Results 21 to 30 of about 185,950 (192)
Differential Signaling Profiles of MC4R Mutations with Three Different Ligands [PDF]
, 2020 The melanocortin 4 receptor (MC4R) is a key player in hypothalamic weight regulation and energy expenditure as part of the leptin-melanocortin pathway. Mutations in this G protein coupled receptor (GPCR) are the most common cause for monogenetic obesity,
Annibale, Paolo +8 more
core +3 more sources
Pharmacological Research, 2022 Kappa opioid receptor (κOR) agonists lack the abuse liability and respiratory depression effects of clinically used mu opioid receptor (μOR) analgesics and are hypothesized to be safer alternatives.
Alexander R. French, Richard M. van Rijn
doaj +1 more source
A Potential Blueprint for the Design of Biased Ligands for Aminergic GPCRs
Medical Sciences Forum, 2022 G protein-coupled receptors (GPCRs) are omnipresent in the regulation of physiological processes and therefore account for the most prominent drug target class.
Marcel Bermudez
doaj +1 more source
Prefrontal signals precede striatal signals for biased credit assignment in motivational learning biases [PDF]
Nature CommunicationsAbstractActions are biased by the outcomes they can produce: Humans are more likely to show action under reward prospect, but hold back under punishment prospect. Such motivational biases derive not only from biased response selection, but also from biased learning: humans tend to attribute rewards to their own actions, but are reluctant to attribute ...
Algermissen, J +4 more
openaire +5 more sources
Paradigm of biased PAR1 (protease-activated receptor-1) activation and inhibition in endothelial cells dissected by phosphoproteomics [PDF]
, 2017 Thrombin is the key serine protease of the coagulation cascade and mediates cellular responses by activation of PARs (protease-activated receptors). The predominant thrombin receptor is PAR1, and in endothelial cells (ECs), thrombin dynamically regulates
Hoogendijk, Arie J. +7 more
core +2 more sources
The β-blocker Nebivolol Is a GRK/β-arrestin Biased Agonist [PDF]
, 2013 Nebivolol, a third generation β-adrenoceptor (β-AR) antagonist (β-blocker), causes vasodilation by inducing nitric oxide (NO) production. The mechanism via which nebivolol induces NO production remains unknown, resulting in the genesis of much of the ...
Andresen, Bradley T. +9 more
core +3 more sources
Bias-inducing allosteric binding site in mu-opioid receptor signaling
SN Applied Sciences, 2021 G-protein-biased agonism of the mu-opioid receptor (μ-OR) is emerging as a promising strategy in analgesia. A deep understanding of how biased agonists modulate and differentiate G-protein-coupled receptors (GPCR) signaling pathways and how this is ...
Andrés F. Marmolejo-Valencia +2 more
doaj +1 more source
Cytoprotective Activated Protein C Averts Nlrp3 Inflammasome–Induced Ischemia-Reperfusion Injury Via Mtorc1 Inhibition [PDF]
, 2017 Cytoprotection by activated protein C (aPC) after ischemia-reperfusion injury (IRI) is associated with apoptosis inhibition. However, IRI is hallmarked by inflammation, and hence, cell-death forms disjunct from immunologically silent apoptosis are, in ...
Al-Dabet, Moh\u27d Mohanad +16 more
core +2 more sources
Biased and G protein-independent signaling of chemokine receptors
Frontiers in Immunology, 2014 Biased signaling or functional selectivity occurs when a 7TM receptor preferentially activates one of several available pathways. It can be divided into three distinct forms: ligand bias, receptor bias, and tissue or cell bias, where it is mediated by ...
Anne eSteen +3 more
doaj +1 more source
Frontiers in Synaptic Neuroscience, 2018 The dopamine D2 receptor (D2R) is known to elicit effects through activating two major signaling pathways mediated by either G proteins (Gi/o) or β-arrestins.
Lani S. Chun +12 more
doaj +1 more source