Identification of active-site inhibitors of glycosyltransferases using a generalizable high-throughput screen
US7344850B2 · kind B2 · utility
Assignee
Inventors
Key dates
| Filing date | Dec 30, 2003 |
| Grant date | Mar 18, 2008 |
| Priority date | — |
| Expiry date | Dec 21, 2024 |
Classification
- Technology area (CPC G)Physics
- CPC primaryG01N2500/02
- WIPO fieldBiotechnology
- WIPO sectorChemistry
Abstract
A method is described for identifying a compound that modulates the ability of a glycosyltransferase to bind a substrate comprising combining a glycosyltransferase, a labeled substrate, and a compound, in a reaction vessel, under conditions known to be suitable for the glycosyltransferase to bind the labeled substrate, measuring an amount of labeled substrate bound to the glycosyltransferase, and comparing the amount to a standardized amount to identify a relative increase or decrease in substrate bound glycosyltransferase, thereby identifying a compound that modulates the ability of the glycosyltransferase to bind the substrate. A composition comprising an effective amount of a compound of Formula I (the substituents of which are described herein), or a stereoisomer, or pharmaceutically acceptable salt thereof, that inhibits the ability of a glycosyltransferase to bind a substrate, in a pharmaceutically acceptable carrier is provided
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.