Compound class:
Peptide
Comment: Zyklophin is a cyclic analogue of dynorphin A-(1−11) with antagonist action selective for the κ opioid receptor. Structure, synthesis and function is described in [2], where it is peptide 2. The peptide is brain-penetrant, and has a relatively short duration of action compared to established small-molecule selective KOR antagonists such as nor-binaltorphimine [1].
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. Aldrich JV, Patkar KA, McLaughlin JP. (2009)
Zyklophin, a systemically active selective kappa opioid receptor peptide antagonist with short duration of action. Proc Natl Acad Sci USA, 106 (43): 18396-401. [PMID:19841255] |
2. Patkar KA, Yan X, Murray TF, Aldrich JV. (2005)
[Nalpha-benzylTyr1,cyclo(D-Asp5,Dap8)]- dynorphin A-(1-11)NH2 cyclized in the "address" domain is a novel kappa-opioid receptor antagonist. J Med Chem, 48 (14): 4500-3. [PMID:15999987] |