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Targets Associated to Immuno Cell Types - Macrophages & monocytes

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The Macrophages & monocytes category includes the following Cell Ontology parent terms:

macrophages (CL:0000235) - A mononuclear phagocyte present in variety of tissues, typically differentiated from monocytes, capable of phagocytosing a variety of extracellular particulate material, including immune complexes, microorganisms, and dead cells.
monocytes (CL:0000576) - Myeloid mononuclear recirculating leukocyte that can act as a precursor of tissue macrophages, osteoclasts and some populations of tissue dendritic cells.

GPCRs
GtoPdb receptor name (family) Cell Type Association Comments Cell Ontology Associations Immunopharmacology Comments
β2-adrenoceptor
(Adrenoceptors)
Monocytes from patients with rheumatoid arthritis express lower levels of β2-ARs compared with healthy subjects.
  • monocyte (CL:0000576)
β2-ARs are expressed on innate and adaptive immune cells of humans and rodents, and are reported to have an immuno-modulating effect [27] ...
5-HT1A receptor
(5-Hydroxytryptamine receptors)
Involved in phagocytosis.
  • macrophage (CL:0000235)
  • monocyte (CL:0000576)
The chemoattractant properties of 5-HT on both human and mouse mast cells are mediated by 5-HT1A receptor [45] ...
5-ht1e receptor
(5-Hydroxytryptamine receptors)
  • monocyte (CL:0000576)
5-HT2A receptor
(5-Hydroxytryptamine receptors)
Involved in chemokine production.
  • macrophage (CL:0000235)
  • monocyte (CL:0000576)
The chemoattractant properties of 5-HT on human eosinophils is mediated by 5-HT2A receptor [11] ...
5-HT2B receptor
(5-Hydroxytryptamine receptors)
Involved in DC chemotaxis. 5-HT2B receptor activation has also been shown to promote anti-inflammatory macrophage polarization.
  • macrophage (CL:0000235)
5-HT4 receptor
(5-Hydroxytryptamine receptors)
Involved in cytokine production/release from DCs.
  • macrophage (CL:0000235)
  • monocyte (CL:0000576)
5-HT has been shown to alter cytokine production by dendritic cells via 5-HT4 and 5-HT7 receptors [1] ...
5-HT7 receptor
(5-Hydroxytryptamine receptors)
5-HT7 receptor activation has been shown to promote anti-inflammatory macrophage polarization.
  • macrophage (CL:0000235)
  • monocyte (CL:0000576)
5-HT has been shown to alter cytokine production by dendritic cells via 5-HT4 and 5-HT7 receptors [1] ...
NK1 receptor
(Tachykinin receptors)
  • monocyte (CL:0000576)
  • macrophage (CL:0000235)
Expression in monocytes, macrophages and T helper cells suggests a role in inflammation/immunity.
FFA2 receptor
(Free fatty acid receptors)
  • monocyte (CL:0000576)
FFA2 is a GPCR activated by short-chain fatty acids, and evidence suggests that FFA2 (and FFA3) mediate beneficial effects associated with a fiber-rich diet. These GPCRs are of interest as targets for the treatment of inflammatory and metabolic diseases. FFA2 is included in GtoImmuPdb as it is highly expressed on immune cells, in particular neutrophils, and evidence points to a role in diseases with dysfunctional neutrophil responses, such as inflammatory bowel disease (IBD). A Phase 2 trial of the clinical candidate GLPG0974 ...
CXCR3
(Chemokine receptors)
  • macrophage (CL:0000235)
CXCR3 is one of more than 20 distinct chemokine receptors expressed in human leukocytes. Chemokines primarily act to promote leukocyte chemotaxis to sites of inflammation. CXCR3 is the receptor for CXCL9, -10 and -11, three CXC chemokines that are preferentially expressed on Th1 lymphocytes.
5-HT2C receptor
(5-Hydroxytryptamine receptors)
  • macrophage (CL:0000235)
GPR65
(Class A Orphans)
  • macrophage (CL:0000235)
  • monocyte (CL:0000576)
Tha expression profile of GPR65 suggests an immunological role. In addition, disruption of GPR65 expression leads to reduced eosinophilia in models of allergic airway disease [44] ...
Ion Channels
GtoPdb receptor name (family) Cell Type Association Comments Cell Ontology Associations Immunopharmacology Comments
TRPC3
(Transient Receptor Potential channels)
TRPC channels (e.g. TRPC3, TRPC6) are involved in macrophage activation.
    Expressed on B cells, T cells, neutrophils and monocytes/macrophages [54] ...
    Enzymes
    GtoPdb receptor name (family) Cell Type Association Comments Cell Ontology Associations Immunopharmacology Comments
    Haem oxygenase 1
    (Haem oxygenase)
    • macrophage (CL:0000235)
    • monocyte (CL:0000576)
    Heme oxygenase (HO) is a rate-limiting enzyme in the catabolism of heme, catalyzing the oxidative cleavage of heme (Fe-protoporphyrin-IX) to render equimolar amounts of biliverdin, ferrous iron (Fe2+), and carbon monoxide (CO).

    Heme oxygenase 1 (HO1) is a Nrf2-regulated gene, whose expression is upregulated as a cytoprotective mechanism in response to cellular stresses including inflammation, ischemia, hypoxia, hyperoxia, hyperthermia, or radiation.

    HO1 has antioxidant, antiinflammatory, antiapoptotic, antiproliferative, and immunomodulatory effects in vascular cells, playing an important role in the prevention of vascular inflammation and atherogenesis (reviewed in [3] ...
    mitogen-activated protein kinase kinase kinase 19
    (STE20 family)
    Expressed in alveolar and interstitial macrophages.
      MAP3K19 is expressed predominantly by alveolar and interstitial macrophages and bronchial epithelial cells in the lung and is overexpressed in chronic obstructive pulmonary disease (COPD) [10] ...
      interleukin 1 receptor associated kinase 3
      (Interleukin-1 receptor-associated kinase (IRAK) family)
      • macrophage (CL:0000235)
      • monocyte (CL:0000576)
      IRAK3 expression is restricted to monocytes and macrophages.
      FGR proto-oncogene, Src family tyrosine kinase
      (Src family)
      • macrophage (CL:0000235)
      • monocyte (CL:0000576)
      Fgr may be involved in neutrophil migration, potentially via binding to intergrins [7] ...
      HCK proto-oncogene, Src family tyrosine kinase
      (Src family)
      • macrophage (CL:0000235)
      • monocyte (CL:0000576)
      Hck is thought to be involved in neutrophil migration, potentially via binding to intergrins [7] ...
      LYN proto-oncogene, Src family tyrosine kinase
      (Src family)
      • macrophage (CL:0000235)
      • monocyte (CL:0000576)
      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 [29,31,60] ...
      YES proto-oncogene 1, Src family tyrosine kinase
      (Src family)
      Low expression level
      • monocyte (CL:0000576)
      • macrophage (CL:0000235)
      Although primarily recognised for its oncogenic activity, we have iincluded YES1 in GtoImmuPdb based on its expression in cells of the immune system.
      Catalytic Receptors
      GtoPdb receptor name (family) Cell Type Association Comments Cell Ontology Associations Immunopharmacology Comments
      TLR6
      (Toll-like receptor family)
      • monocyte (CL:0000576)
      • dendritic cell (CL:0000451)
      TLR6 forms heterodimers with TLR2 to detect a wide range of bacterial lipopeptides from bacterial cell membranes, and effect an immune response [28] ...
      MER proto-oncogene, tyrosine kinase
      (Type XI RTKs: TAM (TYRO3-, AXL- and MER-TK) receptor family)
      Mouse splenic macrophages, marginal zone macrophages, by immunofluorescence staining (Shao et al. 2009); mouse, mature tissue macrophages by mRNA expression (Gautier et al. 2012); mouse dendritic cells (Wallet et al. 2008, Rothlin et al. 2007)
      • macrophage (CL:0000235)
      Mer plays a critical role in regulating self-tolerance mediated between apoptotic cells, dendritic cells, and T cells [8,61] ...
      single Ig and TIR domain containing
      (Immunoglobulin-like family of IL-1 receptors)
      Expression determined by flow cytometry in human PBMCs.
      • macrophage (CL:0000235)
      • monocyte (CL:0000576)
      IL-1R8 has been identified as a natural killer (NK) cell checkpoint that is involved in regulating NK cells' anti-viral and anti-tumour effector functions [50] ...
      Other Protein Targets
      GtoPdb receptor name (family) Cell Type Association Comments Cell Ontology Associations Immunopharmacology Comments
      CD86
      (CD molecules)
      CD86 is expressed on antigen-presenting cells.
      • macrophage (CL:0000235)
      CD86 (B7-2) is a type I membrane immunoglobulin. It is expressed on antigen-presenting cells and in association with CD80 provides the costimulatory signal necessary for T cell activation and survival. CD86 interacts with CD28 or CTLA-4 on T cells. It is the interaction with CTLA-4 that is targeted ...
      CD80
      (CD molecules)
      • macrophage (CL:0000235)
      • monocyte (CL:0000576)
      CD80 (B7-1) is expressed on dendritic cells and activated B cells and monocytes. It is required to provide a costimulatory signal necessary for T cell activation and survival. CD80 works in concert with CD86 to prime T cells. CD80 binds CD28 and CTLA-4 on T cells. It is the interaction with CTLA-4 t ...
      B7-H3 (CD276)
      (CD molecules)
      B7-H3 expression is induced in monocytes by inflammatory cytokines and by phorbol myristate acetate/ionomycin exposure [21].
      • monocyte (CL:0000576)
      B7-H3 is an immunoregulatory receptor involved in T cell activation and IFN-γ production [21,25] ...
      CD33
      (CD molecules)
      • monocyte (CL:0000576)
      CD33 (SIGLEC-3) is a myeloid cell I-type (Ig-type) lectin that binds glycans containing sialic acids [32] ...
      CD33
      (CD molecules)
      • monocyte (CL:0000576)
      CD33 (SIGLEC-3) is a myeloid cell I-type (Ig-type) lectin that binds glycans containing sialic acids [32] ...
      CS1 (CD319)
      (CD molecules)
      • macrophage (CL:0000235)
      • monocyte (CL:0000576)
      CS1 is a member of the signalling lymphocyte activation molecule (SLAM) receptor family. CS1 is a membrane glycoprotein primarily expressed on plasma cells. Homophilic interaction (i.e. interaction with itself) of CS1 induces B cell proliferation and autocrine cytokine secretion, thus playing a role in various immune functions.

      CS1 is a validated molecular target for the development of novel immunotherapeutics with the potential to treat MM, a malignant disease of plasma cells which remains incurable despite advances in treatment (such as bortezomib, lenalidomide and immunotherapies in clinical trial). Indeed, a combination therapy containing the anti-CS1 mAb elotuzumab (elotuzumab + lenalidomide + dexamethasone), was FDA approved for MM in 2015. CS1 expression is also elevated in patients with systemic lupus erythematosus (SLE) [43] ...
      regulator of G-protein signaling 1
      (R4 family)
      • macrophage (CL:0000235)
      RGS1 is expressed in lymphocytes and macrophages and plays a role in leukocyte trafficking and vascular inflammation [13,36,51,55] ...
      CD38
      (CD molecules)
      • monocyte (CL:0000576)
      • macrophage (CL:0000235)
      CD38 is a type II transmembrane glycoprotein, widely expressed on immune cells and involved in cell adhesion and signal transduction. Its extracellular domain acts as an ectoenzyme, catalyzing the conversion of nicotinamide adenine dinucleotide (NAD+) into nicotinamide, adenosine diphosphate-ribose (ADPR), and cyclic ADPR. Expression of CD38 is tightly regulated during B-cell development and maturation [35] ...
      CD52
      (CD molecules)
      • macrophage (CL:0000235)
      • monocyte (CL:0000576)
      CD52 (CAMPATH-1) is a short, glycosylphosphatidylinositol (GPI) anchored peptide expressed on lymphocytes and by cells of the male genital tract. CD52 is required for complement-mediated cell lysis and antibody-mediated cellular cytotoxicity. The approved monoclonal antibody, alemtuzumab ...
      CD74
      (CD molecules)
      • macrophage (CL:0000235)
      • monocyte (CL:0000576)
      CD74 is a type II transmembrane glycoprotein which associates with the MHC class II α and β chains and directs the transport of class II molecules to lysosomal and endosomal compartments [22] ...
      CD80
      (CD molecules)
      • macrophage (CL:0000235)
      • monocyte (CL:0000576)
      CD80 (B7-1) is expressed on dendritic cells and activated B cells and monocytes. It is required to provide a costimulatory signal necessary for T cell activation and survival. CD80 works in concert with CD86 to prime T cells. CD80 binds CD28 and CTLA-4 on T cells. It is the interaction with CTLA-4 t ...
      LILRA4 (CD85g)
      (CD molecules)
      • macrophage (CL:0000235)
      • monocyte (CL:0000576)
      CD85g is involved in activation of eosinophils and homeostatic regulation of the innate immunity of plasmacytoid dendritic cells (pDCs) [19] ...
      CD209 molecule
      (C-type lectin-like receptors (CLRs))
        DC-SIGN is a pathogen-recognition receptor involved in initiating the primary immune response to various viral and bacterial pathogens, as well as antigen presentation and initiation of the adaptive immune response.
        C-type lectin domain family 7 member A
        (C-type lectin-like receptors (CLRs))
        Dectin-1 is widely expressed in macrophage populations.
          Dectin-1 is a pattern recognition receptor involved in initiating the innate immune response upon recognition of various β(1,3)-linked and β(1,6)-linked glucans from fungi and plants. It mediates phagocytosis and the production of inflammatory mediators [16] ...
          C-type lectin domain family 4 member E
          (C-type lectin-like receptors (CLRs))
          • macrophage (CL:0000235)
          Mincle is an FcRγ-associated membrane receptor involved in initiating the innate immune response upon recognition of endogenous and exogenous ligands including Sin3A-associated protein (SAP130), α-mannan on fungal cell walls and mycobacterial cord factor (trehalose-6,6′-dimycolate (TDM)) [17] ...
          CD86
          (CD molecules)
          CD86 is expressed on antigen-presenting cells.
          • macrophage (CL:0000235)
          CD86 (B7-2) is a type I membrane immunoglobulin. It is expressed on antigen-presenting cells and in association with CD80 provides the costimulatory signal necessary for T cell activation and survival. CD86 interacts with CD28 or CTLA-4 on T cells. It is the interaction with CTLA-4 that is targeted ...
          B7-H3 (CD276)
          (CD molecules)
          B7-H3 expression is induced in monocytes by inflammatory cytokines and by phorbol myristate acetate/ionomycin exposure [21].
          • monocyte (CL:0000576)
          B7-H3 is an immunoregulatory receptor involved in T cell activation and IFN-γ production [21,25] ...
          Fc fragment of IgE receptor Ia
          (Fc epsilon receptors)
          Langerhans cells
            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.
            Fc fragment of IgE receptor II
            (Fc epsilon receptors)
            Langerhans cells
              FcεRII (CD23) is the low-affinity receptor for immunoglobulin E (IgE) with a Kd > 100nM. This protein is a C-type lectin found on mature B cells, activated macrophages, eosinophils, follicular dendritic cells, and platelets. It has no structural similarities with other Fc receptors. FcεRII has functions as both a membrane-bound and as a soluble receptor [41,62] ...