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Literature summary for 2.3.3.8 extracted from

  • Li, J.J.; Wang, H.; Tino, J.A.; Robl, J.A.; Herpin, T.F.; Lawrence, R.M.; Biller, S.; Jamil, H.; Ponticiello, R.; Chen, L.; Chu, C.H.; Flynn, N.; Cheng, D.; Zhao, R.; Chen, B.; Schnur, D.; Obermeier, M.T.; Sasseville, V.; Padmanabha, R.; Pike, K.; Harrity, T.
    2-Hydroxy-N-arylbenzenesulfonamides as ATP-citrate lyase inhibitors (2007), Bioorg. Med. Chem. Lett., 17, 3208-3211.
    View publication on PubMed
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Application

Application Comment Organism
medicine 3,5-dichloro-2-hydroxy-N-(4-methoxybiphenyl-3-yl)benzenesulfonamide is a cell-permeable inhibitor with modest potency. It shows an oral availability of 55%, but a half-life of only 2.1 h. After 20 days of treatment, there is a modest lowering of both plasma cholesterol and triglycerides in high-fat fed mice Mus musculus

Inhibitors

Inhibitors Comment Organism Structure
(1S,2S)-1,2-dihydroxypropane-1,2,3-tricarboxylic acid 50% inhibition at 0.00015 mM Homo sapiens
(2E)-3-phenylprop-2-en-1-yl 2-[[(3,5-dichloro-2-hydroxyphenyl)sulfonyl]amino]benzoate 50% inhibition at 0.00034 mM Homo sapiens
(2R)-2-[(2S)-8-(3,5-dichlorophenyl)-2-hydroxyoctyl]-2-hydroxysuccinic acid 50% inhibition at 0.0021 mM Homo sapiens
3,5-dichloro-2-hydroxy-N-(4-methoxybiphenyl-3-yl)benzenesulfonamide 50% inhibition of enzyme at 0.00013 mM, 50% inhibition of total lipid synthesis in HepG-2 cells at 0.008 mM, no cytotoxicity up to 0.05 mM Homo sapiens
3,5-dichloro-2-hydroxy-N-(4-methoxybiphenyl-3-yl)benzenesulfonamide shows an oral availability of 55%, but a half-life of only 2.1 h. After 20 days of treatment, there is a modest lowering of both plasma cholesterol and triglycerides in high-fat fed mice Mus musculus
3,5-dichloro-N-(2,4,6-triphenyl-phenyl)-2-hydroxybenzenesulfonamide 50% inhibition at 0.00019 mM Homo sapiens
3,5-dichloro-N-(3,5-di-tert-butylphenyl)-2-hydroxybenzenesulfonamide 50% inhibition at 0.0011 mM Homo sapiens
5-methyl-2-(1-methylethyl)cyclohexyl 2-[[(3,5-dichloro-2-hydroxyphenyl)sulfonyl]amino]benzoate 50% inhibition at 0.00037 mM Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
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 recombinant enzyme
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Mus musculus
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-
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