Novel STK1-targeted small molecule "antibiotic resistance breaker" compounds

Novel small molecule STK1 inhibitors that “break” the resistance of bacteria strains to antibiotics.

In today’s healthcare landscape, increasingly highly pathogenic and multidrug-resistant S. aureus (MDRSA) strains are replacing traditional methicillin-resistant S. aureus (MRSA) in both community and hospital settings.

The Need

The rise of these resilient multi-drug resistant bacteria has created a pressing need for novel therapeutic solutions. With pharmaceutical companies facing challenges in developing new, broad-spectrum antibiotics, there is a critical demand for the identification of innovative agents to effectively control the dissemination of MRSA/MDRSA.

The Technology

Researchers at The Ohio State University have developed novel compounds that leverage the critical role played by Ser/Thr protein kinase (STK1) in cell wall biosynthesis of and drug resistance in MRSA. MRSA strains lacking STK1 become susceptible to failing cephalosporins, such as Ceftriaxone and Cefotaxime. Thus, STK1, despite being a nonessential protein for MRSA survival, can serve as an important therapeutic agent for combination therapy. The novel compounds provide are small molecule inhibitors of STK1 that act as antibiotic resistance breakers, and reactivate the effectiveness of antibiotics now deemed to be “off the shelf” or failing.

Commercial Applications

  • Antibiotic Development: This technology opens new avenues for the development of antibiotics targeting highly resistant S. aureus strains.
  • Infectious Disease Treatment: The novel compounds can be applied to treat bacterial infections, particularly those caused by multi-drug-resistant S. aureus.
  • Biomedical Research: Researchers can utilize this technology to study the mechanisms of antibiotic resistance and virulencein bacteria.
  • Pharmaceutical Industry: These novel small molecule STK1 inhibitors provide a foundation for the development of innovative drug compounds to combat multi-drug-resistant pathogens.


  • Targeted Resistance Reduction: The novel compounds target S. aureus’s resistance mechanisms, reducing their ability to withstand antibiotics
  • Innovative Antibiotics: The novel compounds facilitate the development of groundbreaking antibiotics to combat highly pathogenic and multi-drug-resistant strains.
  • Public Health Impact: By combating antibiotic-resistant infections, the novel compounds have a significant positive impact on public health.
  • Therapeutic Potential: The small molecule STK1 inhibitors offer a promising avenue for treating bacterial infections, particularly those cause by S. aureus.

US Patent Issued

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