Results 101 to 110 of about 29,885 (192)

Pepducin-mediated cardioprotection via β-arrestin-biased β2-adrenergic receptor-specific signaling [PDF]

open access: yes, 2018
Reperfusion as a therapeutic intervention for acute myocardial infarction-induced cardiac injury itself induces further cardiomyocyte death. β-arrestin (βarr)-biased β-adrenergic receptor (βAR) activation promotes survival signaling responses in vitro ...
Benovic, Jeffrey L.   +7 more
core   +1 more source

Discovery of functionally selective C5aR2 ligands: novel modulators of C5a signalling. [PDF]

open access: yes, 2016
The complement cascade is comprised of a highly sophisticated network of innate immune proteins that are activated in response to invading pathogens or tissue injury. The complement activation peptide, C5a, binds two seven transmembrane receptors, namely
Blaskovich, M.A.   +11 more
core   +1 more source

Cannabigerol reverses mechanical allodynia through α2A‐adrenergic modulation of thalamocortical signaling in chemotherapy‐induced neuropathy

open access: yesBritish Journal of Pharmacology, EarlyView.
Abstract Background and Purpose Chemotherapy‐induced peripheral neuropathy (CIPN) is a prevalent and treatment‐resistant side effect of platinum‐based chemotherapy, characterised by mechanical allodynia. Cannabigerol (CBG), a non‐psychoactive cannabinoid, has shown antinociceptive potential, but its site and mechanism of action remain unclear.
Quinn W. Wade   +7 more
wiley   +1 more source

Phosducin regulates the expression of transducin betagamma subunits in rod photoreceptors and does not contribute to phototransduction adaptation. [PDF]

open access: yes, 2007
For over a decade, phosducin's interaction with the betagamma subunits of the G protein, transducin, has been thought to contribute to light adaptation by dynamically controlling the amount of transducin heterotrimer available for activation by ...
Arshavsky, Vadim Y   +6 more
core  

Cellular and viral peptides bind multiple sites on the N-terminal domain of clathrin [PDF]

open access: yes, 2017
Short peptide motifs in unstructured regions of clathrin-adaptor proteins recruit clathrin to membranes to facilitate post-Golgi membrane transport. Three consensus clathrin-binding peptide sequences have been identified and structural studies show that ...
Graham, SC   +3 more
core   +2 more sources

Drugs that act on both G protein‐coupled receptors (GPCRs) and kinases: potentiation of effects, side effects and general aspects of drug pleiotropy

open access: yesBritish 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

Differential CCR7 Targeting in Dendritic Cells by Three Naturally Occurring CC-Chemokines [PDF]

open access: yes, 2016
The CCR7 ligands CCL19 and CCL21 are increasingly recognized as functionally different (biased). Using mature human dendritic cells (DCs), we show that CCL19 is more potent than CCL21 in inducing 3D chemotaxis.
Anne Steen   +8 more
core   +2 more sources

GIP in Cardiovascular and Kidney Disease: From Physiology to Pharmacology

open access: yesDiabetes, 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

Signal Transduction and Pathogenic Modifications at the Melanocortin-4 Receptor: A Structural Perspective [PDF]

open access: yes, 2019
The melanocortin-4 receptor (MC4R) can be endogenously activated by binding of melanocyte-stimulating hormones (MSH), which mediates anorexigenic effects. In contrast, the agouti-related peptide (AgRP) acts as an endogenous inverse agonist and suppresses
Biebermann, Heike   +10 more
core   +1 more source

Dose–Response Effect of Glucagon on Glucose, Beta‐Cell Secretion and Metabolism in Healthy Individuals

open access: yesDiabetes, 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

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