Slow conformational dynamics of the human A2A adenosine receptor are temporally ordered
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In this article , the authors used total internal reflection fluorescence (TIRF) imaging to investigate the conformational dynamics of the human A2A adenosine receptor (A2AAR), a class A G protein-coupled receptor (GPCR), at the single-molecule level.About:
This article is published in Structure.The article was published on 2022-03-01 and is currently open access. It has received 12 citations till now. The article focuses on the topics: Total internal reflection fluorescence microscope & Fluorescence.read more
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Production of human A2AAR in lipid nanodiscs for 19F-NMR and single-molecule fluorescence spectroscopy
TL;DR: Wei et al. as discussed by the authors described the human A2A adenosine receptor (A2AAR), a class A G protein-coupled receptor (GPCR) for 19F-NMR and single-molecule fluorescence spectroscopy.
Journal ArticleDOI
Dynamics and Mechanistic Underpinnings to Pharmacology of Class A GPCRs - An NMR Perspective.
Shuya K. Huang,R. Scott Prosser +1 more
TL;DR: The structural aspects of GPCR activation and the various pharmacological models that capture aspects of receptor signaling behaviour are described, focusing on class A receptors and insights derived from nuclear magnetic resonance (NMR) and other spectroscopic techniques.
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Sub-millisecond conformational dynamics of the A2A adenosine receptor revealed by single-molecule FRET
TL;DR: In this article , the authors used single-molecule Förster Resonance Energy Transfer (smFRET) to quantify dynamics for individual protein molecules; however, its application to GPCRs is challenging.
Journal ArticleDOI
Conformational fingerprinting of allosteric modulators in metabotropic glutamate receptor 2
TL;DR: In this paper , fluorescence resonance energy transfer (FRET) sensors were used to quantify receptor modulation at each of the three structural domains of the metabotropic glutamate receptor 2 (mGluR2).
Journal ArticleDOI
Anionic Phospholipids Control Mechanisms of GPCR-G Protein Recognition
Naveen Thakur,Arka Ray,Liam Sharp,Beining Jin,Alexander Duong,Niloofar Gopal Pour,Samuel Obeng,Anuradha V. Wijesekara,Zhan-Guo Gao,Christopher R. McCurdy,Kenneth A. Jacobson,Edward Lyman,Matthew T. Eddy +12 more
TL;DR: In this paper , the authors explore the impact of anionic lipids on the function-related conformational equilibria of the human A 2A adenosine receptor (A 2A AR) in bilayers containing defined mixtures of zwitterionic and anionic phospholipids.
References
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TL;DR: The dynamical steady-state probability density is found in an extended phase space with variables x, p/sub x/, V, epsilon-dot, and zeta, where the x are reduced distances and the two variables epsilus-dot andZeta act as thermodynamic friction coefficients.
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LINCS : A linear constraint solver for molecular simulations
TL;DR: Although the derivation of the algorithm is presented in terms of matrices, no matrix matrix multiplications are needed and only the nonzero matrix elements have to be stored, making the method useful for very large molecules.
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Relationship between the inhibition constant (K1) and the concentration of inhibitor which causes 50 per cent inhibition (I50) of an enzymatic reaction.
TL;DR: The analysis described shows K I does not equal I 50 when competitive inhibition kinetics apply; however, K I is equal to I 50 under conditions of either noncompetitive or uncompetitive kinetics.
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