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Studying the Diffusion Characteristics of Different Activity States of the Human Adenosine-A3 Receptor Using Fluorescence Correlation Spectroscopy

Ross Corriden, Leigh Stoddart, Stephen Briddon, Stephen J. Hill
2010 Biophysical Journal  
An activation mechanism emerges whereby conformational substates depend on a multivariate energy landscape encompassing retinal and protein dynamics as well as lipid bilayer interactions. [1] M.  ...  Significant details are now emerging that give new insights into rhodopsin activation and complement FTIR and spin-label approaches. 1509-Pos Multi-Scale Dynamics of Rhodopsin Activation as a Paradigm  ...  Compared with our previous molecular dynamics (MD) studies of the inactive states of rhodopsin 1 and b 2 -adrenergic receptor, 2 these new simulations shed light on the role of the protonation state of  ... 
doi:10.1016/j.bpj.2009.12.1578 fatcat:yrrlc7stdjg67febpgknstodua

Docking studies of agonists and antagonists suggest an activation pathway of the A3 adenosine receptor

Soo-Kyung Kim, Zhan-Guo Gao, Lak Shin Jeong, Kenneth A. Jacobson
2006 Journal of Molecular Graphics and Modelling  
By analogy, outward rotation of the W6.48 side-chain upon activation of an internally-crosslinking mutant M 3 muscarinic receptor was indicated by constrained molecular dynamics (MD).  ...  Structural determinants of ligand efficacy in the human A 3 adenosine receptor (AR) were studied using pharmacophore and docking analyses of various categories of A 3 selective ligands: inverse agonist  ...  Acknowledgements This research was supported by the Intramural Research Program of the NIH, National Institute of Diabetes and Digestive and Kidney Diseases. We thank Dr.  ... 
doi:10.1016/j.jmgm.2006.05.004 pmid:16793299 pmcid:PMC6262875 fatcat:cpo4irjcinesbdqfcup3vu6otq

Structural Mapping of Adenosine Receptor Mutations: Ligand Binding and Signaling Mechanisms

Willem Jespers, Anke C. Schiedel, Laura H. Heitman, Robert M. Cooke, Lisa Kleene, Gerard J.P. van Westen, David E. Gloriam, Christa E. Müller, Eddy Sotelo, Hugo Gutiérrez-de-Terán
2018 TIPS - Trends in Pharmacological Sciences  
The latter group is where we find the four receptors activated by adenosine, consisting of the A1, A2A, A2B and A3 adenosine receptors (ARs) [4].  ...  of the A2A and inactive conformations of the A1 adenosine receptor.  ...  mutations and ligands that stabilize intermediate conformational states are needed to fully understand the activation mechanism.  ... 
doi:10.1016/j.tips.2017.11.001 pmid:29203139 fatcat:thrcikgx3vbirf6g43mwn3zunu

Common activation mechanism of class A GPCRs

Qingtong Zhou, Dehua Yang, Meng Wu, Yu Guo, Wangjing Guo, Li Zhong, Xiaoqing Cai, Antao Dai, Wonjo Jang, Eugene I Shakhnovich, Zhi-Jie Liu, Raymond C Stevens (+4 others)
2019 eLife  
Site-directed mutagenesis experiments support this proposition and reveal that rational mutations of residues in this pathway can be used to obtain receptors that are constitutively active or inactive.  ...  Understanding receptor activation mechanism is critical for discovering novel therapeutics since about one-third of all marketed drugs target members of this family.  ...  A 2A receptor (A 2A R), k-opioid receptor (k-OR) and adenosine A 1A receptor (A 1A R), the active state structure of which was recently determined by cryo-EM.  ... 
doi:10.7554/elife.50279 pmid:31855179 pmcid:PMC6954041 fatcat:3ocfjuetyjc7xohh76vty7l2la

Mechanisms controlling vacuolar H+-adenosine triphosphatase activity: targets for the development of new therapeutic agents for the management of osteoporosis

L. Shannon Holliday, Huynh, Zuo, Toro
2013 Research and Reports in Biochemistry  
Links between controlling mechanisms and subunit a3 have been identified, suggesting that it may be possible to develop agents that disrupt bone resorptive V-ATPase activity while leaving the housekeeping  ...  Recent genetic studies show that mutations in vacuolar H + -adenosine triphosphatase (V-ATPase) subunit isoforms that are selectively expressed in osteoclasts (a3 and d2) lead to both reduced bone resorption  ...  Dr Toro was supported by National Institutes of Health grant T32 DE07200-15 from NIDCR. Disclosure The authors report no conflicts of interest in this work.  ... 
doi:10.2147/rrbc.s28414 fatcat:znammzlttzh7hb6mbcumckulie

Epigenetic mechanisms of hypoxic preconditioning

Elena Rybnikova, Mikhail Samoilov
2015 SpringerPlus  
the University of Paris-Est Creteil (CHORM) and a European Fellowship (Marie Curie IEF).  ...  by the National Epilepsy Fund -"Power of the Small", the Hersenstichting Nederland (NEF 013-1) and Acknowledgements This work has been fi nanced by Estonian Ministry Acknowledgements Funded by GGET.  ...  The adenosine A3 receptor (A3AR) has emerged as a potential target.  ... 
doi:10.1186/2193-1801-4-s1-l39 pmid:27386200 pmcid:PMC4798112 fatcat:jd7laoli5ncmrkcbbedcutz65e

The Activation Mechanism of 2′-5′-Oligoadenylate Synthetase Gives New Insights Into OAS/cGAS Triggers of Innate Immunity

Jan Lohöfener, Nicola Steinke, Penelope Kay-Fedorov, Petra Baruch, Alexey Nikulin, Svetlana Tishchenko, Dietmar J. Manstein, Roman Fedorov
2015 Structure  
state.  ...  Highlights d OAS activation involves a sequential mechanism d Individual roles of dsRNA and substrates in OAS activation are defined d The orientation of the AMP acceptor induces the 2 0 -specificity of  ...  .), and the Program of RAS on Molecular and Cellular Biology (S.T. and A.N.).  ... 
doi:10.1016/j.str.2015.03.012 pmid:25892109 fatcat:cp5kgpqv7jcwzhf6dtj44rzk2a

WNT signaling mechanisms in nociception and sensitization of afferent neurons

Manuela Simonetti
2015 SpringerPlus  
the University of Paris-Est Creteil (CHORM) and a European Fellowship (Marie Curie IEF).  ...  by the National Epilepsy Fund -"Power of the Small", the Hersenstichting Nederland (NEF 013-1) and Acknowledgements This work has been fi nanced by Estonian Ministry Acknowledgements Funded by GGET.  ...  The adenosine A3 receptor (A3AR) has emerged as a potential target.  ... 
doi:10.1186/2193-1801-4-s1-l48 pmid:27386210 pmcid:PMC4798463 fatcat:dkkql2iixzai5k7dfot36k5dde

Mechanisms of mitochondrial quality control in autosomal recessive Parkinson's disease

Olga Corti
2015 SpringerPlus  
the University of Paris-Est Creteil (CHORM) and a European Fellowship (Marie Curie IEF).  ...  by the National Epilepsy Fund -"Power of the Small", the Hersenstichting Nederland (NEF 013-1) and Acknowledgements This work has been fi nanced by Estonian Ministry Acknowledgements Funded by GGET.  ...  The adenosine A3 receptor (A3AR) has emerged as a potential target.  ... 
doi:10.1186/2193-1801-4-s1-l36 pmid:27057479 pmcid:PMC4796103 fatcat:nyulkcdx6ncyjjmm2q6sh6unqm

Mitophagy programs: mechanisms and physiological implications of mitochondrial targeting by autophagy

Anne Hamacher-Brady, Nathan Ryan Brady
2015 Cellular and Molecular Life Sciences (CMLS)  
Recent work has revealed multiple mitophagy programs that operate independently or undergo crosstalk, and require modulated autophagy receptor activities at outer membranes of mitochondria.  ...  Here, we review these mitophagy programs, focusing on pathway mechanisms which recognize and target mitochondria for sequestration by autophagosomes, as well as mechanisms controlling pathway activities  ...  Monitoring mitophagy receptor activity using LC3 immunoprecipitation Finally, a critical tool in the analysis of LIR receptor activities is the immunoprecipitation of tagged-LC3, and analysis of coprecipitated  ... 
doi:10.1007/s00018-015-2087-8 pmid:26611876 pmcid:PMC4735260 fatcat:4horpo3zinhk5eii4yw744i6kq

Extracellular ATP and adenosine induce cell apoptosis of human hepatoma Li-7A cellsviathe A3 adenosine receptor

Long T Wen, Aileen F Knowles
2003 British Journal of Pharmacology  
The mechanism of ATP-elicited cytotoxicity is not fully understood.  ...  Using adenosine receptor agonists and antagonists, as well as inhibitors of adenosine transport and deamination, we showed that the cytotoxic effect of adenosine is specifically mediated by the A3 receptor  ...  The cytotoxic effect of adenosine is mediated by the A3 adenosine receptor. Ligand binding to the receptor activates caspase-3, leading to apoptosis.  ... 
doi:10.1038/sj.bjp.0705523 pmid:14530217 pmcid:PMC1574113 fatcat:j6j2boegvner3ftmmsoefx42lu

The Novel Application of Geometric Morphometrics with Principal Component Analysis to Existing G Protein-Coupled Receptor (GPCR) Structures

Daniel N. Wiseman, Nikita Samra, María Monserrat Román Lara, Samantha C. Penrice, Alan D. Goddard
2021 Pharmaceuticals  
The G protein-coupled receptor (GPCR) superfamily is a large group of membrane proteins which, because of their vast involvement in cell signalling pathways, are implicated in a plethora of disease states  ...  Despite advances in techniques to study these receptors, current prophylaxis is often limited due to the challenging nature of their dynamic, complex structures.  ...  Activation State-The β2-Adrenergic Receptors GPCR activation largely relies upon ligand binding, and so this was the first analysis performed; additionally, the active, intermediate and inactive states  ... 
doi:10.3390/ph14100953 pmid:34681177 fatcat:yhkxh3f7szd4japcndkiabzjye

Hypoxic exosomes orchestrate tumorigenesis: molecular mechanisms and therapeutic implications

Reza Jafari, Reza Rahbarghazi, Mahdi Ahmadi, Mehdi Hassanpour, Jafar Rezaie
2020 Journal of Translational Medicine  
Understanding the detailed mechanisms involved in biogenesis and functions of exosomes under hypoxic conditions may help to develop effective therapies against cancer.  ...  Hypoxic tumor cells undergo broadly metabolic and molecular adaptations and communicate with surrounding cells to provide conditions promising for their homeostasis and metastasis.  ...  Authors' contributions RJ and JR conceived the ideas. JR, MA and MH collected data. RR and JR designed and reviewed the manuscript. All authors reviewed the manuscript.  ... 
doi:10.1186/s12967-020-02662-9 pmid:33302971 fatcat:kfj4xvv2ozh5zg47qvg65ot7ny

Molecular mechanisms of cell proliferation induced by low power laser irradiation

Xuejuan Gao, Da Xing
2009 Journal of Biomedical Science  
Low power laser irradiation (LPLI) promotes proliferation of multiple cells, which (especially red and near infrared light) is mainly through the activation of mitochondrial respiratory chain and the initiation  ...  Activated TPKR could activate its downstream signaling elements, like Ras/Raf/MEK/ ERK, PI3K/Akt/eIF4E, PI3K/Akt/eNOS and PLC-gamma/PKC pathways.  ...  Acknowledgements This research is supported by the National Natural Science Foundation of China (30627003; 30870676) and the Natural Science Foundation of Guangdong Province (7117865).  ... 
doi:10.1186/1423-0127-16-4 pmid:19272168 pmcid:PMC2644974 fatcat:olmhmsyumrc65dxr4roqokccdi

Elucidating the mechanisms of TDP-43 aggregation in a cellular model of motor neuron disease

David Hicks, Marcus Rattray
2015 SpringerPlus  
the University of Paris-Est Creteil (CHORM) and a European Fellowship (Marie Curie IEF).  ...  by the National Epilepsy Fund -"Power of the Small", the Hersenstichting Nederland (NEF 013-1) and Acknowledgements This work has been fi nanced by Estonian Ministry Acknowledgements Funded by GGET.  ...  The adenosine A3 receptor (A3AR) has emerged as a potential target.  ... 
doi:10.1186/2193-1801-4-s1-l23 pmid:27386186 pmcid:PMC4797578 fatcat:53brszlm5fe7bfv5s4rjvgvuaq
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