The First Class of Inhibitors for YEATS Domain as Potential Anti-Cancer Agents

The target therapy dominated the global non small cell lung cancer (NSCLC) therapeutics market in the past few years. Despite the use of EGFR TKIs as first-line therapy can benefit NSCLC patients, the increasing drug resistant on NSCLC treatment makes the cure rate still very low. Novel target therapy specific for NSCLC is developed to cure this disease.

• A recent study have revealed the YEATS2 YEATS domain as a novel therapeutic target for the treatment of NSCLC and other solid tumors (such as liver cancers, pancreatic cancers and ovarian cancers).
• The first-in-class of small-molecule inhibitors targeting the YEATS2 YEATS domain which serve as good leads to develop therapeutic agents for the treatment of NSCLC.

• Selectively disrupting YEATS2-chromatin interaction and inhibition of downstream oncogene transcription (tested by FRAP and CUT&RUN sequencing)
• Cell proliferation inhibition effect on NSCLC and HCC cells (tested by colony formation and cell proliferation assay)
• LS-1-124 shows promising activity to inhibit the growth of NSCLC cells in xenograft mouse model

• Anti-NSCLC drug
• Anti-liver cancer drug
• Anti-pancreatic cancer drug
• Anti-ovarian cancer drug

• US Application No.: 18/185,449
• EP Application No: 23162698.7
• CN Application No: 202310266631.7