brimapitide   Click here for help

GtoPdb Ligand ID: 9101

Synonyms: AM-111 | D-JNKI-1 | XG-102
Immunopharmacology Ligand
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.
Click here for help

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.

✖

View interactive charts of activity data across species
References
1. Barkdull GC, Hondarrague Y, Meyer T, Harris JP, Keithley EM. (2007)
AM-111 reduces hearing loss in a guinea pig model of acute labyrinthitis.
Laryngoscope, 117 (12): 2174-82. [PMID:18322422]
2. Bonny C. (2011)
Cell-permeable peptide inhibitors of the JNK signal transduction pathway.
Patent number: US8080517 B2. Assignee: Xigen Sa. Priority date: 12/09/2005. Publication date: 20/12/2011.
3. Omotehara Y, Hakuba N, Hato N, Okada M, Gyo K. (2011)
Protection against ischemic cochlear damage by intratympanic administration of AM-111.
Otol Neurotol, 32 (9): 1422-7. [PMID:22089955]
4. Reinecke K, Eminel S, Dierck F, Roessner W, Kersting S, Chromik AM, Gavrilova O, Laukevicience A, Leuschner I, Waetzig V et al.. (2012)
The JNK inhibitor XG-102 protects against TNBS-induced colitis.
PLoS ONE, 7 (3): e30985. [PMID:22427801]
5. Suckfuell M, Lisowska G, Domka W, Kabacinska A, Morawski K, Bodlaj R, Klimak P, Kostrica R, Meyer T. (2014)
Efficacy and safety of AM-111 in the treatment of acute sensorineural hearing loss: a double-blind, randomized, placebo-controlled phase II study.
Otol Neurotol, 35 (8): 1317-26. [PMID:24979398]