The DOI matches its Crossref record; 4 of the 4 references it cites were found in a registry or an index.
Structure–Activity Studies on Suramin Analogues as Inhibitors of NAD+‐Dependent Histone Deacetylases (Sirtuins)
Abstract
Suramin is a symmetric polyanionic naphthylurea originally used for the treatment of trypanosomiasis and onchocerciasis. Suramin and diverse analogues exhibit a broad range of biological actions in vitro and in vivo, including, among others, antiproliferative and antiviral activity. Suramin derivatives usually target purinergic binding sites. Class III histone deacetylases (sirtuins) are amidohydrolases that require nicotinamide adenine dinucleotide (NAD+) as a cofactor for their catalytic mechanism. Deacetylation of the target proteins leads to a change in conformation and alters the activity of the proteins in question. Suramin was reported to inhibit human sirtuin 1 (SIRT1). We tested a diverse set of suramin analogues to elucidate the inhibition of the NAD+‐dependent histone deacetylases SIRT1 and SIRT2 and discovered selective inhibitors of human sirtuins with potency in the two‐digit nanomolar range. In addition, the structural requirements for the binding of suramin derivatives to sirtuins were investigated by molecular docking. The recently published X‐ray crystal structure of human SIRT5 in complex with suramin and the human SIRT2 structure were used to analyze the interaction mode of the novel suramin derivatives.
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Cites
Development and validation of a genetic algorithm for flexible docking 1 1Edited by F. E. Cohen
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Multiple roles of HDAC inhibition in neurodegenerative conditions
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Sirtuin activators and inhibitors: Promises, achievements, and challenges
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“The huge diarylurea suramin blocks both the acyl-peptide and the NAD+ binding site potently, but its size and non-specific effects on Sirtuins and many other targets render it less promising for further development (McGeary et al., 2008; Schuetz et al., 2007; Suenkel et al., 2013; Trapp et al., 2007).”
BackgroundThe epigenetics of aging and neurodegeneration
Lardenoije, R., Iatrou, A., Kenis, G., Kompotis, K., Steinbusch, H. W. M., Mastroeni, D., Coleman, P., Lemere, C. A., Hof, P. R., van den Hove, D. L. A., et al. (2015) · Progress in Neurobiology · doi:10.1016/j.pneurobio.2015.05.002 · Cited by 381
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Epigenetics in Alzheimer’s Disease: Perspective of DNA Methylation
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A continuous, fluorogenic sirtuin 2 deacylase assay: substrate screening and inhibitor evaluation
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Metadata
- Authors
- Trapp, J., Meier, R., Hongwiset, D., Kassack, M. U., Sippl, W., & Jung, M.
- Venue
- ChemMedChem
- Publisher
- Wiley
- Published
- 2007-09-26
- Volume
- 2
- Issue
- 10
- Pages
- 1419-1431
- ISSN
- 1860-7179 (ISSN-L)
- 1860-7187
- OpenAlex
- W2111862114
- Cited by
- 193
- References
- 4
- FWCI
- 4.73
- Type
- journal article
- Language
- en
- Open access
- closed
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