G protein-coupled receptors are 7-pass transmembrane receptors that couple to heterotrimeric G proteins to mediate cellular responses to a diverse array of stimuli.
Alexander Bowitch+3 more
doaj +1 more source
Both Ligand- and Cell-Specific Parameters Control Ligand Agonism in a Kinetic Model of G Protein–Coupled Receptor Signaling [PDF]
G protein–coupled receptors (GPCRs) exist in multiple dynamic states (e.g., ligand-bound, inactive, G protein–coupled) that influence G protein activation and ultimately response generation. In quantitative models of GPCR signaling that incorporate these
Kinzer-Ursem, Tamara L.+1 more
core +3 more sources
Effects on Breathing of Agonists to μ-opioid or GABA\u3csub\u3eA\u3c/sub\u3e Receptors Dialyzed into the Ventral Respiratory Column of Awake and Sleeping Goats [PDF]
Pulmonary ventilation (V̇I) in awake and sleeping goats does not change when antagonists to several excitatory G protein-coupled receptors are dialyzed unilaterally into the ventral respiratory column (VRC).
Burgraff, Nicholas J.+7 more
core +1 more source
Probing the role of the cation–π interaction in the binding sites of GPCRs using unnatural amino acids [PDF]
We describe a general application of the nonsense suppression methodology for unnatural amino acid incorporation to probe drug–receptor interactions in functional G protein-coupled receptors (GPCRs), evaluating the binding sites of both the M2 muscarinic
Ballesteros+31 more
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G-Protein Coupled Receptors Targeted by Analgesic Venom Peptides
Chronic pain is a complex and debilitating condition associated with a large personal and socioeconomic burden. Current pharmacological approaches to treating chronic pain such as opioids, antidepressants and anticonvulsants exhibit limited efficacy in ...
James T. Daniel, Richard J. Clark
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Modelization of Thermal Fluctuations in G Protein-Coupled Receptors
We simulate the electrical properties of a device realized by a G protein coupled receptor (GPCR), embedded in its membrane and in contact with two metallic electrodes through which an external voltage is applied.
Akimov, V.+7 more
core +1 more source
Regulators of G protein signalling proteins in the human myometrium [PDF]
The contractile state of the human myometrium is controlled by extracellular signals that promote relaxation or contraction. Many of these signals function through G proteincoupled receptors at the cell surface, stimulating heterotrimeric G proteins and ...
Abramow-Newerly+52 more
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Cloning, characterization and expression of a G-protein-coupled receptor from Lymnaea stagnalis and identification of a leucokinin-like peptide, PSFHSWS amide as its endogenous ligand. [PDF]
Neuropeptides are known to be important signaling molecules in several neural systems of the pond snailLymnaea stagnalis. Although the functions of these peptides have been studied in many neurons, the nature of the postsynaptic signal transduction is ...
Burke, J.F.+7 more
core +6 more sources
Fusion protein strategies for cryo-EM study of G protein-coupled receptors
Here, Zhang et al. explore fusion protein strategies to facilitate cryo-EM structural studies of GPCRs alone- without signal transducers- in ligand bound or unliganded form.
Kaihua Zhang+4 more
doaj +1 more source
The tyrosine phosphatase CD148 is an essential positive regulator of platelet activation and thrombosis [PDF]
Platelets play a fundamental role in hemostasis and thrombosis. They are also involved in pathologic conditions resulting from blocked blood vessels, including myocardial infarction and ischemic stroke.
Abtahian+79 more
core +2 more sources