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Small Molecule Inhibitors Targeting RNA Modifying Enzymes to Modulate Drug Response and Overcome Drug Resistance

Published:
Lead Inventor: Jason Cheng
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SUMMARY

  • DNA hypomethylating agents have been widely used to treat various hematologic and non-hematologic malignancies. However, accumulating evidence has demonstrated that DNA methylation status does not correlate with clinical response to hypomethylating agents. 
  • Two RNA cytosine methyltransferases (RCMTs) NSUN1 and NSUN2 are responsible for catalyzing the majority of 5-methylcytosine in RNA (RNA:mC) and regulate chromatin structure, gene expression and organelle functions in human cells.  NSUN1 and NSUN2 are correlated with a significant shorter survival in almost all cancer subtypes. 
  • The faculty inventor has developed small molecule inhibitors that target RCMTs NSUN1 and NSUN2-mediated active chromatin structures (ACS) to overcome cancer drug resistance.   
  • Additionally, the inventor established a novel fluorescence quenching complex and NSUN1/2-ACS-targeting NSUN1/2ACS/FQRA plate assay for high-throughput drug tests and screening. 

FIGURE

 

ADVANTAGES

ADVANTAGES

  • New mechanisms of action to overcome drug resistance

  • Novel biological anticancer activities

  • Novel fluorescent quenching complex

 

APPLICATIONS

  • Therapeutic alternatives for overcoming cancer drug resistance

  • Quickly predict drug resistance

  • High-throughput drug tests and screening