Analysis of full and partial agonists binding to β2‐adrenergic receptor suggests a role of transmembrane helix V in agonist‐specific conformational changes
The 2.4 Å crystal structure of the β2‐adrenergic receptor (β2AR) in complex with the high‐
affinity inverse agonist (−)‐carazolol provides a detailed structural framework for the analysis …
affinity inverse agonist (−)‐carazolol provides a detailed structural framework for the analysis …
Conserved Binding Mode of Human β2 Adrenergic Receptor Inverse Agonists and Antagonist Revealed by X-ray Crystallography
D Wacker, G Fenalti, MA Brown, V Katritch… - Journal of the …, 2010 - ACS Publications
G protein-coupled receptors (GPCRs) represent a large fraction of current pharmaceutical
targets, and of the GPCRs, the β2 adrenergic receptor (β2AR) is one of the most extensively …
targets, and of the GPCRs, the β2 adrenergic receptor (β2AR) is one of the most extensively …
Structural basis for ligand binding and specificity in adrenergic receptors: implications for GPCR-targeted drug discovery
T Huber, S Menon, TP Sakmar - Biochemistry, 2008 - ACS Publications
Crystal structures of engineered human β2-adrenergic receptors (ARs) in complex with an
inverse agonist ligand, carazolol, provide three-dimensional snapshots of the disposition of …
inverse agonist ligand, carazolol, provide three-dimensional snapshots of the disposition of …
Identifying conformational changes of the β2 adrenoceptor that enable accurate prediction of ligand/receptor interactions and screening for GPCR modulators
The new β 2 Adrenoceptor (β 2 AR) crystal structures provide a high-resolution snapshot of
receptor interactions with two particular partial inverse agonists,(−)-carazolol and timolol …
receptor interactions with two particular partial inverse agonists,(−)-carazolol and timolol …
Ligand entry and exit pathways in the β2-adrenergic receptor
T Wang, Y Duan - Journal of molecular biology, 2009 - Elsevier
The recently determined crystal structure of the human β2-adrenergic (β2AR) G-protein-
coupled receptor provides an excellent structural basis for exploring β2AR–ligand binding …
coupled receptor provides an excellent structural basis for exploring β2AR–ligand binding …
Activation mechanism of the β2-adrenergic receptor
A third of marketed drugs act by binding to a G-protein-coupled receptor (GPCR) and either
triggering or preventing receptor activation. Although recent crystal structures have provided …
triggering or preventing receptor activation. Although recent crystal structures have provided …
[HTML][HTML] Ligand-stabilized conformational states of human β2 adrenergic receptor: insight into G-protein-coupled receptor activation
G-protein-coupled receptors (GPCRs) are known to exist in dynamic equilibrium between
inactive-and several active-state conformations, even in the absence of a ligand. Recent …
inactive-and several active-state conformations, even in the absence of a ligand. Recent …
[HTML][HTML] Ligand-dependent perturbation of the conformational ensemble for the GPCR β2 adrenergic receptor revealed by HDX
GM West, EYT Chien, V Katritch, J Gatchalian… - Structure, 2011 - cell.com
Mechanism of G protein-coupled receptor (GPCR) activation and their modulation by
functionally distinct ligands remains elusive. Using the technique of amide …
functionally distinct ligands remains elusive. Using the technique of amide …
Insights into the Role of Asp792.50 in β2 Adrenergic Receptor Activation from Molecular Dynamics Simulations
Achieving a molecular-level understanding of G-protein-coupled receptor (GPCR) activation
has been a long-standing goal in biology and could be important for the development of …
has been a long-standing goal in biology and could be important for the development of …
[HTML][HTML] Efficacy of the β2-adrenergic receptor is determined by conformational equilibrium in the transmembrane region
Y Kofuku, T Ueda, J Okude, Y Shiraishi… - Nature …, 2012 - nature.com
Many drugs that target G-protein-coupled receptors (GPCRs) induce or inhibit their signal
transduction with different strengths, which affect their therapeutic properties. However, the …
transduction with different strengths, which affect their therapeutic properties. However, the …