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Synonyms: AM-111 | D-JNKI-1 | XG-102
Compound class:
Peptide or derivative
Comment: Brimapitide is a highly selective, non-competitive, long-acting inhibitor of c-jun N-terminal kinase (JNK). The peptide is an investigational drug for the intratympanic (i.t.) treatment of acute sensorineural hearing loss (ASNHL). Structurally the peptide consists of 20 amino acids from C-Jun-amino-terminal kinase-interacting protein 1 (JIP-1) fused to a carrier peptide derived from HIV-TAT48-57 (TAT) peptide PPRRRQRRKKRG. The peptide is constructed in a D-retro-inverso configuration to render it protease resistant. The TAT peptide mediates cell permeability. The sequence is claimed in patent US8080517 (SEQ ID NO: 11, D-JNKI1) [2]. The research codes XG-102 and AM-111 seem to be applied to this investigational agent.
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. ✖ |
| Bioactivity Comments |
| Patent US8080517 reports the biological activity of brimaptide in different assays to determine its neuroprotective and other effects in vitro and in vivo [2]. Direct binding studies are not reported. We have mapped brimaptide to JNK3 in the interaction table, as this appears to be the isozyme used in [2], but it is likely to inhibit kinase activity of all JNK enzymes. Anti-inflammatory effects in mouse models of acute inflammatory bowel disease (IBD) are also reported [4]. |
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