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Literature summary for 2.3.1.286 extracted from

  • Kokkonen, P.; Mellini, P.; Nyrhilä, O.; Rahnasto-Rilla, M.; Suuronen, T.; Kiviranta P.; Huhtiniemi, T.; Poso, A.; Jarho, E.; Lahtela-Kakkonen, M.
    Quantitative insights for the design of substrate-based SIRT1 inhibitors (2014), Eur. J. Pharm. Sci., 59, 12-19.
    View publication on PubMed
Search for more literature for 2.3.1.286

Application

Application Comment Organism
medicine the enzyme is a promising drug target in the treatment of age-related diseases, such as neurodegenerative diseases and cancer Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
(4R)-1-(tert-butoxycarbonyl)-4-hydroxyprolyl-N-benzyl-N6-ethanethioyl-L-lysinamide 0.05 mM, 83.4% inhibition Homo sapiens
(4R)-1-(tert-butoxycarbonyl)-N-[(2S)-6-(ethanethioylamino)-1-oxo-1-[(2-oxo-2-phenylethyl)amino]hexan-2-yl]-4-hydroxyprolinamide 0.05 mM, 97.1% inhibition Homo sapiens
(4R)-4-hydroxyprolyl-N-benzyl-N6-ethanethioyl-L-lysinamide 0.05 mM, 89.3% inhibition Homo sapiens
(4R)-N-[(2S)-6-(ethanethioylamino)-1-oxo-1-[(2-oxo-2-phenylethyl)amino]hexan-2-yl]-4-hydroxyprolinamide 0.05 mM, 96.8% inhibition Homo sapiens
1-(tert-butoxycarbonyl)prolyl-N-benzyl-N6-ethanethioyl-L-lysinamide 0.05 mM, 93.7% inhibition Homo sapiens
methyl N2-(tert-butoxycarbonyl)-N6-ethanethioyl-L-lysyl-D-alaninate 0.05 mM, 81.3% inhibition Homo sapiens
N-[(2S)-6-(ethanethioylamino)-1-oxo-1-[(2-oxo-2-phenylethyl)amino]hexan-2-yl]-5-oxoprolinamide 0.05 mM, 98.2% inhibition Homo sapiens
N-[(2S)-6-(ethanethioylamino)-1-[[2-(morpholin-4-yl)ethyl]amino]-1-oxohexan-2-yl]-6-oxoheptanamide 0.05 mM, 61.1% inhibition Homo sapiens
N2-(tert-butoxycarbonyl)-N6-ethanethioyl-N-[2-(4-methoxyphenyl)-2-oxoethyl]-L-lysinamide 0.05 mM, 95.6% inhibition Homo sapiens
N2-(tert-butoxycarbonyl)-N6-ethanethioyl-N-[2-(morpholin-4-yl)ethyl]-L-lysinamide 0.05 mM, 37.5% inhibition Homo sapiens
N2-[(benzyloxy)carbonyl]-N6-ethanethioyl-N-[2-(morpholin-4-yl)ethyl]-L-lysinamide 0.05 mM, 54.9% inhibition Homo sapiens
N6-ethanethioyl-N2-(6-oxoheptanoyl)-N-(2-oxo-2-phenylethyl)-L-lysinamide 0.05 mM, 97.7% inhibition Homo sapiens
prolyl-N-benzyl-N6-ethanethioyl-L-lysinamide 0.05 mM, 94.8% inhibition Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens Q96EB6
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Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
NAD+ + [Fluor de Lys]-N6-acetyl-L-lysine Fluor de Lys is a fluorogenic, acetylated peptide substrate for human sirtuin 1, based on residues 379-382 of p53 (Arg-His-Lys-Lys(Ac)), a site of regulatory acetylation by the p300 and CBP acetyltransferases Homo sapiens nicotinamide + [Fluor de Lys]-L-lysine + 2'-O-acetyl-ADP-ribose
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 ?

Synonyms

Synonyms Comment Organism
SIRT1
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 Homo sapiens
sirtuin 1
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 Homo sapiens