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A method of sensitization of cancer cells to EGFR inhibitors

Description:

Method allowing to increase sensitivity and/or overcome resistance to EGFR inhibitors in cancer cells through inhibition of palmitoyltransferase DHHC20. 

 

Inventor

Eric Witze

 

Problem

Inappropriate activation of the epidermal growth factor receptor (EGFR) contributes to a variety of human malignancies and correlates with poor prognosis and resistance to therapy. Whereas therapy targeting EGFR is currently approved for non-small cell lung carcinomas (NSCLC), advanced colorectal cancer, glioma, pancreatic carcinoma and head and neck tumors; triple negative breast cancer and NSCLC often show resistance to currently available therapies.

 

 

Solution

Dr. Eric Witze’s lab at Penn has found that inhibition of palmitoyltransferase DHHC20 in cancer cells creates a dependence on EGFR signaling for cancer cell survival. Using a palmitoyltransferase inhibitor researchers demonstrated increased sensitivity to Gefitinib in EGFR-activated cancer cells as well as reversal of insensitivity to Gefitinib in lung cancer cells.

  

Advantages

• Sensitization of drug-resistant cancers

• Potential reduction of the treatment doses and side-effects

• Potential use in recurrent cancer patients

 

 

Applications

• Combinational therapy combining EGFR inhibitors and DHHC20 inhibitors

 

 

Stage of Development

In vitro data

   

Desired partnerships

Collaboration

Co-development

Drug discovery