Results 21 to 30 of about 187,893 (285)

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, Biebermann, Heike, Dimitriou, Ioanna Maria, Krude, Heiko, Kühnen, Peter, Lohse, Martin J., Paisdzior, Sarah, Scheerer, Patrick, Schöpe, Paul Curtis   +8 more
core   +3 more sources

An updated assessment of the translational promise of G-protein-biased kappa opioid receptor agonists to treat pain and other indications without debilitating adverse effects

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

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., Bastepe, Murat, Blessing, Christopher P., Erickson, Catherine E., Gul, Rukhsana, Holowka, David, Jackson, Edwin K., Liu, Tammy, Nguyen, Jenny, Pulakat, Lakshmi   +9 more
core   +6 more sources

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

Biased regulation of glucocorticoid receptors signaling

Biomedicine & Pharmacotherapy, 2023
Glucocorticoids (GCs), steroid hormones that depend on glucocorticoid receptor (GR) binding for their action, are essential for regulating numerous homeostatic functions in the body.GR signals are biased, that is, GR signals are various in different tissue cells, disease states and ligands.
LIjuan Mao, jingyu chen, Wei Wei
openaire   +2 more sources

Shining light on location-biased cAMP signaling [PDF]

Journal of Biological Chemistry, 2021
cAMP is the indispensable second messenger regulating cell metabolism and function in response to extracellular hormones and neurotransmitters. cAMP is produced via the activation of G protein-coupled receptors located at both the cell surface and inside the cell. Recently, Tsvetanova et al. explored cAMP generation in distinct locations and the impact
Jean-Pierre Vilardaga, Ieva Sutkeviciute, Karina A. Peña   +2 more
openaire   +2 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., Meijer, Alexander B., Mertens, Koen, Simpson, Pelle J., van Alphen, Floris P.J., van den Biggelaar, Maartje, van den Eshof, Bart L., Zanivan, Sara   +7 more
core   +2 more sources

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, Bock, Fabian, Braun-Dullaeus, Ruediger C., Camerer, Eric, Dockendorff, Chris, Elwakiel, Ahmed, Esmon, Charles T., Gadi, Ihsan, Ghosh, Sanchita, Griffin, John H., Huber, Tobias B., Isermann, Berend, Kohli, Shrey, Manoharan, Jayakumar, Nazir, Sumra, Ranjan, Satish, Shahzad, Khurrum   +16 more
core   +2 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, Abraham Madariaga-Mazón, Karina Martinez-Mayorga   +2 more
doaj   +1 more source

Data + pilot biases in modern GNSS signals [PDF]

GPS Solutions, 2023
AbstractWhile traditional GNSS signals are always modulated with navigation data, various modern signals provide a distinct pilot channel without data modulation to support long coherent integration times. Intra-signal biases between the data and pilot components of such signals are evaluated for satellites of the GPS, Galileo, BeiDou-3, and QZSS ...
Montenbruck, Oliver, Steigenberger, Peter, Sleewaegen, Jean-Marie   +2 more
openaire   +1 more source