3334-56-3Relevant articles and documents
A Set of Highly Sensitive Sirtuin Fluorescence Probes for Screening Small-Molecular Sirtuin Defatty-Acylase Inhibitors
Nakajima, Yuya,Kawaguchi, Mitsuyasu,Ieda, Naoya,Nakagawa, Hidehiko
supporting information, p. 617 - 624 (2021/04/07)
Human sirtuins (SIRT1-7) regulate not only deacetylation but also deacylation of fatty acid-derived acyl moieties (defatty-acylation) at the ?-amino group of lysine residues. SIRT-subtype-specific defatty-acylase activity modulators are needed for detailed investigation of the biological roles of these enzymes, and to find suitable small molecules, we require appropriate screening systems. Here, we designed and synthesized a set of SIRT defatty-acylase activity probes with various quencher moieties and peptide sequences based on our previously developed one-step FRET-based SIRT probe SFP3, using improved methodology. Scanning of this set of probes with SIRT isozymes revealed that certain probe/isozyme combinations showed especially high responses. To illustrate the utility of the combinations thus identified, we applied compound 18/SIRT2 for inhibitor screening of a large chemical library. This enabled us to discover a new small molecule SIRT2-specific defatty-acylase inhibitor.
SYNERGISTS
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Page/Page column 43-44, (2011/10/13)
Compounds of formula (I): wherein Ar represents an, optionally substituted, aryl or heteroaryl group, R represents an, optionally substituted, aryl or heteroaryl group, an optionally substituted straight or branched chain C1.10-alkyl, R1/
Amphiphilic compounds for sequential monolayer deposition
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, (2008/06/13)
Amphiphilic compounds and oligomers and polymers derived therefrom suitable for Langmuir Blodgett deposition having the general formula where M is a molecular moiety., x and y may be the same or different and are between 1 and 6, preferably 2 or 3,B1