A -Arrestin-Biased Agonist of the Parathyroid Hormone Receptor (PTH1R) Promotes Bone Formation Independent of G Protein Activation
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منابع مشابه
Discovery and characterization of a G protein-biased agonist that inhibits β-arrestin recruitment to the D2 dopamine receptor.
A high-throughput screening campaign was conducted to interrogate a 380,000+ small-molecule library for novel D2 dopamine receptor modulators using a calcium mobilization assay. Active agonist compounds from the primary screen were examined for orthogonal D2 dopamine receptor signaling activities including cAMP modulation and β-arrestin recruitment. Although the majority of the subsequently con...
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S Discovery and Characterization of a G Protein–Biased Agonist That Inhibits b-Arrestin Recruitment to the D2 Dopamine Receptor R. Benjamin Free, Lani S. Chun, Amy E. Moritz, Brittney N. Miller, Trevor B. Doyle, Jennie L. Conroy, Adrian Padron, Julie A. Meade, Jingbo Xiao, Xin Hu, Andrés E. Dulcey, Yang Han, Lihua Duan, Steve Titus, Melanie Bryant-Genevier, Elena Barnaeva, Marc Ferrer, Jonathan...
متن کاملNoribogaine is a G-protein biased κ-opioid receptor agonist
Noribogaine is the long-lived human metabolite of the anti-addictive substance ibogaine. Noribogaine efficaciously reaches the brain with concentrations up to 20 μM after acute therapeutic dose of 40 mg/kg ibogaine in animals. Noribogaine displays atypical opioid-like components in vivo, anti-addictive effects and potent modulatory properties of the tolerance to opiates for which the mode of ac...
متن کاملPhosphorylation-independent inhibition of parathyroid hormone receptor signaling by G protein-coupled receptor kinases.
Homologous desensitization of G protein-coupled receptors is thought to occur in several steps: binding of G protein-coupled receptor kinases (GRKs) to receptors, receptor phosphorylation, kinase dissociation, and finally binding of beta-arrestins to phosphorylated receptors. It generally is assumed that only the last step inhibits receptor signaling. Investigating the parathyroid hormone (PTH)...
متن کاملAgonist-biased signaling at the histamine H4 receptor: JNJ7777120 recruits β-arrestin without activating G proteins.
The G(i/o)-coupled histamine H(4) receptor is highly expressed in hemopoietic cells and is a promising new target for the treatment of chronic inflammatory diseases. 1-[(5-Chloro-1H-indol-2-yl)carbonyl]-4-methyl-piperazine (JNJ7777120) has been described as a selective antagonist at the H(4) receptor and is widely used to characterize the physiological role of the H(4) receptor. We have investi...
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ژورنال
عنوان ژورنال: Science Translational Medicine
سال: 2009
ISSN: 1946-6234,1946-6242
DOI: 10.1126/scitranslmed.3000071