Global ETD Search
Search theses and dissertations gathered from participating repositories worldwide. Every result links back to the library that holds it. No account is needed.
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Showing 1 to 5 of 5 for “"Ligand Bias"”.
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Ligand Bias by the Endogenous Agonists of CCR7
… activity. Here we test the hypothesis that these ligands are biased agonists that differentially activate the G-protein coupled Receptor Kinase (GRK)/ b-arrestin system.</p><p>In order to test whether these ligands have distinct activity, murine T lymphocytes were used to compare the effects of …
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FUNCTIONAL SELECTIVITY DOWNSTREAM OF Gαi/o-COUPLED RECEPTORS
… GPCR responses provide opportunities for biased or functionally selective ligands to preferentially modulate one signaling pathway over another. Studies with several GPCRs have suggested that selective activation of signaling pathways downstream of a GPCR may lead to safer and more …
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GPR55 and N-acyl Amino Acids
… to assess these novel lipids as potential GPR55 ligands. Three cell lines were utilised, a stably transfected HEK293 cell line that overexpresses 3xHA N-terminus tagged hGPR55 (hGPR55-HEK293 cells) and control HEK293 cells. In addition, the DU145 a prostate cancer cell line which is reported to …
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Fusion Proteins as Selective Inducers of Constitutive Activity and Tools to Discriminate the Biased Signaling Profile of β2 Adrenoceptor Ligands
… and (c) pharmacologic modulation by β2AR ligands. Since both fusion proteins remained functional to ligand stimuli, we quantified the pharmacological properties of affinity, efficacy, and potency for cAMP accumulation and ERK1/2 phosphorylation as surrogates of the Gs and βarr2 pathways, …
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The Identification and Pharmacological Characterisation of Novel Apelin Receptor Agonists In Vitro and In Vivo
… apelin receptor and two endogenous peptide ligands, apelin and elabela. It is implicated as a potential therapeutic for a number of diseases; however, the endogenous peptides are limited by half-life and bioavailability. This study aims to identify and pharmacologically characterise apelin …