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ligand

How to activate mast cells: Receptors and Ligands Master Table (part 3)

Receptor Ligand (molecules that bind to the receptor) Result
Nicotinic acetylcholine receptor Acetylcholine Increases severity of anaphylaxis
NOD1, NOD2 Bacterial products Cytokines; dependent upon ligand
Paired Ig-like receptor B (PIR-B) Inhibitory
Peripheral benzodiazepine receptor Benzodiazepines Inhibits mediator release
Platelet endothelial cell adhesion molecule (PECAM-1) Inhibitory
Progesterone receptor Progesterone Inhibits mediator release
Prostaglandin E receptors, EP2, Prostaglandin E Downregulates IgE mediated response, inhibits prostaglandin and leukotriene production

 
Prostaglandin E receptors, EP3, EP4 Prostaglandin E Increases IgE mediated degranulation : histamine, tryptase, carboxypeptide, chymase, heparin, chondroitin

 

Increases IgE dependent cytokine production

 
Protease activated receptors 1-4 (PAR1-4) Serine proteases (trypsin, tryptase, chymase) Histamine release, mast cell activation
Purinoreceptor P2Y11 ATP Production of prostaglandins and leukotrienes
Purinoreceptor P2Y2 ATP, UTP Production of prostaglandins and leukotrienes
Purinoreceptors P2Y1, P2Y12, P2Y13 ADP Production of prostaglandins and leukotrienes
Sialic acid binding Inhibitory
Sphingosine-1-phosphate S1P1 Sphingosine-1-phosphate Chemotaxis

 
Sphingosine-1-phosphate S1P2 Sphingosine-1-phosphate Degranulation : histamine, tryptase, carboxypeptide, chymase, heparin, chondroitin

 

De novo:
IL-3, IL-4, IL-5 IL-6, IL-8, IL-10, IL-13, TNF, GM-CSF, CCL2, CCL3, CCL5

 
ST2 IL-33 Cytokines
TGFb receptor 1 TGFb Decreases IgE dependent degranulation, IgE dependent TNF production
TLR1-9 Bacterial and viral products Cytokines ; dependent upon ligand
Urokinase receptor Urokinase Movement of mast cells
Vitamin D receptor Vitamin D Mast cell development
β2-adrenoreceptor Adrenaline Inhibits FcεRI degranulation and cytokine production and secretion

How to activate mast cells: Receptors and Ligands Master Table (part 2)

Receptor Ligand (molecules that bind to the receptor) Result
Gp49B1 Gp49B1-αvβ3 Inhibits IgE activation
GPCR mimetic MRGX2 Mastoparan, cortistatin, PAMP-12, somatostatin, neuropeptide FF, oxytocin, substance P Degranulation: Histamine, tryptase, carboxypeptide, chymas, heparin, chondroitin, renin
GPR34 Lysophosphatidylserine, b defensins, LL-37?? Enhances degranulation:  Histamine, tryptase, carboxypeptide, chymas, heparin, chondroitin, renin

 

De novo:

PGD2, PGE2, LTC4, IL-2, IL03, IL-5, IL-1b, TNF, IL-31, GM-CSF, IL-5, TNFg
GPR92 Lysophosphatidic acid Cytokine production and release
Ig-like lectins Inhibitory
IL-10 receptor IL-10 Decreases IgE dependent release of IL-3, IL-4, IL-5 IL-6, IL-8, IL-10, IL-13, TNF, GM-CSF, CCL2, CCL3, CCL5
IL-3 receptor IL-3 Increases IgE dependent release of histamine and leukotriene C4
IL-4 receptor IL-4 Increases IgE dependent release of histamine, leukotriene C4 and IL-5 release
IL-5 receptor IL-5 Increases IgE dependent secretion :
IL-3, IL-4, IL-5 IL-6, IL-8, IL-10, IL-13, TNF, GM-CSF, CCL2, CCL3, CCL5

 
Leptin receptor Leptin Immunomodulation
Cysteinyl Leukotriene receptor 1, 2 Leukotrienes Cytokine production and proliferation
LPA1, LPA3 Lysophosphatidic acid Encourage development
Mast cell function associated antigen (MAFA) Inhibitory
MHC I Antigenic peptides For activating other immune cells
MHC II Antigenic peptides For activating other immune cells
MRGX2 Mastoparan, somatostatin, substance P, platelet factor 4, mellitin

 

 Degranulation: Histamine, tryptase, carboxypeptide, chymas, heparin, chondroitin, renin

 

De novo: IL-3, IL-8, TNFa, GM-CSF
Myeloid associated Ig-like receptor 1 Unknown Inhibition of mast cell activation and mediator release
Neurokinin receptors: NK1R, NK2R, NK3R, VPAC2 Substance P, CGRP, hemokinin A, VIP, nerve growth factor, neuropeptide Y Substance P: Degranulation:

Histamine, tryptase, carboxypeptide, chymas, heparin, chondroitin, renin

 

Produce and release cytokines

 

VIP, Neuropeptide Y: induce release of histamine

 

CGRP:

Degranulation:

Histamine, tryptase, carboxypeptide, chymas, heparin, chondroitin, renin
Neurotensin receptor Neurotensin Degranulation
Neurotrophin receptor TrkA NGF Degranulation: histamine, serotonin, NGF
Neurotrophin receptor TrkB BDNF, NT-4 No degranulation
Neurotrophin receptor TrkC Neurotrophin 3 No degranulation

How to activate mast cells: Receptors and ligands Master Table (part 1)

There are many receptors on mast cells.  The molecules that bind to these receptors are called ligands.  Different receptors can cause activation in different ways.

I am posting this table a little at a time as I anticipate getting a lot of questions about it.  I put this together for my own reference and I didn’t keep track of all sources.  I am hoping to go through the literature again and track this at some point.

These tables are not exhaustive, and I’ll add to them over time as I have the chance.

Receptor Ligand (molecules that bind to the receptor) Result
0X40 0X40 ligand Suppression of mast cell activation
A2A, A2B, A3 Adenosine At low concentration, degranulation:

histamine, tryptase, carboxypeptide, chymase, heparin, chondroitin

De novo: IL-1b, IL-3, IL-4, IL-8, IL-13

 

At high concentration, inhibits FcεRI degranulation
C3α receptor C3α De novo:
IL-3, IL-4, IL-5 IL-6, IL-8, IL-10, IL-13, TNF, GM-CSF, CCL2, CCL3, CCL5

 

Degranulation : histamine, tryptase, carboxypeptide, chymase, heparin, chondroitin

 

Increases IgE and IgG dependent degranulation
C5α receptor C5α Degranulation : histamine, tryptase, carboxypeptide, chymase, heparin, chondroitin

 
Cannabinoid CB2 receptor 2-arachidonoyl-glycerol, anandamide Suppression of mast cell activity
CCR1 CCL3 (MIP1α), CCL5 (RANTES) Degranulation : histamine, tryptase, carboxypeptide, chymase, heparin, chondroitin
CCR3 CCL11 No degranulation
Increases IgE dependent secretion: IL-3, IL-4, IL-5 IL-6, IL-8, IL-10, IL-13, TNF, GM-CSF, CCL2, CCL3, CCL5
CCR4 CCL2 (MCP-1) No degranulation, reléase of cytokines
CCR5 CCL3 (MIP1α), CCL5 (RANTES), CCL4 (MIP1β) No degranulation, reléase of cytokines
CD200 receptor CD200 (OX2) Inhibitory
Cd300α receptor Eosinophilic granule proteins Inhibitory
CD47 (integrin associated protein, IAP) Integrins Histamine secretion
CD48 E. coli, M. tuberculosis Degranulation : histamine, tryptase, carboxypeptide, chymase, heparin, chondroitin

 

De novo : TNFa, IL-6
CD72 CD100 Inhibits CKIT activation
CKIT receptor tyrosine kinase (CD117) Stem cell factor De novo:
PGD2, leukotriene B4, leukotriene C4, PAF, IL-3, IL-4, IL-5 IL-6, IL-8, IL-10, IL-13, TNF, GM-CSF, CCL2, CCL3, CCL5

 

Increased IgE dependent degranulation: histamine, tryptase, carboxypeptide, chymase, heparin, chondroitin
Corticotropin/ corticotropin releasing hormone receptor CRH, urocortin Secretion of VEGF
CX3CL1 Fractalkine No degranulation
CX3CR1 Chemokines No degranulation, reléase of cytokines
Estrogen receptor Estrogens Increased IgE dependent degranulation: histamine, tryptase, carboxypeptide, chymase, heparin, chondroitin
ETA Endothelin-1 Degranulation: Histamine, tryptase, carboxypeptide, chymase, heparin, chondroitin, renin

 

De novo: TNFa, IL-6, VEGF, TGF-b1
ETB Endothelin-1 Unknown
FcαR (CD89) IgA Unknown
FcγRIIA, FcγRI, FcγRIIIA IgG/antigen Degranulation: Histamine, tryptase, carboxypeptide, chymase, heparin, chondroitin, renin

 

De novo:
PGD2, leukotriene B4, leukotriene C4, PAF, IL-3, IL-4, IL-5 IL-6, IL-8, IL-10, IL-13, TNF, GM-CSF, CCL2, CCL3, CCL5
FcγRIIIB IgG/antigen Cannot induce activation
FcεRI IgE with or without antigen Degranulation: Histamine, tryptase, carboxypeptide, chymas, heparin, chondroitin, renin

 

De novo:
PGD2, leukotriene B4, leukotriene C4, PAF, IL-3, IL-4, IL-5 IL-6, IL-8, IL-10, IL-13, TNF, GM-CSF, CCL2, CCL3, CCL5