Results 71 to 80 of about 11,641 (225)
A single extracellular amino acid in Free Fatty Acid Receptor 2 defines antagonist species selectivity and G protein selection bias [PDF]
, 2017 Free Fatty Acid Receptor 2 is a GPCR activated by short chain fatty acids produced in high levels in the lower gut by microbial fermentation of non-digestible carbohydrates.
Aoki, Junken +9 more
core +3 more sources
β-Arrestin-biased Agonism at the β2-Adrenergic Receptor [PDF]
Journal of Biological Chemistry, 2008 Classically, the beta 2-adrenergic receptor (beta 2AR) and other members of the seven-transmembrane receptor (7TMR) superfamily activate G protein-dependent signaling pathways in response to ligand stimulus. It has recently been discovered, however, that a number of 7TMRs, including beta 2AR, can signal via beta-arrestin-dependent pathways independent ...
Matthew T, Drake +5 more
openaire +2 more sources
Chronic Diseases and Translational Medicine, EarlyView.Endogenous GLP‐1 and exogenous GLP‐1 RAs activate GLP‐1R‐expressing vagal afferents in the portal vein, projecting to the nucleus tractus solitarius (NTS). This input engages brainstem–hypothalamic circuits that regulate metabolic homeostasis. Hypothalamic efferent vagal output to the liver suppresses lipogenesis, enhances triglyceride export, and ...
Gabriel Amorim Moreira Alves +8 more
wiley +1 more source
Receptor activity modifying protein-directed G protein signaling specificity for the calcitonin gene-related peptide family of receptors [PDF]
, 2016 The calcitonin gene-related peptide (CGRP) family of G protein-coupled receptors (GPCRs) is formed through association of the calcitonin receptor-like receptor (CLR) and one of three receptor activitymodifying proteins (RAMPs).
Weston, Cathryn +11 more
core +4 more sources
Advances in Achieving Opioid Analgesia Without Side Effects
Frontiers in Pharmacology, 2018 Opioids are the most effective drugs for the treatment of severe pain, but they also cause addiction and overdose deaths, which have led to a worldwide opioid crisis. Therefore, the development of safer opioids is urgently needed.
Halina Machelska, Melih Ö. Celik
doaj +1 more source
Short-term hemodynamic effects of apelin in patients with pulmonary arterial hypertension [PDF]
, 2018 Apelin agonism causes systemic vasodilatation and increased cardiac contractility in humans, and improves pulmonary arterial hypertension (PAH) in animal models.
Alastalo +23 more
core +4 more sources
Receptor Endocytosis as a Mechanism of Biased Agonism at CXCR3
The FASEB Journal, 2021 G Protein Coupled Receptors (GPCRs) are the largest class of receptors in the human genome. They are expressed in virtually every cell type and are implicated in numerous physiological processes. GPCR signaling is highly specific due to biased agonism, in which different ligands, receptors, or cellular systems selectively activate different signaling ...
Noelia Boldizsar +4 more
openaire +1 more source
A Systematic Review on Disease‐Modifying Therapies in Parkinsonian Disorders
Clinical Pharmacology &Therapeutics, EarlyView.Parkinsonian disorders, including Parkinson's disease, Lewy body dementia, multiple system atrophy, and progressive supranuclear palsy, are progressive neurodegenerative conditions with no treatment options to slow disease progression. This systematic review provides an overview of evidence of disease‐modifying therapies that have been evaluated in ...
Pepijn P.N.M. Eijsvogel +3 more
wiley +1 more source
Signal transduction mechanism of biased ligands at histamine H2 receptors [PDF]
, 2014 7TMRs (seven-transmembrane receptors) exist as conformational collections in which different conformations would lead to differential downstream behaviours such as receptor phosphorylation, G-protein activation and receptor internalization.
Alonso, Natalia +5 more
core +1 more source
Biased Agonism in Drug Discovery—Is It Too Soon to Choose a Path? [PDF]
Molecular Pharmacology, 2018 A single receptor can activate multiple signaling pathways that have distinct or even opposite effects on cell function. Biased agonists stabilize receptor conformations preferentially stimulating one of these pathways, and therefore allow a more targeted modulation of cell function and treatment of disease. Dedicated development of biased agonists has
Michel, Martin C., Charlton, Steven J.
openaire +2 more sources