ArticleChemMedChem2020
Activation of Sirtuin 2 Inhibitors Employing Photoswitchable Geometry and Aqueous Solubility.
Article in ChemMedChem, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 5 papers.
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Who cites it
5 citing papers in PubMed.
- Photoresponsive Small Molecule Inhibitors for the Remote Control of Enzyme Activity.Chemistry, an Asian journal · 2022Review
- Article
- Molecular photoswitches in aqueous environments.Chemical Society reviews · 2021Review
- Diarylethene-Based Photoswitchable Inhibitors of Serine Proteases.Angewandte Chemie (International ed. in English) · 2021Article
- Activation of Sirtuin 2 Inhibitors Employing Photoswitchable Geometry and Aqueous Solubility.ChemMedChem · 2020Article
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Authors and funding
8 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Because isoenzymes of the experimentally and therapeutically extremely relevant sirtuin family show high similarity, addressing the unique selectivity pocket of sirtuin 2 is a promising strategy towards selective inhibitors. An unrelated approach towards selective inhibition of isoenzymes with varied tissue distribution is targeted drug delivery or spatiotemporal activation by photochemical activation. Azologization of two nicotinamide-mimicking lead structures was undertaken to combine both approaches and yielded a set of 33 azobenzenes and azopyridines that have been evaluated for their photochemical behaviour and bioactivity. For some compounds, inhibitory activity reached the sub-micromolar range in their thermodynamically favoured E form and could be decreased by photoisomerization to the metastable Z form. Besides, derivatization with long-chain fatty acids yielded potent sirtuin 2 inhibitors, featuring another intriguing aspect of azo-based photoswitches. In these compounds, switching to the Z isomer increased aqueous solubility and thereby enhanced biological activity by up to a factor of 21. The biological activity of two compounds was confirmed by hyperacetylation of sirtuin specific histone proteins in a cell-based activity assay.
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Registered trials
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