Related Experiment Video

Updated: Mar 8, 2026

An Ex vivo Mast Cell Degranulation Assay using Crude Peritoneal Exudate Cells and Natural Antigen Stimulation
08:25

An Ex vivo Mast Cell Degranulation Assay using Crude Peritoneal Exudate Cells and Natural Antigen Stimulation

Published on: April 27, 2021

2.7K

Effects of fostriecin on β2-adrenoceptor-driven responses in human mast cells

Reza Bastan1, Nahid Eskandari2, Hamidrez J Ardakani2

  • 1a Department of Human Vaccines , Razi Serum and Vaccine Research Institute , Karaj , Iran.

Journal of Immunotoxicology
|January 17, 2017
PubMed

Insights

Fostriecin, a protein phosphatase-2A inhibitor, reduced maximal responses to salbutamol in human mast cells. This suggests protein phosphatase-2A plays a key role in regulating mast cell beta-2 adrenoceptors.

Area of Science:

  • Immunology
  • Cell Biology
  • Pharmacology

Background:

  • Mast cell activation involves intracellular signaling pathways, including phosphorylation regulated by phosphatases.
  • Protein phosphatases, particularly protein phosphatase-2A (PP2A), are crucial regulators of these phosphorylation events.

Purpose of the Study:

  • To investigate the effects of fostriecin, a selective PP2A inhibitor, on beta-2 adrenoceptor-mediated responses in human mast cells.
  • To examine the role of PP2A in regulating histamine release, beta-2 adrenoceptor function, and desensitization in mast cells.

Main Methods:

  • Human mast cells (HLMC) were incubated with fostriecin (10^-6 M) for 24 hours.
  • The effects of fostriecin on salbutamol-induced histamine release and beta-2 adrenoceptor desensitization were assessed.

Main Results:

  • Long-term incubation with fostriecin significantly reduced the maximal response to salbutamol (from 41.2% to 29.9%).
  • Fostriecin pretreatment attenuated the inhibitory effects of salbutamol on histamine release.
  • PP2A inhibition impacted beta-2 adrenoceptor-driven responses and desensitization in mast cells.

Conclusions:

  • Protein phosphatase-2A plays a significant role in regulating the function of beta-2 adrenoceptors in human mast cells.
  • Targeting PP2A may modulate mast cell responses, offering potential therapeutic avenues.
Keywords:
Desensitizationfostriecinhistaminemast cell

More Related Videos

Screening Peptides that Activate MRGPRX2 using Engineered HEK Cells12:38

Screening Peptides that Activate MRGPRX2 using Engineered HEK Cells

Published on: November 6, 2021

3.2K
Analyzing the Functions of Mast Cells In Vivo Using 'Mast Cell Knock-in' Mice09:07

Analyzing the Functions of Mast Cells In Vivo Using 'Mast Cell Knock-in' Mice

Published on: May 27, 2015

11.1K

Related Concept Videos

Adrenergic Receptors: β Subtype01:26

Adrenergic Receptors: β Subtype

β-adrenoceptors have varied sensitivities towards adrenaline, noradrenaline, and isoprenaline. The order of agonist potency is as follows:
Isoprenaline > Adrenaline > Noradrenaline
Neurotransmitter binding to these receptors causes activation of adenylyl cyclase resulting in increased concentrations of cAMP and modulation of calcium ion channels within the cell. They are further classified into β1, β2, and β3 subtypes.
β1-adrenoceptors: β1-adrenoceptors...
4.2K
Antiasthma Drugs: Mast Cell Stabilizers and Anti-IgE Drugs01:25

Antiasthma Drugs: Mast Cell Stabilizers and Anti-IgE Drugs

Asthma is a chronic respiratory condition for which new therapeutic avenues, including anti-inflammatory drugs like mast cell stabilizers and anti-IgE treatments, continue to be developed.
Mast cell stabilizers, such as cromolyn (also known as sodium cromoglycate) and nedocromil (Tilade), are effective drugs in asthma management. These stabilizers hinder histamine release by skillfully obstructing the activation of mast cells and other cellular entities. Notably, they navigate this task without...
2.1K
Adrenergic Receptors (Adrenoceptors): Classification01:27

Adrenergic Receptors (Adrenoceptors): Classification

Adrenergic receptors, or adrenoceptors, respond to the autonomic neurotransmitter noradrenaline and other endogenous catecholamine agonists. They are classified into two main families, α and β, based on their pharmacological response and are further subdivided depending on their location, elicited response, and affinity to specific agonists or antagonists.
α-Adrenoceptors
α-Adrenoceptors are classified into two main subtypes: α1 and α2. The α1 adrenoceptors,...
5.4K
Adrenergic Receptors: ɑ Subtype01:31

Adrenergic Receptors: ɑ Subtype

Adrenoceptors are classified into α and ꞵ classes based on their potencies to catecholamine agonists. α-adrenoceptors show the following order of catecholamine potency:
Adrenaline ≥ Noradrenaline >> Isoprenaline
α-adrenoceptors are further divided into α1 and α2-adrenoceptors.
α1-Adrenoceptors: These receptors are located postsynaptically on the effector organs and cause constriction of smooth muscle mediated by activation of phospholipase...
3.1K
Antiasthma Drugs: β2-Adrenoceptor Agonists01:25

Antiasthma Drugs: β2-Adrenoceptor Agonists

Bronchodilators are critical in managing asthma, a chronic respiratory condition characterized by airway constriction due to inflammation and hyper-reactivity. Specifically, bronchodilators ease this constriction by relaxing the bronchial muscles, facilitating easier breathing.
One class of bronchodilators includes β2-adrenoceptor agonists. These agents target the β2-adrenoceptors located on bronchial smooth muscle cells. By stimulating these receptors, β2-agonists induce...
1.9K
Adrenergic Antagonists: Pharmacological Actions of β-Receptor Blockers01:27

Adrenergic Antagonists: Pharmacological Actions of β-Receptor Blockers

β-receptor blockers significantly impact the cardiovascular system by counteracting catecholamine-induced sympathetic responses. These medications decrease heart rate, contractility, and cardiac output, potentially leading to cardiac depression, life-threatening bradycardia, and death. Therapeutically, β-blockers function as mild antihypertensives and are utilized in treating angina pectoris and cardiac arrhythmias. However, nonselective β-blockers inhibit β2-receptors in...
1.8K