• Corpus ID: 29676128

Histamine H 2 Receptor Trafficking : Role of Arrestin , Dynamin , and Clathrin in Histamine H 2 Receptor Internalization

  title={Histamine H 2 Receptor Trafficking : Role of Arrestin , Dynamin , and Clathrin in Histamine H 2 Receptor Internalization},
  author={Natalia Cristina Fern{\'a}ndez and Federico Monczor and Alberto Baldi and Carlos Alberto Davio and Carina Shayo},
Agonist-induced internalization of G protein-coupled receptors (GPCRs) has been implicated in receptor desensitization, resensitization, and down-regulation. In the present study, we sought to establish whether the histamine H2 receptor (H2r) agonist amthamine, besides promoting receptor desensitization, induced H2r internalization. We further studied the mechanisms involved and its potential role in receptor resensitization. In COS7 transfected cells, amthamine induced H2r time-dependent… 

Physiological implications of biased signaling at histamine H2 receptors

The findings indicate that while famotidine acts as inverse agonist diminishing cAMP basal levels, it mimics the effects of histamine and the agonist amthamine concerning receptor desensitization and internalization, and support that ligand bias is not only a pharmacological curiosity but has physiological and pharmacological implications on cell metabolism.

Label-Free Investigations on the G Protein Dependent Signaling Pathways of Histamine Receptors

A non-invasive dynamic mass redistribution (DMR) assay for the human H1–4Rs expressed in HEK cells is established, showing excellent signal-to-background ratios above 100 for histamine (HIS) and higher than 24 for inverse agonists with pEC50 values consistent with literature.

International Union of Basic and Clinical Pharmacology. XCVIII. Histamine Receptors

The H3R is an autoreceptor and heteroreceptor providing negative feedback on histaminergic and inhibition on other neurons, a block of these actions promotes waking and the development of anti-inflammatory drugs is anticipated.

The Role of Serine/Threonine and Tyrosine Protein Phosphatases in Common Snail Command Neurons in a Cellular Analog of Habituation

Comparison of the experimental data and simulation-derived calculated curves of changes in the ACh current showed that the main target of protein phosphatases is the neuron’s transport system, i.e., the cytoskeleton and motor proteins.

Conjugation of chlorin p6 to histamine enhances its cellular uptake and phototoxicity in oral cancer cells

Results suggest that conjugating Cp6 with histamine can help improve the effectiveness of PDT in oral cancer cells by enhancing its intracellular delivery.

Current Knowledge and Perspectives on Histamine H1 and H2 Receptor Pharmacology: Functional Selectivity, Receptor Crosstalk, and Repositioning of Classic Histaminergic Ligands

Novel aspects of the pharmacology and molecular mechanisms of histamine receptors that should be contemplated for optimizing current therapies, repositioning histaminergic ligands for new therapeutic uses, or even including agonists of the histamine system in the treatment of different pathologies such as leukemia or neurodegenerative disorders are discussed.

G-protein coupled receptor resensitization-appreciating the balancing act of receptor function.

Analysis of β-adrenergic receptor as a proto-type GPCR to discuss mechanisms regulating receptor function and other GPCRs are also described to put forth a view point on the universality of such mechanisms.



Histamine H2 receptor desensitization: involvement of a select array of G protein-coupled receptor kinases.

Results indicate that in H2r-transfected COS-7 cells, exposure to an agonist caused desensitization controlled by H2 r phosphorylation via GRK2 and GRK3, the most potent of the G protein-coupled receptor kinases.

The Dynamin-dependent, Arrestin-independent Internalization of 5-Hydroxytryptamine 2A (5-HT2A) Serotonin Receptors Reveals Differential Sorting of Arrestins and 5-HT2A Receptors during Endocytosis* 210

The arrestin and dynamin dependences of agonist- and antagonist-mediated internalization were investigated in live cells using green fluorescent protein (GFP)-tagged 5-HT2A receptors (SR2-GFP) and demonstrated that both agonists and antagonists were dynamin-dependent.

Visualization of agonist-induced internalization of histamine H2 receptors.

Histamine H2 receptors were tagged at the N-terminus with the eight amino acid Flag epitope to allow the immunological identification of the receptor peptide with the monoclonal anti-Flag M2 antibody, indicating that histamine causes H2 receptor internalization via a cAMP-independent pathway.

Reduction of G protein-coupled receptor kinase 2 expression in U-937 cells attenuates H2 histamine receptor desensitization and induces cell maturation.

Results indicate a direct correlation between the expression of GRK2 and the desensitization of natively expressed H2 receptors in U-937 cells, suggesting thatGRK2 plays a major role in the regulation of these receptors' response.

Internalization of the m2 Muscarinic Acetylcholine Receptor

The results suggest that the phosphorylation-mediated regulation of the m2 mAChR may involve arrestin-dependent and -independent events.

Molecular Determinants Underlying the Formation of Stable Intracellular G Protein-coupled Receptor-β-Arrestin Complexes after Receptor Endocytosis*

Using receptor mutagenesis, the ability of β-arrestin to remain associated with these receptors is mediated by specific clusters of serine and threonine residues located in the receptor carboxyl-terminal tail, which provide novel targets for regulating GPCR responsiveness and treating diseases resulting from abnormal G PCR/β-Arrestin interactions.

Internalization of beta-adrenergic receptor in A431 cells involves non-coated vesicles.

It is found that an intracellular potassium depletion treatment known to inhibit endocytosis, did not affect the normal pattern of desensitization of beta-adrenergic receptors and was not affected by the fact that clathrin-coated pits or vesicles participated.

Agonist-induced redistribution of bradykinin B2 receptor in caveolae.

Redistribution of receptors within the plasma membrane as well as between the plasma membrane and various cell compartments presents an important way of regulating the cellular responsiveness to

Involvement of caveolin in ligand-induced recruitment and internalization of A(1) adenosine receptor and adenosine deaminase in an epithelial cell line.

It is shown that A( 1)R and ADA form a stable complex in the cell surface of LLC-PK(1) cells and that agonist-induced internalization of the A (1) adenosine receptor and ADA is mediated by clathrin-independent endocytosis.

Novel roles for arrestins in the post-endocytic trafficking of G protein-coupled receptors.