cortex of APP/PS1 mouse after chronic treatment with Istradefylline. Istradefylline promoted the activity of γ-secretase which could lead to increased Aβ production...
2016: PloS One
https://www.readbyqxmd.com/read/27821588/smooth-muscle-cell-pro-angiogenic-phenotype-induced-by-cyclopentenyl-cytosine-promotes-endothelial-cell-proliferation-and-migration
#12
Rui Tang, Gui Zhang, Shi-You Chen
Vascular smooth muscle cells (SMCs) and endothelial cells (ECs) have a close contact with the blood vessel. SMC phenotypes can be altered during pathological vascular remodeling. However, how SMC phenotypes affect EC properties remain largely unknown. In the present study, we found that platelet-derived growth factor (PDGF)-BB-induced synthetic SMC suppressed EC proliferation and migration while exhibiting an increased expression of anti-angiogenic factors such as endostatin and decreased pro-angiogenic factors including C-X-C motif ligand 1 (CXCL1)...
November 7, 2016: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/27818940/critical-role-for-adenosine-receptor-a2a-in-%C3%AE-cell-proliferation
#13
Nadja Schulz, Ka-Cheuk Liu, Jérémie Charbord, Charlotte L Mattsson, Lingjie Tao, Dominika Tworus, Olov Andersson
OBJECTIVE: Pharmacological activation of adenosine signaling has been shown to increase β-cell proliferation and thereby β-cell regeneration in zebrafish and rodent models of diabetes. However, whether adenosine has an endogenous role in regulating β-cell proliferation is unknown. The objective of this study was to determine whether endogenous adenosine regulates β-cell proliferation-either in the basal state or states of increased demand for insulin-and to delineate the mechanisms involved...
November 2016: Molecular Metabolism
https://www.readbyqxmd.com/read/27812030/predicting-subtype-selectivity-for-adenosine-receptor-ligands-with-three-dimensional-biologically-relevant-spectrum-brs-3d
#14
Song-Bing He, Ben Hu, Zheng-Kun Kuang, Dong Wang, De-Xin Kong
Adenosine receptors (ARs) are potential therapeutic targets for Parkinson's disease, diabetes, pain, stroke and cancers. Prediction of subtype selectivity is therefore important from both therapeutic and mechanistic perspectives. In this paper, we introduced a shape similarity profile as molecular descriptor, namely three-dimensional biologically relevant spectrum (BRS-3D), for AR selectivity prediction. Pairwise regression and discrimination models were built with the support vector machine methods. The average determination coefficient (r(2)) of the regression models was 0...
November 4, 2016: Scientific Reports
https://www.readbyqxmd.com/read/27810394/validation-of-a-na-shift-binding-assay-for-estimation-of-the-intrinsic-efficacy-of-ligands-at-the-a2a-adenosine-receptor
#15
François Noël, Fernando M do Monte
INTRODUCTION: Determination of the intrinsic efficacy of ligands at the A2A receptor is important for selecting drug candidates, e.g. in the case of inflammatory diseases where agonists are searched for or in Parkinson disease (antagonists). METHODS: Three functional binding assays were compared with up to seven ligands with different efficacies: the GTP-shift method based on the decrease of affinity observed with agonists when GTP is added to the competition binding assay; the Ki ratio method based on the different affinity states of the receptor when using an agonist or antagonist radioligand and the Na(+)-shift assay based on the difference of affinity of agonists when tested in a medium containing a divalent cation (50mM MgCl2) favoring the G protein coupled agonist-receptor complex or sodium (100mM NaCl) as negative allosteric modulator...
November 1, 2016: Journal of Pharmacological and Toxicological Methods
https://www.readbyqxmd.com/read/27803241/structure-activity-relationships-of-the-sustained-effects-of-adenosine-a2a-receptor-agonists-driven-by-slow-dissociation-kinetics
#16
J Daniel Hothersall, Dong Guo, Sunil Sarda, Robert J Sheppard, Hongming Chen, Wesley Keur, Michael J Waring, Adriaan P IJzerman, Stephen J Hill, Ian L Dale, Philip B Rawlins
The duration of action of adenosine A2A receptor (A2A) agonists is critical for their clinical efficacy, and we sought to better understand how this can be optimized. The in vitro temporal response profiles of a panel of A2A agonists were studied using cAMP assays in recombinantly (CHO) and endogenously (SH-SY5Y) expressing cells. Some agonists (e.g., 3cd; UK-432,097) but not others (e.g., 3ac; CGS-21680) demonstrated sustained wash-resistant agonism, where residual receptor activation continued after washout...
January 2017: Molecular Pharmacology
https://www.readbyqxmd.com/read/27799962/protective-effects-of-adenosine-receptor-agonist-in-a-cirrhotic-liver-resection-model
#17
Emil Iskandarov, Pramod Kadaba Srinivasan, Wang Xin, Christian Bleilevens, Mamdouh Afify, Astrit Hamza, Lai Wei, Koichiro Hata, Boyukkishi Agayev, Rene Tolba
OBJECTIVES: To investigate the role of CGS21680, a selective adenosine A2A receptor agonist, on a bile-duct-ligated cirrhotic liver resection model in rats. METHODS: Male Wistar rats were allotted into 3 groups (n = 7 per time-point): the control group, the bile duct ligation + CGS21680 group (BDL + CGS), and the bile duct ligation group (BDL). Biliary cirrhosis had been previously induced by ligature of the common bile duct in the BDL + CGS and BDL groups. After 2 weeks, the animals underwent partial hepatectomy (50%)...
August 2016: Hepatitis Monthly
https://www.readbyqxmd.com/read/27799539/membrane-protein-structure-determination-by-sad-sir-or-siras-phasing-in-serial-femtosecond-crystallography-using-an-iododetergent
#18
Takanori Nakane, Shinya Hanashima, Mamoru Suzuki, Haruka Saiki, Taichi Hayashi, Keisuke Kakinouchi, Shigeru Sugiyama, Satoshi Kawatake, Shigeru Matsuoka, Nobuaki Matsumori, Eriko Nango, Jun Kobayashi, Tatsuro Shimamura, Kanako Kimura, Chihiro Mori, Naoki Kunishima, Michihiro Sugahara, Yoko Takakyu, Shigeyuki Inoue, Tetsuya Masuda, Toshiaki Hosaka, Kensuke Tono, Yasumasa Joti, Takashi Kameshima, Takaki Hatsui, Makina Yabashi, Tsuyoshi Inoue, Osamu Nureki, So Iwata, Michio Murata, Eiichi Mizohata
The 3D structure determination of biological macromolecules by X-ray crystallography suffers from a phase problem: to perform Fourier transformation to calculate real space density maps, both intensities and phases of structure factors are necessary; however, measured diffraction patterns give only intensities. Although serial femtosecond crystallography (SFX) using X-ray free electron lasers (XFELs) has been steadily developed since 2009, experimental phasing still remains challenging. Here, using 7.0-keV (1...
October 31, 2016: Proceedings of the National Academy of Sciences of the United States of America
https://www.readbyqxmd.com/read/27792010/theobromine-induced-changes-in-a1-purinergic-receptor-gene-expression-and-distribution-in-a-rat-brain-alzheimer-s-disease-model
#19
Jesus Mendiola-Precoma, Karla Padilla, Alfredo Rodríguez-Cruz, Laura C Berumen, Ricardo Miledi, Guadalupe García-Alcocer
Dementia caused by Alzheimer's disease (AD) is mainly characterized by accumulation in the brain of extra- and intraneuronal amyloid-β (Aβ) and tau proteins, respectively, which selectively affect specific regions, particularly the neocortex and the hippocampus. Sporadic AD is mainly caused by an increase in apolipoprotein E, a component of chylomicrons, which are cholesterol transporters in the brain. Recent studies have shown that high lipid levels, especially cholesterol, are linked to AD. Adenosine is an atypical neurotransmitter that regulates a wide range of physiological functions by activating four P1 receptors (A1, A2A, A2B, and A3) and P2 purinergic receptors that are G protein-coupled...
October 24, 2016: Journal of Alzheimer's Disease: JAD
https://www.readbyqxmd.com/read/27791262/polydeoxyribonucleotides-pdrns-from-skin-to-musculoskeletal-tissue-regeneration-via-adenosine-a2a-receptor-involvement-a-mini-review
#20
REVIEW
Francesca Veronesi, Dante Dallari, Giacomo Sabbioni, Chiara Carubbi, Lucia Martini, Milena Fini
Polydeoxyribonucleotides (PDRNs) are low molecular weight DNA molecules of natural origin that stimulate cell migration and growth, extracellular matrix (ECM) protein production and reduce inflammation. Most preclinical and clinical studies on tissue regeneration with PDRNs focused on skin, and only few are about musculoskeletal tissues. Starting from an overview on skin regeneration studies, through the analysis of in vitro, in vivo and clinical studies (1990-2016), the present review aimed at defining the effects of PDRN and their mechanisms of action in the regeneration of musculoskeletal tissues...
October 28, 2016: Journal of Cellular Physiology
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