Target nature :
CAS n° :
Mecanism of action :
neutraligand. its binding to CCL17 prevents binding to CCR4
Physico-chemical properties :
solubility: up to 100 µM in buffer
Probe availability :
GreenPharma company / Ambinter
Princeps reference :
Abboud, D., Villa, P., Daubeuf, F., Utard, V., Haiech, J., Bonnet, D., Hibert, M., Bernard, P., Galzi, J.L.*, Frossard, N.* (2015) A strategy to discover decoy chemokine ligands with an anti-inflammatory activity, Sci Rep. 2015 Oct 7;5:14746. doi: 10.1038/srep14746
More bibliography :
Abboud D, Hanson J., Chemokine neutralization as an innovative therapeutic strategy for atopic dermatitis.; Drug Discov Today. 2017 Apr;22(4):702-711. doi: 10.1016/j.drudis.2016.11.023. Epub 2016 Dec 9.
Other available information on the probe :
to be filled
Other information on the target :
CCR4 is expressed on Th2-type helper lymphocytes, eosinophils and dendritic cells.
CCL17, CCL22 and CCR4 contribute to the pathogenesis of atopic diseases, like asthma and atopic dermatitis, as the expression of both ligands and their receptor is enhanced in asthmatic patients and AD skin lesions.
Selectivity profile :
GPN 279 does not affect cellular responses evoked by CCL3, CCL4, CCL5, CCL22, CXCL8, CXCL10, CXCL11 and CXCL12
In vivo data :
in a model of allergic asthma induced by Ovalbumin application GPN 279, administered intraperitoneally at 350 µMol/kg inhibits recruitment of eosinophils in the bronchoalveolar lavage.
In vitro data :
KD for CCL17 is in the range of 50 nM (tryptophan fluorescence assay)
At 10 µM, GPN 279 block 50% of cellular calcium elevation in CCR4-expressing HEK cells
GPN 279 inhibits CCL22-mediated internalisation of CCR4 with IC50 = 0,5 µM
GPN 279 block CCR4+ HUT78T cells migration invitro with an IC50 value = 3x10-8M
No toxicity has been detected after 2 weeks daily treatment at 350 µMol/kg
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