Results 31 to 40 of about 11,641 (225)
Recent updates on GPCR biased agonism [PDF]
Pharmacological Research, 2016 G protein-coupled receptors (GPCRs) are the most important targets for drug discovery and not surprisingly ∼40% of all drugs currently in the market act on these receptors. Currently, one of the most active areas in GPCRs signaling is biased agonism, a phenomenon that occurs when a given ligand is able to preferentially activate one (or some) of the ...
André S. Pupo +5 more
openaire +3 more sources
Frontiers in Neuroscience, 2021 Nociceptin/orphanin FQ controls several functions, including pain transmission, via stimulation of the N/OFQ peptide (NOP) receptor. Here we tested the hypothesis that NOP biased agonism may be instrumental for identifying innovative analgesics. In vitro
Joaquim Azevedo Neto +7 more
doaj +1 more source
Biased agonism at G protein-coupled receptors
Cellular Signalling, 2021 G protein-coupled receptors (GPCRs) represent the largest family of approved therapeutic targets. Ligands stimulating these receptors specifically activate multiple signalling pathways that induce not only the desired therapeutic response, but sometimes untolerated side effects that limit their clinical use.
Karim, Nagi, Onaran, H. Ongun
openaire +4 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 +2 more
doaj +1 more source
Frontiers in Pharmacology, 2021 Adenosine A1 receptors (A1R) are a potential target for cardiac injury treatment due to their cardioprotective/antihypertrophic actions, but drug development has been hampered by on-target side effects such as bradycardia and altered renal hemodynamics ...
Patricia Rueda +11 more
doaj +1 more source
Frontiers in Molecular Biosciences, 2023 Noradrenergic projections from the brainstem locus coeruleus drive arousal, attentiveness, mood, and memory, but specific adrenoceptor (AR) function across the varied brain cell types has not been extensively characterized, especially with agonists. This
Rachel A. Matt +5 more
doaj +1 more source
F1000 Biology Reports, 2009 Seven-transmembrane receptors are commonly coupled to multiple signaling pathways in cells. The simple model describing agonists for these receptors as producing a common active state to induce uniform activation of the pathways linked to the receptor has been shown to be untenable in light of a large body of data that suggest that some agonists ...
openaire +2 more sources
A novel mechanism of action for angiotensin-(1-7) via the angiotensin type 1 receptor [PDF]
, 2016 No abstract ...
Nicklin, Stuart A.
core +1 more source
Structural Basis of the Diversity of Adrenergic Receptors
Cell Reports, 2019 Summary: Adrenergic receptors are highly homologous while at the same time display a wide diversity of ligand and G-protein binding, and understanding this diversity is key for designing selective or biased drugs for them.
Lu Qu +11 more
doaj +1 more source
Multidisciplinary Consideration of Potential Pathophysiologic Mechanisms of Paradoxical Erythema with Topical Brimonidine Therapy. [PDF]
, 2016 Rosacea is a chronic inflammatory disease with transient and non-transient redness as key characteristics. Brimonidine is a selective α2-adrenergic receptor (AR) agonist approved for persistent facial erythema of rosacea based on significant efficacy and
Detmar, Michael +6 more
core +2 more sources