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Sulfotransferase inhibitors

a technology of sulfotransferase and inhibitor, which is applied in the direction of biocide, drug composition, immunological disorders, etc., can solve the problem that their possibility of being used as therapeutic agents is extremely low

Inactive Publication Date: 2006-06-15
SEIKAGAKU KOGYO CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0022] (11) A medicament for treating or preventing diseases caused by acceleration of sulfotransferase ac...

Problems solved by technology

However, since the former shows nonspecific antagonism upon the sulfate group transfer by a sulfotransferase, and the latter destroys the Golgi body which is the field of sugar chain synthesis, they have activity of strongly inhibiting biosynthesis of not only chondroitin sulfate but also other glycosaminoglycans and glycoproteins, so that their possibility to be used as therapeutic agents was extremely low.

Method used

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Examples

Experimental program
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example 1

Preparation of the Substances of the Present Invention:

[0054] (1) Preparation of Substance 1 of the Present Invention

[0055] In 1.5 cm3 of dry pyridine, 21.7 mg (0.073 mmol) of phenyl 2-acetamide-2-deoxy-α-D-galactopyranoside (Compound 1) was dissolved, and 20.1 mg (0.126 mmol) of sulfur trioxide-pyridine complex was added thereto, followed by stirring at room temperature for 6 hours. To the reaction mixture, 1.5 cm3 of methanol was added, and the mixture was passed through a column of Na+ type ion exchange resin (PARTISIL10SAX, manufactured by Whatman), and the eluate was concentrated under reduced pressure to obtain 34.4 mg of Compound 2 (Substance 1 of the present invention). Compound 2 was purified by high performance liquid chromatography (HPLC) using a column of ion exchange resin (PARTISIL10SAX, manufactured by Whatman) and by gel filtration (using a Superdex 30 column, manufactured by Pharmacia Biotech). Substance 1 of the present invention prepared in this manner was ana...

example 2

[0073] The enzyme activity was measured by modifying the method described in J. Biol. Chem., 276, 43894-43900 (2001). As the standard reaction solution, 2.5 μmol of imidazole-HCl (pH 6.8), 0.5 μmol of CaCl2, 1 μmol of reduced type glutathione, 25 nmol in galactosamine equivalent of chondroitin sulfate A (derived from whale cartilage, manufactured by Seikagaku Corporation), 50 pmol of [35S]PAPS (active sulfate: about 5.0×105 cpm: prepared according to Anal. Biochem., 148, 303-310 (1985)), and human-derived GalNAc4S6ST prepared according to the method described in J. Biol. Chem., 276, 43894-43900 (2001) were added to 50 μl. The reaction was started by adding each of Substance 1 of the present invention, Substance 2 of the present invention, Substance 3 of the present invention, Substance 4 of the present invention, Substance 5 of the present invention and Substance 6 of the present invention to this reaction system to give a final concentration of 50 nmol, 125 nmol or 250 nmol.

[0074]...

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PUM

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Abstract

A galactosamine derivative represented by the following formula (1): wherein R1, R2 and R5 each independently represents SO3− or H, and at least one of them represents SO3−; R3 represents H, acetyl or SO3−; R4 represents H, a substituted or unsubstituted alkyl group, a substituted or unsubstituted alkenyl group, a substituted or unsubstituted alkynyl group, a substituted or unsubstituted acyl group, a substituted or unsubstituted aryl group, or a substituted or unsubstituted aralkyl group; X represents O, S, NH or CH2; and represents an α bond or a β bond, and a sulfotransferase inhibitor comprising the derivative.

Description

TECHNICAL FIELD [0001] The present invention relates to a sulfotransferase inhibitor, more particularly to an inhibitor which inhibits activity of a sulfotransferase (hereinafter sometimes referred to as “GalNAc4S6ST”) having activity of activating sulfation of a hydroxyl group bound to the 6-position of the 4-sulfated galactosamine residue contained in the basic backbone of chondroitin sulfate as a kind of glycosaminoglycans. BACKGROUND OF THE INVENTION [0002] Chondroitin sulfate is a kind of glycosaminoglycans, which is a polysaccharide having a backbone in which a disaccharide resulting from the bonding of glucuronic acid and N-acetylgalactosamine via 1-3 glycosidic linkage is connected in a row via 1-4 glycosidic linkage (hereinafter also referred to as “basic backbone”) and having sulfate groups. [0003] In addition to the glycosaminoglycans such as chondroitin sulfate, in many cases, proteoglycans, glycoproteins and glycolipids have sulfate groups, and many types of sulfotransf...

Claims

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Application Information

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IPC IPC(8): A61K31/7024A61K31/7008A61K31/7034A61P1/00A61P11/06A61P17/00A61P25/00A61P25/02A61P25/18A61P25/24A61P25/28A61P29/00A61P37/06A61P43/00C07H15/203
CPCA61K31/7034C07H15/203A61P1/00A61P1/04A61P11/06A61P17/00A61P25/00A61P25/02A61P25/18A61P25/20A61P25/24A61P25/28A61P29/00A61P37/02A61P37/06A61P37/08A61P43/00
Inventor HABUCHI, OSAMINAKANO, HIROFUMISAWADA, TOSHIHIKOFUJII, SONOKOOHTAKE, SHIORI
Owner SEIKAGAKU KOGYO CO LTD
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