Compound class:
Synthetic organic
Comment: Compound 86 is reported as a selective inhibitor of sirtuin 2 (SIRT2) [1], a NAD-dependent protein deacetylase with protective effects neurodegenerative disease. Compound 86 is shown to be competitive with NAD+ and the enzyme's peptide substrate, with acceptable blood-brain barrier penetrance (a property essential for any drug being developed for neuroprotective activity).
Drug-like SIRT2 inhibitors are being developed to determine if SIRT2 blockade could be of clinical benefit in Parkinson's disease [2]. ![]() 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. Ai T, Wilson DJ, More SS, Xie J, Chen L. (2016)
5-((3-Amidobenzyl)oxy)nicotinamides as Sirtuin 2 Inhibitors. J Med Chem, 59 (7): 2928-41. [PMID:26982234] |
2. Donmez G, Outeiro TF. (2013)
SIRT1 and SIRT2: emerging targets in neurodegeneration. EMBO Mol Med, 5 (3): 344-52. [PMID:23417962] |
3. Luk KC, Kehm V, Carroll J, Zhang B, O'Brien P, Trojanowski JQ, Lee VM. (2012)
Pathological α-synuclein transmission initiates Parkinson-like neurodegeneration in nontransgenic mice. Science, 338 (6109): 949-53. [PMID:23161999] |
4. Wang MS, Boddapati S, Emadi S, Sierks MR. (2010)
Curcumin reduces alpha-synuclein induced cytotoxicity in Parkinson's disease cell model. BMC Neurosci, 11: 57. [PMID:20433710] |