Yonathan Lissanu Deribe, PhD, MD

Research Project:
Using New Drug Development Technology to Target SMARCA4 Lung Cancer

Grant Awarded:

Innovation Award

Research Topics:

biomarkers
combination therapies experimental therapeutics

Research Disease:

lung cancer

Despite recent advances, the majority of patients with lung cancer lack effective therapeutic options. There is a dire need for additional treatment approaches. DNA sequencing studies have identified frequent mutations in a gene known as SMARCA4 in 15% of advanced lung cancers. We have recently identified a gene named SMARCA2 that is required for growth of SMARCA4 mutant lung cancer. However, identifying selective inhibitors of SMARCA2 has been challenging. We have now developed novel SMARCA2 degrading small molecules based on a new drug-development technology called proteolysis targeting chimera (PROTAC). We demonstrated that a compound called YD23 potently and selectively induces degradation of SMARCA2. We further showed that YD23 selectively inhibits growth of SMARCA4 mutant lung cancer cells. Our findings will be used to guide future development of YD23 in patients with SMARCA4 mutant lung cancer.

Page last updated: April 20, 2024

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