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Synonyms: compound 4 [PMID: 18835160] | CRX-601 | CRX601 | GSK'091 | GSK-1795091
Compound class: Synthetic organic
Comment: GSK1795091 is a dendritic glycolipid TLR4 agonist with potential immunoadjuvant activity [2-3]. Structurally it is a mimetic of bacterial lipid A . TLR4 plays a key role in the activation of the innate immune response. Activating TLR4 stimulates dendritic cells (DCs), monocytes and macrophages to increase production of pro-inflammatory cytokines (IFNγ, TNFα, interleukins (IL), IL-1 beta, -6 and -12). This mechanism produces a Th1 immune response that offers adjuvant potential in combination with tumour antigen vaccines, and a subsequent cytotoxic T-lymphocyte response against the targeted tumour cells. It also enhances the immune response to checkpoint inhibitor cancer therapies.
Ligand Activity Visualisation Charts
These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.✖
1. Bazin HG, Murray TJ, Bowen WS, Mozaffarian A, Fling SP, Bess LS, Livesay MT, Arnold JS, Johnson CL, Ryter KT et al.. (2008)
The 'Ethereal' nature of TLR4 agonism and antagonism in the AGP class of lipid A mimetics.
Bioorg Med Chem Lett, 18 (20): 5350-4. [PMID:18835160]
2. Oberoi HS, Yorgensen YM, Morasse A, Evans JT, Burkhart DJ. (2016)
PEG modified liposomes containing CRX-601 adjuvant in combination with methylglycol chitosan enhance the murine sublingual immune response to influenza vaccination.
J Control Release, 223: 64-74. [PMID:26551346]
3. Spinner JL, Oberoi HS, Yorgensen YM, Poirier DS, Burkhart DJ, Plante M, Evans JT. (2015)
Methylglycol chitosan and a synthetic TLR4 agonist enhance immune responses to influenza vaccine administered sublingually.
Vaccine, 33 (43): 5845-5853. [PMID:26392012]