Synonyms: compound 5 [PMID: 27994760]
Compound class:
Synthetic organic
Comment: C391 is a protease activated receptor 2 (PAR2) antagonist [5]. It is a small peptidomimetic derivative of the PAR2 agonist 2-furoyl-LIGRLO-amide [1]. PAR2 antagonists have potential for treating inflammatory, respiratory, gastrointestinal, neurological, and metabolic disorders.
Ligand Activity Visualisation ChartsThese 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. ✖ |
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References |
1. Boitano S, Hoffman J, Flynn AN, Asiedu MN, Tillu DV, Zhang Z, Sherwood CL, Rivas CM, DeFea KA, Vagner J et al.. (2015)
The novel PAR2 ligand C391 blocks multiple PAR2 signalling pathways in vitro and in vivo. Br J Pharmacol, 172 (18): 4535-4545. [PMID:26140338] |
2. Cocks TM, Moffatt JD. (2000)
Protease-activated receptors: sentries for inflammation?. Trends Pharmacol Sci, 21 (3): 103-8. [PMID:10689364] |
3. Ferrell WR, Lockhart JC, Kelso EB, Dunning L, Plevin R, Meek SE, Smith AJ, Hunter GD, McLean JS, McGarry F et al.. (2003)
Essential role for proteinase-activated receptor-2 in arthritis. J Clin Invest, 111 (1): 35-41. [PMID:12511586] |
4. Kanke T, Takizawa T, Kabeya M, Kawabata A. (2005)
Physiology and pathophysiology of proteinase-activated receptors (PARs): PAR-2 as a potential therapeutic target. J Pharmacol Sci, 97 (1): 38-42. [PMID:15655295] |
5. Yau MK, Liu L, Suen JY, Lim J, Lohman RJ, Jiang Y, Cotterell AJ, Barry GD, Mak JY, Vesey DA et al.. (2016)
PAR2 Modulators Derived from GB88. ACS Med Chem Lett, 7 (12): 1179-1184. [PMID:27994760] |