Assertion: adenosine | /r/HasProperty | a2a receptor
Facets:
Source sentences:
text: Antimetastatic effects of blocking PD-1 and the adenosine A2A receptor.
text: Caffeine also causes the release of dopamine in the dorsal striatum and nucleus accumbens core (a substructure within the ventral striatum), but not the nucleus accumbens shell, by antagonizing A 1 receptors in the axon terminal of dopamine neurons and A 1 –A 2A heterodimers (a receptor complex composed of 1 adenosine A 1 receptor and 1 adenosine A 2A receptor) in the axon terminal of glutamate neurons.
text: Potential therapeutic interest of adenosine A2A receptors in psychiatric disorders.
text: Caffeine promotes anti-tumor immune response during tumor initiation: involvement of the adenosine A2A receptor.
text: The structure of the adenosine A2A receptor described here provides new insight into the structural features which define the GPCR active state, the regions which interact with signal transduction proteins, and how receptors interact to form signalling complexes.
text: predicting the three-dimensional structural representation of the target protein, or part thereof, by modelling the structural representation on all or the selected coordinates of the adenosine A2A receptor.
text: It will be appreciated that in all aspects of the invention which utilise the coordinates of the adenosine A2A receptor, it is not necessary to utilise all the coordinates of Table (i), but merely a portion of them, e.g. a set of coordinates representing atoms of particular interest in relation to a particular use.
text: It is appreciated that the coordinates of the adenosine A2A receptor used in the invention may be optionally varied and a subset of the coordinates or the varied coordinates may be selected (and constitute selected coordinates).
text: All GPCRs are included in the scope of the invention and their structure may be modelled by using the coordinates of the adenosine A2A receptor.
text: Typically, modelling a structural representation of a target is done by homology modelling whereby homologous regions between the adenosine A2A receptor and the target protein are matched and the coordinate data of the adenosine A2A receptor used to predict a structural representation of the target protein.
text: Typically, modelling a structural representation of a target is done by homology modelling whereby homologous regions between the adenosine A2A receptor and the target protein are matched and the coordinate data of the adenosine A2A receptor used to predict a structural representation of the target protein.
text: we mean any adenosine A2A receptor which has at least 75% sequence identity with human adenosine A2A receptor as well as adenosine A2A receptors from other species and mutants thereof.
text: Preferably, the adenosine A2A receptor has at least 80% amino acid sequence identity to human adenosine A2A receptor, and more preferably at least 85%, 90%, 95% or 99% amino acid sequence identity.
text: For example, the binding partner may bind to the dimerisation interface or bind to another region of the adenosine A2A receptor which nevertheless modulates dimerisation.
text: Such conformational requirements include the overall three-dimensional structure and orientation of the binding partner in relation to all or a portion of the binding region, or the spacing between functional groups of a binding partner comprising several binding partners that directly interact with the adenosine A2A receptor.
text: For example the invention involves the computational screening of small molecule databases for binding partners that can bind in whole, or in part, to the adenosine A2A receptor.
text: If the theoretical structure of the given entity suggests insufficient interaction and association between it and the adenosine A2A receptor, testing of the entity is obviated.
text: Thus in a further embodiment of the third and fourth aspects of the invention, the methods further comprise the steps of obtaining or synthesising the one or more binding partners of an adenosine A∑A receptor; and optionally contacting the one or more binding partners with an adenosine A2A receptor to determine the ability of the one or more binding partners to interact with the adenosine A2A receptor.
text: Thus in a further embodiment of the third and fourth aspects of the invention, the methods further comprise the steps of obtaining or synthesising the one or more binding partners of an adenosine A∑A receptor; and optionally contacting the one or more binding partners with an adenosine A2A receptor to determine the ability of the one or more binding partners to interact with the adenosine A2A receptor.
text: Various methods known in the art may be used to determine binding between an adenosine A2A receptor and a binding partner including those described in
text: A 2 A receptor of Table (i), optionally varied by a root mean square deviation of residue backbone atoms of not more than 1.08 A, or selected coordinates thereof, are used to analyse the a crystal complex of the adenosine A2A receptor and binding partner.
text: Accordingly, a fifth aspect of the invention provides a method for the analysis of the interaction of one or more binding partners with adenosine A2A receptor, comprising: obtaining or synthesising one or more binding partners; forming one or more crystallised complexes of an adenosine Aa_, receptor and a binding partner; and analysing the one or more complexes by X-ray crystallography by employing the coordinates of the human adenosine A ¾ receptor structure, of Table (i), optionally varied by a root mean square deviation of residue backbone atoms of not more than 1.08 A, or selected coordinates thereof, to determine the ability of the one or more binding partners to interact with the adenosine A2A receptor.
text: A critical role of the adenosine A2A receptor in extrastriatal neurons in modulating psychomotor activity as revealed by opposite phenotypes of striatum and forebrain A2A receptor knock-outs.
text: Activation processes in ligand-activated G protein-coupled receptors: a case study of the adenosine A 2A receptor.
text: Caffeine also causes the release of dopamine in the dorsal striatum and nucleus accumbens core (a substructure within the ventral striatum), but not the nucleus accumbens shell, by antagonizing A 1 receptors in the axon terminal of dopamine neurons and A 1 –A 2A heterodimers (a receptor complex composed of 1 adenosine A 1 receptor and 1 adenosine A 2A receptor) in the axon terminal of glutamate neurons.