High-resolution crystal structure of an engineered human beta2-adrenergic G protein-coupled receptor.

By Vadim Cherezov, D. Rosenbaum, M. Hanson, S. Rasmussen, Foon Sun Thian, T. S. Kobilka, Hee-Jung Choi, P. Kuhn, William I. Weis, Brian K. Kobilka and 1 more. 2007

727 citations recorded by the source corpus.

Subfields: Computational Biology & Bioinformatics

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Citations in the corpus

TonB-dependent transporters: regulation, structure, and function (2010, background): “This work confirms that lipidic cubic phase crystallization could be as useful for the crystallization of β-barrel outer membrane proteins as it is for α-helical inner membrane proteins (14).”
G protein-coupled receptors: structure- and function-based drug discovery (2021, background): “The first crystal structure of GPCR extracted from exogenously expressed host cells, the human β2-adrenergic receptor (β2AR, gene name: ADRB2) bound to an antagonist, was disclosed in 2007, representing a milestone in GPCR structural biology.(7) Several innovative methods, especially the incorporati”
Structure-based drug discovery and protein targets in the CNS. (2011, methodology): “, 2008), an additional domain (Cherezov et al., 2007) or complexation with antibody (Rosenbaum et al.”
Structure-Function of the G-protein-Coupled Receptor Superfamily (2012, methodology): “Structures of inactive R (PDB code 2RH1, gray) (27), nanobody-bound R* (PDB code 3P0G, yellow) (22) and G protein-bound R*G (PDB code 3SN6, orange) (21) states are superimposed at the extracellular part of the helix above Pro2886.”
A glimpse of structural biology through X-ray crystallography. (2014, background): “, 2000), crystal structures of the recombinant G-protein-coupled receptor (GPCR) were reported on b2 adrenergic receptor (Cherezov et al., 2007; Rasmussen et al., 2007).”
GOMoDo: A GPCRs Online Modeling and Docking Webserver (2013, neutral): “(PDB code: 2RH1 [46]).”
Ultrafast neuronal imaging of dopamine dynamics with designed genetically encoded sensors (2018, methodology): “Primary sequence of sensor design was threaded with partial thread routine onto template PDB structures of inactive β2 adrenergic receptor (41) (ID: 2RH1) and unbound state of GCaMP3 (42) (ID: 4IK3).”
Computational modeling of membrane proteins (2014, background): “8 Comparably long timescales were required for the breakthroughs in GPCR structure determination, which started with the crystal structure of b -AR,9 after many years of failed crystallization trials.”
Using Sequence Similarity Networks for Visualization of Relationships Across Diverse Protein Superfamilies (2009, background): “The sequences that are associated with or that are extremely similar to high resolution structures are noted [PDB identifiers 1F88[22], 2VT4[23], 3EML[26], 2RH1[24], and 2R4R[25]].”
Structural insights into the dynamic process of β2-adrenergic receptor signaling (2015, neutral): “…the b2AR have provided high-resolution insight into two conformations associated with GPCR function: an inactive, inverse agonist-bound state and the active state in complex with an agonist and the G protein Gs (Cherezov et al., 2007; Rasmussen et al., 2007, 2011a, 2011b; Rosenbaum et al., 2007).”
Status of GPCR modeling and docking as reflected by community-wide GPCR Dock 2010 assessment (2011, neutral): “, 2008) forms; human b2 (Cherezov et al., 2007) and turkey b1 (Warne et al.”
Loss of constitutive activity is correlated with increased thermostability of the human adenosine A2A receptor (2013, background): “…the development of GPCR fusion proteins, where a T4 lysozyme replaces the conformationally dynamic third intracellular loop (ICL3), for example (Cherezov et al., 2007; Jaakola et al., 2008; Chien et al., 2010; Wu et al., 2010; 2012; Shimamura et al., 2011; Xu et al., 2011; Granier et al.,…”
Modern homology modeling of G-protein coupled receptors: which structural template to use? (2009, background): “The second structure of Hs_Adrb2 was obtained by protein engineering, replacing the IC3 loop sequence from Q230 to S262 with a well folded soluble protein, T4-lysozyme 15.”
5-HT2C Receptor Structures Reveal the Structural Basis of GPCR Polypharmacology (2018, neutral): “Additionally, carazolol and tiotropium exert their therapeutic effects by interacting with multiple adrenergic (Cherezov et al., 2007; Moukhametzianov et al., 2011) and muscarinic acetylcholine receptors (Kruse et al., 2012; Thal et al., 2016), respectively.”
An Overview of the Top Ten Detergents Used for Membrane Protein Crystallization (2017, background): “, for photosynthetic proteins [3,4], transporters and channels [5–8], and GPCRs [9].”