Targeting NAD biosynthesis in bacterial pathogens

US8785499B2 · kind B2 · utility

Assignees

• UNIVERSITY OF MARYLAND, BALTIMORE · US
• The Board of Regents of the University of Texas System · US
• Sanford-Burnham Medical Research Institute · US

Inventors

• Alexander D. MACKERELL, JR. · Baltimore, US
• Hong Zhang · Dallas, US
• Andrei Osterman · San Diego, US
• Rohit Kolhatkar · Loves Park, US

Key dates

• Filing date: Jul 12, 2010
• Grant date: Jul 22, 2014
• Expiry date: Feb 25, 2031

Classification

• Technology area (CPC A): Human Necessities
• CPC primary: A61P31/04
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

The emergence of multidrug-resistant pathogens necessitates the search for new antibiotics acting on previously unexplored targets. Nicotinate mononucleotide adenylyltransferase of the NadD family, an essential enzyme of NAD biosynthesis in most bacteria, was selected as a target for structure-based inhibitor development. To this end, the inventors have identified small molecule compounds that inhibit bacterial target enzymes by interacting with a novel inhibitory binding site on the enzyme while having no effect on functionally equivalent human enzymes.