The molecular basis of G protein–coupled receptor activation
WI Weis, BK Kobilka - Annual review of biochemistry, 2018 - annualreviews.org
G protein–coupled receptors (GPCRs) mediate the majority of cellular responses to external
stimuli. Upon activation by a ligand, the receptor binds to a partner heterotrimeric G protein …
stimuli. Upon activation by a ligand, the receptor binds to a partner heterotrimeric G protein …
Microbial and animal rhodopsins: structures, functions, and molecular mechanisms
OP Ernst, DT Lodowski, M Elstner, P Hegemann… - Chemical …, 2014 - ACS Publications
Organisms of all domains of life use photoreceptor proteins to sense and respond to light.
The light-sensitivity of photoreceptor proteins arises from bound chromophores such as …
The light-sensitivity of photoreceptor proteins arises from bound chromophores such as …
[HTML][HTML] Structural insights into the dynamic process of β2-adrenergic receptor signaling
G-protein-coupled receptors (GPCRs) transduce signals from the extracellular environment
to intracellular proteins. To gain structural insight into the regulation of receptor cytoplasmic …
to intracellular proteins. To gain structural insight into the regulation of receptor cytoplasmic …
GPCR drug discovery: integrating solution NMR data with crystal and cryo-EM structures
I Shimada, T Ueda, Y Kofuku, MT Eddy… - Nature Reviews Drug …, 2019 - nature.com
The 826 G protein-coupled receptors (GPCRs) in the human proteome regulate key
physiological processes and thus have long been attractive drug targets. With the crystal …
physiological processes and thus have long been attractive drug targets. With the crystal …
Activation of the A2A adenosine G-protein-coupled receptor by conformational selection
Conformational selection and induced fit are two prevailing mechanisms, to explain the
molecular basis for ligand-based activation of receptors. G-protein-coupled receptors are the …
molecular basis for ligand-based activation of receptors. G-protein-coupled receptors are the …
Allosteric coupling of drug binding and intracellular signaling in the A2A adenosine receptor
Signaling across cellular membranes, the 826 human G protein-coupled receptors (GPCRs)
govern a wide range of vital physiological processes, making GPCRs prominent drug …
govern a wide range of vital physiological processes, making GPCRs prominent drug …
Nanobodies to study G protein–coupled receptor structure and function
Ligand-induced activation of G protein–coupled receptors (GPCRs) is a key mechanism
permitting communication between cells and organs. Enormous progress has recently …
permitting communication between cells and organs. Enormous progress has recently …
Propagation of conformational changes during μ-opioid receptor activation
R Sounier, C Mas, J Steyaert, T Laeremans, A Manglik… - Nature, 2015 - nature.com
Abstract µ-Opioid receptors (µORs) are G-protein-coupled receptors that are activated by a
structurally diverse spectrum of natural and synthetic agonists including endogenous …
structurally diverse spectrum of natural and synthetic agonists including endogenous …
Mechanistic insights into allosteric regulation of the A2A adenosine G protein-coupled receptor by physiological cations
Cations play key roles in regulating G-protein-coupled receptors (GPCRs), although their
mechanisms are poorly understood. Here, 19F NMR is used to delineate the effects of …
mechanisms are poorly understood. Here, 19F NMR is used to delineate the effects of …
The role of protein dynamics in GPCR function: insights from the β2AR and rhodopsin
G protein-coupled receptors (GPCRs) are versatile signaling proteins that mediate complex
cellular responses to hormones and neurotransmitters. Recent advances in GPCR …
cellular responses to hormones and neurotransmitters. Recent advances in GPCR …