Target intelligence / Profile preview

Mast cell membrane-associated calcium-dependent binding site (Cromolyn-binding protein)

Target
Cromolyn-binding protein
Molecular classification
Membrane protein, Ion channel regulator, Calcium-binding protein
01

Overview

The mast cell membrane-associated calcium-dependent binding site is a specialized protein complex or site on the surface of mast cells that mediates the action of mast cell stabilizers like cromolyn sodium. These sites are involved in the regulation of calcium ion transport across the cell membrane, which is a critical step in the activation and subsequent degranulation of mast cells. When a ligand binds to these sites, it prevents the calcium influx that normally follows the cross-linking of IgE receptors by allergens. By maintaining the stability of the mast cell membrane, these sites prevent the release of preformed mediators such as histamine and the synthesis of newly formed mediators like leukotrienes and prostaglandins. This mechanism makes these binding sites a key therapeutic target for the prophylactic treatment of allergic conditions, including asthma and allergic rhinitis, where mast cell activation plays a central role in the pathophysiology of the disease.

Other names
Cromolyn binding siteDisodium cromoglycate binding siteMast cell stabilizer receptorCromolyn-binding protein (CBP)
02

Mechanism of action

Binding to these membrane-associated sites prevents the opening of calcium channels (such as chloride-dependent calcium channels or ORAI channels) in response to IgE-antigen stimulation, thereby inhibiting the influx of calcium ions necessary for mast cell degranulation and the release of inflammatory mediators like histamine and leukotrienes.

03

Biological functions

Regulation of calcium influxMast cell stabilizationInhibition of degranulationSignal transduction
04

Disease associations

AsthmaAllergic rhinitisMastocytosisAllergic conjunctivitisInflammation
05

Safety considerations

Poor oral bioavailabilityLocal irritation (cough or bronchospasm upon inhalation)Short half-life requiring frequent dosingHypersensitivity reactions (rare)
06

Interacting drugs

Cromolyn sodium

2 more in the full profile.

07

Biomarkers

Exhaled nitric oxide (FeNO)Sputum eosinophilsSerum IgE levels

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