Results 111 to 120 of about 46,183 (248)
British Journal of Pharmacology, EarlyView.Abstract Background A drug designed for a specific target often interacts with multiple targets, either unintentionally or as part of its intended mechanism of action. This has been called pharmacological pleiotropy or polypharmacology. There are key endogenous ligands such as ATP, GABA and glutamate that act on various proteins in humans. Furthermore,
Hampus Ljunggren +8 more
wiley +1 more source
A Fungal Arrestin Protein Contributes to Cell Cycle Progression and Pathogenesis
mBio, 2019 Arrestins, a structurally specialized and functionally diverse group of proteins, are central regulators of adaptive cellular responses in eukaryotes.
Calla L. Telzrow +4 more
doaj +1 more source
PAR1 Agonists Stimulate APC-Like Endothelial Cytoprotection and Confer Resistance to Thromboinflammatory Injury [PDF]
, 2018 Stimulation of protease-activated receptor 1 (PAR1) on endothelium by activated protein C (APC) is protective in several animal models of disease, and APC has been used clinically in severe sepsis and wound healing.
Aisiku, Omozuanvbo +10 more
core +1 more source
Concepts of GPCR-controlled navigation in the immune system
, 2019 G-protein-coupled receptor (GPCR) signaling is essential for the spatiotemporal control of leukocyte dynamics during immune responses. For efficient navigation through mammalian tissues, most leukocyte types express more than one GPCR on their surface ...
Boneschansker L +26 more
core +1 more source
GIP in Cardiovascular and Kidney Disease: From Physiology to Pharmacology
Diabetes, Obesity and Metabolism, EarlyView.ABSTRACT Aims To provide a comprehensive overview of the cardiovascular and renal effects of glucose‐dependent insulinotropic polypeptide (GIP) by integrating its physiological role with recent human trial data on tirzepatide, the first dual GIP and glucagon‐like peptide‐1 (GLP‐1) receptor agonist.
Michelantonio De Fano +4 more
wiley +1 more source
Behavioral Characterization of β-Arrestin 1 Knockout Mice in Anxiety-Like and Alcohol Behaviors
Frontiers in Behavioral Neuroscience, 2018 β-Arrestin 1 and 2 are highly expressed proteins involved in the desensitization of G protein-coupled receptor signaling which also regulate a variety of intracellular signaling pathways.
Meridith T. Robins +5 more
doaj +1 more source
Diabetes, Obesity and Metabolism, EarlyView.ABSTRACT Aim Glucagon is a key regulator of glucose and energy metabolism, yet the dose–response effects of glucagon on markers of metabolism in humans are not fully characterised. We investigated the dose‐dependent effects of glucagon on glucose metabolism, β‐cell secretion and markers of hepatic metabolism in healthy adults.
Sophie Betty Brock +4 more
wiley +1 more source
Pharmacological ResearchG protein-coupled receptors (GPCRs) exist within a landscape of interconvertible conformational states and in dynamic equilibrium between monomers and higher-order oligomers, both influenced by ligand binding.
Gemma Navarro +7 more
doaj +1 more source
Arrestin-biased AT1R agonism induces acute catecholamine secretion through TRPC3 coupling
Nature Communications, 2017 Angiotensin II type 1 receptor (AT1R)-mediated acute catecholamine release is modulated by β-arrestin. Here the authors show that β-arrestin-1 recruits the Ca2+channel TRPC3 and the PLCγ to the AT1R-β-arrestin complex, triggering G protein-independent ...
Chun-Hua Liu +26 more
doaj +1 more source
Lock, relax, load, and shoot: a molecular perspective on Nedd4 regulation
The FEBS Journal, EarlyView.Structural basis of inactive and active states of the Nedd4 HECT E3 ligase subfamily, following a ‘lock, relax, load, and shoot’ mechanism. In the locked, autoinhibited state, intramolecular domain interactions restrain the HECT domain. Relaxation releases these restraints, allowing loading of ubiquitin onto the catalytic cysteine, followed by the ...
Masa Janosev +2 more
wiley +1 more source