Biased agonism
نویسندگان
چکیده
منابع مشابه
Biased 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 ...
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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...
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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...
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CB1 cannabinoid receptors (CB1Rs) are attractive therapeutic targets for numerous central nervous system disorders. However, clinical application of cannabinoid ligands has been hampered owing to their adverse on-target effects. Ligand-biased signaling from, and allosteric modulation of, CB1Rs offer pharmacological approaches that may enable the development of improved CB1R drugs, through modul...
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ژورنال
عنوان ژورنال: F1000 Biology Reports
سال: 2009
ISSN: 1757-594X
DOI: 10.3410/b1-87