- Nε-Modified lysine containing inhibitors for SIRT1 and SIRT2
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Sirtuins catalyze the NAD+ dependent deacetylation of N ε-acetyl lysine residues to nicotinamide, O′-acetyl-ADP- ribose (OAADPR) and Nε-deacetylated lysine. Here, an easy-to-synthesize Ac-Ala-Lys-Ala sequence has been used as a probe for the screening of novel Nε-modified lysine containing inhibitors against SIRT1 and SIRT2. Nε-Selenoacetyl and N ε-isothiovaleryl were the most potent moieties found in this study, comparable to the widely studied Nε-thioacetyl group. The Nε-3,3-dimethylacryl and Nε-isovaleryl moieties gave significant inhibition in comparison to the Nε-acetyl group present in the substrates. In addition, the studied Nε- alkanoyl, Nε-α,β-unsaturated carbonyl and N ε-aroyl moieties showed that the acetyl binding pocket can accept rather large groups, but is sensitive to even small changes in electronic and steric properties of the Nε-modification. These results are applicable for further screening of Nε-acetyl analogues.
- Huhtiniemi, Tero,Suuronen, Tiina,Lahtela-Kakkonen, Maija,Bruijn, Tanja,J??skel?inen, Sanna,Poso, Antti,Salminen, Antero,Lepp?nen, Jukka,Jarho, Elina
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supporting information; experimental part
p. 5616 - 5625
(2010/09/14)
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- Amino acid derivatives as HIV aspartyl protease inhibitors
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The present invention relates to a class of amino acid derivatives with HIV aspartyl protease inhibitory properties.
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- 9-Fluorenylmethyl Pentafluorophenyl Carbonate as a Useful Reagent for the Preparation of N-9-Fluorenylmethyloxycarbonylamino Acids and their Pentafluorophenyl Esters
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9-Fluorenylmethyl pentafluorophenyl carbonate is a useful reagent for the efficient, side reaction-free introduction of N-9-fluorenylmethyloxycarbonyl protecting group into amino acids and for the subsequent preparation of their pentafluorophenyl esters.Some new compounds of both types are described.
- Schoen, Istvan,Kisfaludy, Lajos
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p. 303 - 305
(2007/10/02)
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