Compound class:
Peptide or derivative
Comment: Compstatin is a cyclic 13 amino acid peptide inhibitor of complement component 3 (C3) [4-5]. Compstatin and analogues are being examined for immunomodulatory activity [1-2,6] in inflammatory and degenerative diseases [3].
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. ✖ |
References |
1. Mastellos DC, Ricklin D, Hajishengallis E, Hajishengallis G, Lambris JD. (2016)
Complement therapeutics in inflammatory diseases: promising drug candidates for C3-targeted intervention. Mol Oral Microbiol, 31 (1): 3-17. [PMID:26332138] |
2. Mastellos DC, Yancopoulou D, Kokkinos P, Huber-Lang M, Hajishengallis G, Biglarnia AR, Lupu F, Nilsson B, Risitano AM, Ricklin D et al.. (2015)
Compstatin: a C3-targeted complement inhibitor reaching its prime for bedside intervention. Eur J Clin Invest, 45 (4): 423-40. [PMID:25678219] |
3. Morgan BP, Harris CL. (2015)
Complement, a target for therapy in inflammatory and degenerative diseases. Nat Rev Drug Discov, 14 (12): 857-77. [PMID:26493766] |
4. Sahu A, Kay BK, Lambris JD. (1996)
Inhibition of human complement by a C3-binding peptide isolated from a phage-displayed random peptide library. J Immunol, 157 (2): 884-91. [PMID:8752942] |
5. Sahu A, Soulika AM, Morikis D, Spruce L, Moore WT, Lambris JD. (2000)
Binding kinetics, structure-activity relationship, and biotransformation of the complement inhibitor compstatin. J Immunol, 165 (5): 2491-9. [PMID:10946275] |
6. Zhang Y, Shao D, Ricklin D, Hilkin BM, Nester CM, Lambris JD, Smith RJ. (2015)
Compstatin analog Cp40 inhibits complement dysregulation in vitro in C3 glomerulopathy. Immunobiology, 220 (8): 993-8. [PMID:25982307] |