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Mast cell surface protein (individual names include "Fc epsilon RI", "KIT receptor", "CD98hc", "Siglec-8", "MRGPRX2", etc., but no single canonical name exists for the group) (None for the group; individual abbreviations include FcεRI, KIT, CD98hc, etc.)

Target
None for the group; individual abbreviations include FcεRI, KIT, CD98hc, etc.
Molecular classification
Receptor (Fc epsilon RI, MRGPRX2, Siglec-8, KIT/CD117), Enzyme (e.g., CD98hc-associated transporters), Transporter (CD98hc), Other (cell adhesion molecules, antigens such as CD30, CD33, CD52, CD123)
01

Overview

Mast cell surface proteins represent a heterogeneous group of membrane-bound molecules central to mast cell biology. They include receptors such as Fc epsilon RI (high-affinity IgE receptor) critical for allergic responses, KIT (CD117) vital for mast cell growth and survival, Siglec-8 associated with inhibition and depletion, CD98hc involved in cell adhesion and proliferation, and others. These proteins serve roles in immune surveillance, allergic inflammation, cardiovascular and bone homeostasis, and can be dysregulated in disorders such as mastocytosis, allergy, and cancers. Drugs targeting select mast cell surface proteins have shown efficacy in treating mast cell-driven diseases, but the broad distribution of many markers also poses safety and specificity challenges[2][4][6][7][5][3][1].

Other names
Mast cell membrane proteinsMast cell surface markersMast cell receptors (includes Fc epsilon RI, KIT, Siglec-8, MRGPRX2)
02

Mechanism of action

Inhibition of receptor tyrosine kinases (KIT inhibitors); Antibody-mediated depletion/blockade (Siglec-8, CD33); Inhibition of Fc epsilon RI/IgE-mediated activation (experimental antisense oligonucleotides); Inhibition/blockade of MRGPRX2 receptor signaling

03

Biological functions

Immune responseAllergic reactionCell proliferation (KIT-mediated)Signal transductionDegranulation (release of inflammatory mediators)Host defense (against microbes, parasites)Cell adhesion (CD98hc)
04

Disease associations

Cancer (mastocytosis, gastrointestinal stromal tumors, other solid tumors)InflammationAllergy/anaphylaxisMast cell activation syndrome (MCAS)Infection (host defense)
05

Safety considerations

Risk of immunosuppression due to mast cell depletionIncreased risk of infectionPotential exacerbation of allergic/autoimmune reactions if targeting is nonspecificOn-target toxicities (e.g., myelosuppression by KIT inhibitors)Need for precise surface marker selection to avoid effects on non-mast cells
06

Interacting drugs

7 more in the full profile.

07

Biomarkers

CD117 (KIT)FcεRIαSiglec-6, Siglec-8CD98hc (overexpression in mastocytosis)

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