BACKGROUND:  The rise of community- and hospital-acquired methicillin resistant Staphylococcus aureus (MRSA) is a major health problem that has created a pressing need for new antibiotics. More than 90,000 Americans acquire potentially deadly MRSA infections each year, which annually are estimated to kill more people than AIDS in the United States. Proteins displayed on the surface of S. aureus play key roles in the infection process as they promote bacterial adhesion to host cells and tissue, acquire essential nutrients and circumvent the immune response. Most surface proteins in S. aureus are attached to the cell wall by the Sortase A (SrtA) enzyme. Thus, sortase enzymes are a universal target for therapeutic agents against Gram-positive bacteria.

INNOVATION:  Researchers at UCLA have identified several compounds that inhibit the S. aureus SrtA sortase and function as potent anti-infective agents. Many of these molecules also inhibit the sortase enzyme from B. anthracis suggesting that they may be generalized sortase inhibitors.

POTENTIAL APPLICATIONS 

• Treat bacterial infections, especially those caused by Methicillin-resistant S. aureus (MRSA), B. anthracis and possibly other Gram-positive bacteria

ADVANTAGES

• Stops the infection but does not kill the bacteria, therefore less chance of developing drug resistance
• 10 to 100 times more active than previously reported compounds

Reference: UCLA Case No. 2009-666