Substrate analogs for MurG, methods of making same and assays using same

US6703213B2 · kind B2 · utility

Assignee

• THE TRUSTEES OF PRINCETON UNIVERSITY · US

Inventors

• Suzanne Walker Kahne · Princeton, US
• Hongbin Men · Princeton, US
• Peter Park · Rochester, US
• Min Ge · Nanjing, CN

Key dates

• Filing date: Apr 22, 2002
• Grant date: Mar 9, 2004
• Expiry date: Apr 22, 2022

Classification

• Technology area (CPC Y): Emerging Cross-Sectional Technologies
• CPC primary: Y10S530/812
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

General methods for monitoring the activity of MurG, a GlcNAc transferase involved in bacterial cell wall biosynthesis, is disclosed. More particularly, the synthesis of simplified substrate analogs of Lipid I (the natural substrate for MurG), which function as acceptors for UDP-GlcNAc in an enzymatic reaction catalyzed by MurG, is described. Assays using the substrate analogs of the invention are further disclosed, which are useful for identifying a variety of other substrates, including inhibitors of MurG activity, for facilitating mechanistic and/or structural studies of the enzyme and for other uses. High throughput assays are also described.