Targets Associated to Immuno Cell Types - Mast cells

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The Mast cells category includes the following Cell Ontology parent terms:

mast cell (CL:0000097) - A cell that is found in almost all tissues containing numerous basophilic granules and capable of releasing large amounts of histamine and heparin upon activation. Progenitors leave bone marrow and mature in connective and mucosal tissue. Mature mast cells are found in all tissues, except the bloodstream. Their phenotype is CD117-high, CD123-negative, CD193-positive, CD200R3-positive, and FceRI-high. Stem-cell factor (KIT-ligand; SCF) is the main controlling signal of their survival and development.

GPCRs
GtoPdb receptor name (family) Cell Type Association Comments Cell Ontology Associations Immunopharmacology Comments
CCR3
(Chemokine receptors)
CCR3 is expressed on mast cells, basophils, and Th2 lymphocytes
  • mast cell (CL:0000097)
CCR3 is one of more than 20 distinct chemokine receptors expressed in human leukocytes. Chemokines primarily act to promote leukocyte chemotaxis to sites of inflammation.
5-HT1A receptor
(5-Hydroxytryptamine receptors)
Involved in mast cell chemotaxix.
  • mast cell (CL:0000097)
The chemoattractant properties of 5-HT on both human and mouse mast cells are mediated by 5-HT1A receptor [32] ...
CB1 receptor
(Cannabinoid receptors)
Mast cells express both cannabinoid receptors, although the CB1 receptor is most abundantly expressed in the central nervous system.
  • mast cell (CL:0000097)
CB1 receptor is involved in controlling mast cell degranulation and maturation [56] ...
H1 receptor
(Histamine receptors)
In humans, mast cells express H1R, H2R and H4R.
  • mast cell (CL:0000097)
The H1 receptor was the first of the family to be targeted for clinical use, with antagonists (anti-histamines) developed that are still used widely to treat alleric inflammation such as rhinitis, allergic conjunctivitis, urticaria and even anaphylaxis.
H2 receptor
(Histamine receptors)
In humans, mast cells express H1R, H2R and H4R.
  • mast cell (CL:0000097)
Histamine action via the H2 receptor inhibits eosinophil, mast cell and neutrophil chemotaxis, IL-12 production by dendritic cells and also suppresses Th2 cells and cytokine formation. In airway inflammation the H2 receptor mediates bronchial smooth muscle relaxation, vasodilation and mucus production [46] ...
H3 receptor
(Histamine receptors)
In humans, H3R expression is restricted to brain mast cells.
  • mast cell (CL:0000097)
H3 receptor expression is low in peripheral tissues, but high in neuronal mast cells and eosinophils. It is not currently considered an important target in allergy.
H4 receptor
(Histamine receptors)
In humans, mast cells express H1R, H2R and H4R.
  • mast cell (CL:0000097)
H4 receptor is primarily expressed in mast cells and eosinophils, but is also found on human neutrophils and basophils, and plays an important role in modulating eosinophil chemotaxis [40,61] ...
S1P2 receptor
(Lysophospholipid (S1P) receptors)
Cord blood mast cells express S1P1R and S1P2R
  • mast cell (CL:0000097)
Activation of S1P2R has pro-inflammatory effects (e.g. mast cell degranulation, regulation of pro-inflammatory cytokine production, and cytokine and chemokine release [30,43] ...
S1P1 receptor
(Lysophospholipid (S1P) receptors)
Cord blood mast cells express S1P1R and S1P2R
  • mast cell (CL:0000097)
S1P1R activation by agonists downregulates allergic inflammation (i.e. it has an inhibitory effect) [24-25,52] ...
CB2 receptor
(Cannabinoid receptors)
Mast cells express both cannabinoid receptors.
  • mast cell (CL:0000097)
CB2 receptor on eosinophils mainly mediates anti-inflammatory and immunomodulatory actions e.g. downregulation of pro-inflammatory mediator release. Pharmacological targeting with the CB2 receptor selective antagonist SR144528 attenuates the recruitment of eosinophils and ear swelling in a murine chronic contact dermatitis model [41] ...
MRGPRX2
(Class A Orphans)
  • mast cell (CL:0000097)
Expression of MRGPRX2 was initially reported predominantly in sensory neurons of the dorsal root ganglion. More recently expression has been detected in human mast cells. In these cells the receptor is activated by the antimicrobial peptide LL-37, resulting in calcium mobilisation and degranulation [36,55] ...
Enzymes
GtoPdb receptor name (family) Cell Type Association Comments Cell Ontology Associations Immunopharmacology Comments
PLCγ1
(Phosphoinositide-specific phospholipase C)
  • mast cell (CL:0000097)
Two structurally similar isoforms of PLCγ are expressed by mast cells (PLCγ1 and PLCγ2). Both are important enzymes in the integrated signalling pathways leading to mast cell activation [19,51] ...
PLCγ2
(Phosphoinositide-specific phospholipase C)
  • mast cell (CL:0000097)
Two structurally similar isoforms of PLCγ are expressed by mast cells (PLCγ1 and PLCγ2). Both are important enzymes in the integrated signalling pathways leading to mast cell activation [19,51] ...
FER tyrosine kinase
(Fer family)
  • mast cell (CL:0000097)
FER acts downstream of the activated high affinity immunoglobulin epsilon receptor (FCεR1) and plays a role in FCεR1-mediated signaling in mast cells, regulation of mast cell degranulation, leukocyte recruitment, and leukocyte extravasation following bacterial lipopolysaccharide (LPS ...
FYN proto-oncogene, Src family tyrosine kinase
(Src family)
  • mast cell (CL:0000097)
Animal models and cell line studies indicate a critical role for Fyn in proximal T-cell antigen receptor (TCR) signal transduction [44] ...
LYN proto-oncogene, Src family tyrosine kinase
(Src family)
  • mast cell (CL:0000097)
LYN is a Src family tyrosine kinase, expressed predominantly in hematopoietic cells, but also in neural, liver, and adipose tissues. LYN appears to function as a rheostat to modulate B cell signaling, and can be activating or inhibitory in action, depending on the B cell receptor and interacting protein complement present in particular cells [13,17,59] ...
SRC proto-oncogene, non-receptor tyrosine kinase
(Src family)
  • mast cell (CL:0000097)
Src family tyrosine kinases act as general modulators of immune cell signaling, playing diverse signaling functions, both inhibitory and stimulatory, in immunoreceptor and integrin signaling pathways [33] ...
cathepsin C
(C1: Papain)
    Cathepsin C is a lysosomal cysteine protease constitutively expressed at high levels in lung, kidney, liver and spleen. As well as activity in lysosomal protein degradation, catheposin C also plays a key role in the activation of granule serine proteases in cytotoxic T cells, natural killer cells (g ...
    Catalytic Receptors
    GtoPdb receptor name (family) Cell Type Association Comments Cell Ontology Associations Immunopharmacology Comments
    KIT proto-oncogene receptor tyrosine kinase
    (Type III RTKs: PDGFR, CSFR, Kit, FLT3 receptor family)
    KIT is expressed by mast cell precursors and mature mast cells.
    • mast cell (CL:0000097)
    Stem cell factor (SCF) and its receptor KIT (c-KIT) play an essential part in mast cell biology. In addition to CSF/KIT-mediated regulation of mast cell development, proliferation and survival, KIT is also reported to be involved in the adhesion of mast cells to human airway epithelial cells (a homing and adhesion role), suggesting a mechanism that could be targeted for anti-asthmatic potential [20] ...
    Interleukin-1 receptor-like 1
    (Immunoglobulin-like family of IL-1 receptors)
      IL1RL1 (ST2) is the ligand binding subunit of the functional receptor for IL-33. It is mainly expressed on mast cells, eosinophils and other immune cells [16] ...
      Thymic stromal lymphopoietin receptor
      (IL-2 receptor family)
      Functional TLSP receptors are reported on the surface of mast cells.
      • mast cell (CL:0000097)
      TLSP/TLSPR signalling promotes release of pro-inflammatory Th2 mediators by mast cells and eosinophils [38] ...
      Transporters
      GtoPdb receptor name (family) Cell Type Association Comments Cell Ontology Associations Immunopharmacology Comments
      Vesicular polyamine transporter
      (SLC18 family of vesicular amine transporters)
      • mast cell (CL:0000097)
      VPAT is expressed by mast cells and is responsible for vesicular storage of the polyamines, spermine and spermidine, in granules distinct from those containing histamine or serotonin [57] ...
      Other Protein Targets
      GtoPdb receptor name (family) Cell Type Association Comments Cell Ontology Associations Immunopharmacology Comments
      regulator of G-protein signaling 13
      (R4 family)
      • mast cell (CL:0000097)
      RGS13 inhibits CXCL12- and CXCL13-induced MAPK activation, and chemotaxis [53] ...
      CD300a
      (CD molecules)
      Functional CD300a is expressed on human mast cells.
      • mast cell (CL:0000097)
      CD300a is a member of the CD300 family of leucocyte surface receptors [11] ...
      Fc fragment of IgE receptor Ia
      (Fc epsilon receptors)
        The product of the FCεR1A gene is a single-pass type I membrane protein that is a high-affinity receptor for immunoglobulin E (IgE). It is the ligand binding subunit of the tetrameric FCεRI, exhibiting a Kd of ~0.1nM.