Inhibitors of Sir2: evaluation of splitomicin analogues. Posakony, J., Hirao, M., Stevens, S., Simon, J. a, & Bedalov, A. Journal of medicinal chemistry, 47(10):2635–44, May, 2004. ISBN: 2066676241![Inhibitors of Sir2: evaluation of splitomicin analogues. [link]](https://bibbase.org/img/filetypes/link.svg "link")
Paper doi abstract bibtex Splitomicin (1) and 41 analogues were prepared and evaluated in cell-based Sir2 inhibition and toxicity assays and an in vitro Sir2 inhibition assay. Lactone ring or naphthalene (positions 7-9) substituents decrease activity, but other naphthalene substitutions (positions 5 and 6) are well-tolerated. The hydrolytically unstable aromatic lactone is important for activity. Lactone hydrolysis rates were used as a measure of reactivity; hydrolysis rates correlate with inhibitory activity. The most potent Sir2 inhibitors were structurally similar to and had hydrolysis rates similar to 1.
@article{Posakony2004,
title = {Inhibitors of {Sir2}: evaluation of splitomicin analogues.},
volume = {47},
issn = {0022-2623},
url = {http://www.ncbi.nlm.nih.gov/pubmed/15115404},
doi = {10.1021/jm030473r},
abstract = {Splitomicin (1) and 41 analogues were prepared and evaluated in cell-based Sir2 inhibition and toxicity assays and an in vitro Sir2 inhibition assay. Lactone ring or naphthalene (positions 7-9) substituents decrease activity, but other naphthalene substitutions (positions 5 and 6) are well-tolerated. The hydrolytically unstable aromatic lactone is important for activity. Lactone hydrolysis rates were used as a measure of reactivity; hydrolysis rates correlate with inhibitory activity. The most potent Sir2 inhibitors were structurally similar to and had hydrolysis rates similar to 1.},
number = {10},
journal = {Journal of medicinal chemistry},
author = {Posakony, Jeff and Hirao, Maki and Stevens, Sam and Simon, Julian a and Bedalov, Antonio},
month = may,
year = {2004},
pmid = {15115404},
note = {ISBN: 2066676241},
keywords = {\#nosource, Histone Deacetylase Inhibitors, Lactones, Lactones: chemistry, Naphthalenes, Naphthalenes: chemical synthesis, Naphthalenes: chemistry, Naphthalenes: pharmacology, Pyrones, Pyrones: chemical synthesis, Pyrones: chemistry, Pyrones: pharmacology, Saccharomyc, Saccharomyces cerevisiae, Saccharomyces cerevisiae: drug effects, Saccharomyces cerevisiae: enzymology, Silent Information Regulator Proteins, Sirtuin 2, Sirtuins, Sirtuins: antagonists \& inhibitors, Structure-Activity Relationship},
pages = {2635--44},
}
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