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Literature summary for 3.4.21.112 extracted from

  • Hawkins, J.L.; Robbins, M.D.; Warren, L.C.; Xia, D.; Petras, S.F.; Valentine, J.J.; Varghese, A.H.; Wang, I.K.; Subashi, T.A.; Shelly, L.D.; Hay, B.A.; Landschulz, K.T.; Geoghegan, K.F.; Harwood, H.J.
    Pharmacologic inhibition of site 1 protease activity inhibits sterol regulatory element-binding protein processing and reduces lipogenic enzyme gene expression and lipid synthesis in cultured cells and experimental animals (2008), J. Pharmacol. Exp. Ther., 326, 801-808.
    View publication on PubMed
Search for more literature for 3.4.21.112

Application

Application Comment Organism
medicine small-molecule S1P inhibitors are capable of reducing cholesterol and fatty acid synthesis in vivo and, therefore, represent a potential new class of therapeutic agents for dyslipidemia and for a variety of cardiometabolic risk factors associated with diabetes, obesity, and the metabolic syndrome Homo sapiens

Cloned(Commentary)

Cloned (Comment) Organism
cDNA encoding amino acids 17 to 997, encompassing the prodomain, catalytic domain, and cysteine-rich domain of soluble site 1 protease (sS1P) is expressed in CHO cells Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
(R)-4-((diethylamino)methyl)-N-(2-methoxyphenethyl)-N-(pyrrolidin-3-yl)benzamide inhibits endogenous SREBP processing in Chinese hamster ovary cells. Compound down-regulates the signal from an SRE-luciferase reporter gene in human embryonic kidney 293 cells and the expression of endogenous SREBP target genes in cultured HepG2 cells. In mice treated with the compound for 24 h, the expression of hepatic SREBP target genes is suppressed, and the hepatic rates of cholesterol and fatty acid synthesis are reduced Homo sapiens
(S)-4-((diethylamino)methyl)-N-(2-methoxyphenethyl)-N-(pyrrolidin-3-yl)benzamide purified S-enantiomer Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens Q14703
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
Ac-VFRSLK-7-amido-4-methylcoumarin + H2O
-
 Homo sapiens ?
-
 ?
Dabcyl-Arg-His-Ser-Ser-Arg-Arg-Leu-Leu-Arg-Ala-Leu-Glu-Gly-Gly-Lys(tetramethylrhodamine)-OH + H2O
-
 Homo sapiens ?
-
 ?
Dabcyl-Ser-Gly-Ser-Gly-Arg-Ser-Val-Leu-Ser-Phe-Glu-Ser-Gly-Ser-Lys(tetramethylrhodamine)-Arg-OH + H2O
-
 Homo sapiens ?
-
 ?

Synonyms

Synonyms Comment Organism
S1P
-
 Homo sapiens
SREBP site 1 protease
-
 Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
 assay at Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
8
-
 assay at Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000175
-
 inhibitory profile is determined by measuring the luciferase activity of a transfected sterol regulatory element (SRE)-TATA-luciferase construct into HEK-293 cells Homo sapiens (R)-4-((diethylamino)methyl)-N-(2-methoxyphenethyl)-N-(pyrrolidin-3-yl)benzamide
0.000393
-
 inhibitory profile is determined by measuring the luciferase activity of a transfected sterol regulatory element (SRE)-TATA-luciferase construct into HEK-293 cells Homo sapiens (S)-4-((diethylamino)methyl)-N-(2-methoxyphenethyl)-N-(pyrrolidin-3-yl)benzamide
0.0005
-
 in HepG2 cells, compound inhibits cholesterol synthesis, with an IC50 of 0.0005 mM Homo sapiens (R)-4-((diethylamino)methyl)-N-(2-methoxyphenethyl)-N-(pyrrolidin-3-yl)benzamide
0.000971
-
 purified S-enantiomer, inhibitory profile is determined by measuring the luciferase activity of a transfected sterol regulatory element (SRE)-TATA-luciferase construct into HEK-293 cells Homo sapiens (S)-4-((diethylamino)methyl)-N-(2-methoxyphenethyl)-N-(pyrrolidin-3-yl)benzamide