Results 11 to 20 of about 185,950 (192)
Molecular mechanisms of fentanyl mediated β-arrestin biased signaling. [PDF]
PLoS Computational Biology, 2020 The development of novel analgesics with improved safety profiles to combat the opioid epidemic represents a central question to G protein coupled receptor structural biology and pharmacology: What chemical features dictate G protein or β-arrestin ...
Parker W de Waal +7 more
doaj +2 more sources
How Ligands Achieve Biased Signaling toward Arrestins. [PDF]
BiochemistryG protein-coupled receptors (GPCRs) mediate the effects of various endogenous and extracellular stimuli through multiple transducers, including heterotrimeric G proteins, GPCR kinases (GRKs), and arrestins. Biased signaling, which preferentially activates certain G protein or GRK/arrestin signaling pathways, provides great opportunities for developing ...
Jiang Q, Che T.
europepmc +3 more sources
Structural Insights into CB1 Receptor Biased Signaling. [PDF]
Int J Mol Sci, 2019 The endocannabinoid system has emerged as a promising target for the treatment of numerous diseases, including cancer, neurodegenerative disorders, and metabolic syndromes. Thus far, two cannabinoid receptors, CB1 and CB2, have been discovered, which are found predominantly in the central nervous system (CB1) or the immune system (CB2), among other ...
Al-Zoubi R, Morales P, Reggio PH.
europepmc +5 more sources
Anxiety biases audiovisual processing of social signals [PDF]
Behavioural Brain Research, 2021 In everyday life, information from multiple senses is integrated for a holistic understanding of emotion. Despite evidence of atypical multisensory perception in populations with socio-emotional difficulties (e.g., autistic individuals), little research to date has examined how anxiety impacts on multisensory emotion perception.
Naomi Heffer +4 more
openaire +2 more sources
Biased Signaling at Chemokine Receptors [PDF]
Journal of Biological Chemistry, 2015 The ability of G protein-coupled receptors (GPCRs) to activate selective signaling pathways according to the conformation stabilized by bound ligands (signaling bias) is a challenging concept in the GPCR field. Signaling bias has been documented for several GPCRs, including chemokine receptors.
Corbisier, Jenny +4 more
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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
Frontiers in Chemistry, 2021 Allosteric modulators (AMs) of G-protein coupled receptors (GPCRs) are desirable drug targets because they can produce fewer on-target side effects, improved selectivity, and better biological specificity (e.g., biased signaling or probe dependence) than
Keith M. Olson +4 more
doaj +1 more source
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 +2 more
openaire +2 more sources
Frontiers in Endocrinology, 2021 Seven transmembrane receptors (7TMRs), often termed G protein-coupled receptors (GPCRs), are the most common target of therapeutic drugs used today. Many studies suggest that distinct members of the GPCR superfamily represent potential targets for the ...
Camila Oliveira de Souza +2 more
doaj +1 more source
Structure, Function, and Pharmaceutical Ligands of 5-Hydroxytryptamine 2B Receptor
Pharmaceuticals, 2021 Since the first characterization of the 5-hydroxytryptamine 2B receptor (5-HT2BR) in 1992, significant progress has been made in 5-HT2BR research. Herein, we summarize the biological function, structure, and small-molecule pharmaceutical ligands of the 5-
Qing Wang +3 more
doaj +1 more source