منابع مشابه
Fulfilling the Promise of "Biased" G Protein-Coupled Receptor Agonism.
The fact that over 30% of current pharmaceuticals target heptahelical G protein-coupled receptors (GPCRs) attests to their tractability as drug targets. Although GPCR drug development has traditionally focused on conventional agonists and antagonists, the growing appreciation that GPCRs mediate physiologically relevant effects via both G protein and non-G protein effectors has prompted the sear...
متن کاملBiased agonism
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 produce activation of some but not all available ...
متن کاملDivergent transducer-specific molecular efficacies generate biased agonism at a G protein-coupled receptor (GPCR).
The concept of "biased agonism" arises from the recognition that the ability of an agonist to induce a receptor-mediated response (i.e. "efficacy") can differ across the multiple signal transduction pathways (e.g. G protein and β-arrestin (βarr)) emanating from a single GPCR. Despite the therapeutic promise of biased agonism, the molecular mechanism(s) whereby biased agonists selectively engage...
متن کاملIsoform-specific biased agonism of histamine H3 receptor agonists
This article has not been copyedited and formatted. The final version may differ from this version. Abbreviations Imetit, 2-(1H-imidazol-5-yl)ethyl imidothiocarbamate, iodoproxyfan, 3-(1H-imidazol-4-yl)propyl-(4-iodophenyl)-methyl ether, proxyfan, 4-[3-(benzyloxy)propyl]-1H-imidazole, NαMH, N-α-methylhistamine dihydrochloride, pERK, phosphorylated extracellular signal-regulated kinase, RαMH, (R...
متن کاملThe Biased G-Protein-Coupled Receptor Agonism Bridges the Gap between the Insulin Receptor and the Metabolic Syndrome
Insulin signaling, as mediated through the insulin receptor (IR), plays a critical role in metabolism. Aberrations in this signaling cascade lead to several pathologies, the majority of which are classified under the umbrella term "metabolic syndrome". Although many of these pathologies are associated with insulin resistance, the exact mechanisms are not well understood. One area of current int...
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ژورنال
عنوان ژورنال: Journal of Cardiovascular Pharmacology
سال: 2016
ISSN: 0160-2446
DOI: 10.1097/fjc.0000000000000356