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adenosine a2a receptor

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https://www.readbyqxmd.com/read/29792714/docking-screens-for-dual-inhibitors-of-disparate-drug-targets-for-parkinson-s-disease
#1
Mariama Jaiteh, Alexey Zeifman, Marcus Saarinen, Per Svenningsson, José M Brea, Maria Isabel Loza, Jens Carlsson
Modulation of multiple biological targets with a single drug can lead to synergistic therapeutic effects and has been demonstrated to be essential for efficient treatment of CNS disorders. However, rational design of compounds that interact with several targets is very challenging. Here, we demonstrate that structure-based virtual screening can guide the discovery of multi-target ligands of unrelated proteins relevant for Parkinson's disease. A library with 5.4 million molecules was docked to crystal structures of the A2A adenosine receptor (A2AAR) and monoamine oxidase B (MAO-B)...
May 24, 2018: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29790247/the-promotion-of-tissue-engineering-blood-vessel-patency-by-cgs21680-through-regulating-pro-inflammatory-activities-of-endothelial-progenitor-cell
#2
Wen Chen, Li Xiao, Jian Bai, Wen Zeng, Mingcan Yang, Bingyi Shi, Chuhong Zhu
The mobilization and homing of endothelial progenitor cells (EPCs) contribute to the rapid endothelialization of tissue engineering blood vessel (TEBV). Inflammation can affect TEBV patency, and monocytes/macrophages (MM) are the main effector cells. But it is not clear how EPCs interact with MM after TEBV transplantation. Our results showed acellular materials would not directly cause acute and severe inflammatory responses but activate E-selectin expression in homing EPCs, gradually promoting the polarization of MM to the M1...
May 23, 2018: Journal of Biomedical Materials Research. Part A
https://www.readbyqxmd.com/read/29770921/neuronal-adenosine-a-2a-receptor-overexpression-is-neuroprotective-towards-3-nitropropionic-acid-induced-striatal-toxicity-a-rat-model-of-huntington-s-disease
#3
Maria Rosaria Domenici, Valentina Chiodi, Mirko Averna, Monica Armida, Antonella Pèzzola, Rita Pepponi, Antonella Ferrante, Michael Bader, Kjell Fuxe, Patrizia Popoli
The A2A adenosine receptor (A2A R) is widely distributed on different cellular types in the brain, where it exerts a broad spectrum of pathophysiological functions, and for which a role in different neurodegenerative diseases has been hypothesized or demonstrated. To investigate the role of neuronal A2A Rs in neurodegeneration, we evaluated in vitro and in vivo the effect of the neurotoxin 3-nitropropionic acid (3-NP) in a transgenic rat strain overexpressing A2A Rs under the control of the neural-specific enolase promoter (NSEA2A rats)...
May 16, 2018: Purinergic Signalling
https://www.readbyqxmd.com/read/29769005/adenosine-synthetic-methods-of-its-derivatives-and-antitumor-activity
#4
Margarita Gutierrez, Francisco Valdes, Victor Luna, Barbara Arevalo, Nelson Brown
Since 1929, several researchers have conducted studies in relation the nucleoside of adenosine (1) mainly distribution identifying, characterizing their biological importance and synthetic chemistry to which this type of molecule has been subjected to obtain multiple of its derivatives. The receptors that interact with adenosine and its derivatives, called purinergic receptors, are classified as A1, A2A, A2B and A3. In the presence of agonists and antagonists, these receptors are involved in various physiological processes and diseases...
May 16, 2018: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/29761007/behavioral-changes-induced-through-adenosine-a2a-receptor-ligands-in-a-rat-depression-model-induced-by-olfactory-bulbectomy
#5
Karla Margarita Padilla, Andres Quintanar-Setephano, Fabian López-Vallejo, Laura Cristina Berumen, Ricardo Miledi, Guadalupe García-Alcocer
Background: Major depressive disorders are characterized by their severity and long-lasting symptoms, which make such disorders highly disabling illnesses. Unfortunately, 50% of major depressive patients experience relapses, perhaps partly because drug research has been performed only in animal models that screen for antidepressant drugs that appear to only ameliorate acute depression symptoms. The bilateral olfactory bulbectomy (OBX) animal model presents the advantage of mimicking the symptoms of chronic depression by means of brain surgery...
May 2018: Brain and Behavior
https://www.readbyqxmd.com/read/29753566/design-and-synthesis-of-2-6-disubstituted-8-amino-imidazo-1-2a-pyridines-a-promising-privileged-structure
#6
Rajaa Boulahjar, Angela Rincon Arias, Raphaël Bolteau, Nicolas Renault, Mathilde Coevoet, Amélie Barczyk, Romain Duroux, Saïd Yous, Patricia Melnyk, Laurence Agouridas
Imidazo[1,2a]pyridines have gained much interest in the field of medicinal chemistry research. In the aim of accessing new privileged structure, we decided to design and synthesize 8-aminated-imidazo[1,2a]pyridines substituted on positions 2 and 6. This scaffold, rarely found in the literature, was obtained via palladium-catalyzed coupling reactions (Suzuki reaction or N-hydroxysuccinimidyl activated ester method) and tested on adenosine receptor A2A . We demonstrated how incorporation of an exocyclic amine enhanced affinity towards this receptor while maintaining low cytotoxicity...
April 30, 2018: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/29745882/the-adenosinergic-system-a-potential-player-in-the-pathogenesis-of-anca-associated-vasculitis
#7
REVIEW
Lovis Kling, Bernhard K Krämer, Benito A Yard, Anna-Isabelle Kälsch
Antineutrophil cytoplasmic antibody (ANCA)-associated vasculitis (AAV) is a potentially lethal autoimmune disease whose pathology comprises disturbed T cell differentiation and functionality accompanied by dysfunctional autoreactive immunoglobulin development, culminating in destructive innate immune response as well. Purines, adenine nucleotides and adenosine in particular, have been elucidated as potent extracellular mediators for fine adjustment of these pivotal processes establishing human immunity. Therefore, the extracellular purinergic microenvironment is under control of ectonucleotidases CD39 and CD73 degrading pro-inflammatory adenosine triphosphate (ATP) to anti-inflammatory adenosine as well as adenosine deaminase bound to CD26 deactivating adenosine...
May 3, 2018: Clinical and Experimental Rheumatology
https://www.readbyqxmd.com/read/29740323/the-selective-antagonism-of-adenosine-a-2b-receptors-reduces-the-synaptic-failure-and-neuronal-death-induced-by-oxygen-and-glucose-deprivation-in-rat-ca1-hippocampus-in-vitro
#8
Irene Fusco, Filippo Ugolini, Daniele Lana, Elisabetta Coppi, Ilaria Dettori, Lisa Gaviano, Daniele Nosi, Federica Cherchi, Felicita Pedata, Maria G Giovannini, Anna M Pugliese
Ischemia is a multifactorial pathology characterized by different events evolving in time. Immediately after the ischemic insult, primary brain damage is due to the massive increase of extracellular glutamate. Adenosine in the brain increases dramatically during ischemia in concentrations able to stimulate all its receptors, A1 , A2A , A2B , and A3 . Although adenosine exerts clear neuroprotective effects through A1 receptors during ischemia, the use of selective A1 receptor agonists is hampered by their undesirable peripheral side effects...
2018: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/29740319/pharmacological-blockade-of-adenosine-a-2a-but-not-a-1-receptors-enhances-goal-directed-valuation-in-satiety-based-instrumental-behavior
#9
Yan Li, Xinran Pan, Yan He, Yang Ruan, Linshan Huang, Yuling Zhou, Zhidong Hou, Chaoxiang He, Zhe Wang, Xiong Zhang, Jiang-Fan Chen
The balance and smooth shift between flexible, goal-directed behaviors and repetitive, habitual actions are critical to optimal performance of behavioral tasks. The striatum plays an essential role in control of goal-directed versus habitual behaviors through a rich interplay of the numerous neurotransmitters and neuromodulators to modify the input, processing and output functions of the striatum. The adenosine receptors (namely A2A R and A1 R), with their high expression pattern in the striatum and abilities to interact and integrate dopamine, glutamate and cannabinoid signals in the striatum, may represent novel therapeutic targets for modulating instrumental behavior...
2018: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/29731713/cytokine-induced-killer-cells-express-cd39-cd38-cd203a-cd73-ectoenzymes-and-p1-adenosinergic-receptors
#10
Alberto L Horenstein, Antonella Chillemi, Roberta Zini, Valeria Quarona, Nicoletta Bianchi, Rossella Manfredini, Roberto Gambari, Fabio Malavasi, Davide Ferrari
Cytokine-induced killer (CIK) cells, a heterogeneous T cell population obtained by in vitro differentiation of peripheral blood mononuclear cells (PBMC), represent a promising immunological approach in cancer. Numerous studies have explored the role of CD38, CD39, CD203a/PC-1, and CD73 in generating extracellular adenosine (ADO) and thus in shaping the tumor niche in favor of proliferation. The findings shown here reveal that CIK cells are able to produce extracellular ADO via traditional (CD39/CD73) and/or alternative (CD38/CD203a/CD73 or CD203a/CD73) pathways...
2018: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/29730168/adenosine-a-2a-receptor-blockade-attenuates-spatial-memory-deficit-and-extent-of-demyelination-areas-in-lyolecithin-induced-demyelination-model
#11
Atefeh Akbari, Mohsen Khalili-Fomeshi, Manouchehr Ashrafpour, Ali Akbar Moghadamnia, Maryam Ghasemi-Kasman
In recent years, inactivation of A2A adenosine receptors has been emerged as a novel strategy for treatment of several neurodegenerative diseases. Although numerous studies have shown the beneficial effects of A2A receptors blockade on spatial memory, the impacts of selective adenosine A2A receptors on memory performance has not yet been examined in the context of demyelination. In the present study, we evaluated the effect of A2A receptor antagonist SCH58261 on spatial memory and myelination in an experimental model of focal demyelination in rat fimbria...
May 3, 2018: Life Sciences
https://www.readbyqxmd.com/read/29729889/the-inflammatory-state-of-adipose-tissue-is-not-affected-by-the-anti-inflammatory-response-of-the-a2a-adenosine-system-and-mir-221-pten
#12
J D Cortés-Garcia, M Briones-Espinoza, M Vega-Cárdenas, V M Ruíz-Rodríguez, A Mendez-Mancilla, Arturo E Gómez-Otero, J M Vargas Morales, M H García-Hernández, D P Portales-Pérez
Obesity is a chronic inflammatory state with cytokines, adipokines, and miRNAs. The A2a-adenosine system decreases activation and cytokine release in immune cells. MiR-221 is upregulated in carcinogenesis and inflammatory processes, where its targets PTEN and ETS-1, negatively regulates the Akt pathway and induces the release of pro-inflammatory cytokines, respectively. However, the roles of the A2a-adenosine system and miR-221 in adipose tissue are unknown. The aim of this work was to evaluate the A2a-adenosine and miRNA pathways as immune modulators in adipose tissue...
May 3, 2018: International Journal of Biochemistry & Cell Biology
https://www.readbyqxmd.com/read/29726815/cryo-em-structure-of-the-adenosine-a-2a-receptor-coupled-to-an-engineered-heterotrimeric-g-protein
#13
Javier García-Nafría, Yang Lee, Xiaochen Bai, Byron Carpenter, Christopher G Tate
The adenosine A2A receptor (A2A R) is a prototypical G protein-coupled receptor (GPCR) that couples to the heterotrimeric G protein GS . Here we determine the structure by electron cryo-microscopy (cryo-EM) of A2A R at pH 7.5 bound to the small molecule agonist NECA and coupled to an engineered heterotrimeric G protein, which contains mini-GS , the βγ subunits and nanobody Nb35. Most regions of the complex have a resolution of ~3.8 Å or better. Comparison with the 3.4 Å resolution crystal structure shows that the receptor and mini-GS are virtually identical and that the density of the side chains and ligand are of comparable quality...
May 4, 2018: ELife
https://www.readbyqxmd.com/read/29720380/car-t-cells-surface-engineered-with-drug-encapsulated-nanoparticles-can-ameliorate-intratumoral-t-cell-hypofunction
#14
Natnaree Siriwon, Yu Jeong Kim, Elizabeth Louise Siegler, Xianhui Chen, Jennifer A Rohrs, Yarong Liu, Pin Wang
One limiting factor of CAR T-cell therapy for treatment of solid cancers is the suppressive tumor microenvironment, which inactivates the function of tumor infiltrating lymphocytes (TILs) through the production of immunosuppressive molecules such as adenosine. Adenosine inhibits the function of CD4+ and CD8+ T cells by binding to and activating the A2a adenosine receptor (A2aR) expressed on their surface. This suppression pathway can be blocked using the A2aR-specific small molecule antagonist SCH-58261 (SCH), but its applications have been limited owing to difficulties delivering this drug to immune cells within the tumor microenvironment (TME)...
May 2, 2018: Cancer Immunology Research
https://www.readbyqxmd.com/read/29717153/cystatin-f-involvement-in-adenosine-a-2a-receptor-mediated-neuroinflammation-in-bv2-microglial-cells
#15
Wei Duan, Haoxiang Wang, Qinlin Fan, Lin Chen, Heqing Huang, Hong Ran
Our previous studies have shown adenosine A2A R activation markedly promotes the expression of cystatin F (CF) and exacerbates the white matter lesions induced by hypoxic brain injuries. Thus, we hypothesized that CF was probably involved in neuroinflammation of activated microglia induced by A2A R activation. We transfected the BV2 cells with a CF shRNA vector and examined the production of pro-inflammatory cytokines in hypoxic-BV2 cells in which A2A R was activated or inactivated to confirm this hypothesis...
May 1, 2018: Scientific Reports
https://www.readbyqxmd.com/read/29713276/amyotrophic-lateral-sclerosis-als-and-adenosine-receptors
#16
REVIEW
Ana M Sebastião, Nádia Rei, Joaquim A Ribeiro
In the present review we discuss the potential involvement of adenosinergic signaling, in particular the role of adenosine receptors, in amyotrophic lateral sclerosis (ALS). Though the literature on this topic is not abundant, the information so far available on adenosine receptors in animal models of ALS highlights the interest to continue to explore the role of these receptors in this neurodegenerative disease. Indeed, all motor neurons affected in ALS are responsive to adenosine receptor ligands but interestingly, there are alterations in pre-symptomatic or early symptomatic stages that mirror those in advanced disease stages...
2018: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/29702147/adenosine-signalling-and-the-immune-system-when-a-lot-could-be-too-much
#17
REVIEW
Luca Antonioli, Matteo Fornai, Corrado Blandizzi, Pál Pacher, György Haskó
Adenosine is increasingly recognized as a key mediator of the immune response. Signals delivered by extracellular adenosine are detected and transduced by G-protein-coupled cell-surface receptors, classified into four subtypes: A1 , A2A , A2B and A3 . These receptors, expressed virtually on all immune cells, modulate all aspects of immune/inflammatory responses. These immunoregulatory effects, which are mostly anti-inflammatory, contribute to the general tissue protective effects of adenosine and its receptors...
April 24, 2018: Immunology Letters
https://www.readbyqxmd.com/read/29693117/adenosine-a-2a-receptor-activation-reverses-hypoxia%C3%A2-induced-rat-pulmonary-artery-smooth-muscle-cell-proliferation-via-cyclic-amp%C3%A2-mediated-inhibition-of-the-sdf1%C3%A2-cxc4-signaling-pathway
#18
Yang Wang, Lei Ying, Ke-Ke Jin, Yan Nan, Suhua Hu, Xueqin Wu, Ruyi Qi, Xin Luo, Liangxing Wang
The occurrence and the subsequent development of pulmonary arterial hypertension (PAH) involve complicated mechanisms. Of these, the proliferation of pulmonary artery smooth muscle cells (PASMCs) has been indicated to be closely associated with its progression. Therefore, therapeutic methods targeting PASMCs to inhibit proliferation is an effective method for alleviating PAH. The present study was designed to determine the role of the adenosine A(2A) receptor (A2A receptor) in hypoxia‑induced rat PASMC (RPASMC) proliferation...
April 16, 2018: International Journal of Molecular Medicine
https://www.readbyqxmd.com/read/29692361/a-defect-in-kca3-1-channel-activity-limits-the-ability-of-cd8-t-cells-from-cancer-patients-to-infiltrate-an-adenosine-rich-microenvironment
#19
Ameet A Chimote, Andras Balajthy, Michael J Arnold, Hannah S Newton, Peter Hajdu, Julianne Qualtieri, Trisha Wise-Draper, Laura Conforti
The limited ability of cytotoxic T cells to infiltrate solid tumors hampers immune surveillance and the efficacy of immunotherapies in cancer. Adenosine accumulates in solid tumors and inhibits tumor-specific T cells. Adenosine inhibits T cell motility through the A2A receptor (A2A R) and suppression of KCa3.1 channels. We conducted three-dimensional chemotaxis experiments to elucidate the effect of adenosine on the migration of peripheral blood CD8+ T cells from head and neck squamous cell carcinoma (HNSCC) patients...
April 24, 2018: Science Signaling
https://www.readbyqxmd.com/read/29692248/a2a-adenosine-receptor-antagonists-as-therapeutic-candidates-are-they-still-an-interesting-challenge
#20
Barbara Cacciari, Stephanie Federico, Giampiero Spalluto
In the past decades, many efforts were done to develope ligands for the adenosine receptors, with the purpose to individuate agonists and antagonists affine and selective for each subtypes , named A1, A2A, A2B, and A3. These intense studies allowed a deeper and deeper knowledge of the nature and, moreover, of the pathophysiological roles of all the adenosine receptor subtypes. In particular, the involvment of the A2A adenosine receptor subtype in some physiological mechanisms in the brain, that could be related to important diseases such as the Parkinson's disease, encouraged the research in this field...
April 22, 2018: Mini Reviews in Medicinal Chemistry
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