RGNCY-0131 (MEQ SeRS activator/VEGFA repressor)

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MEQ is a novel SeRS activator which is a post-transcriptional repressor of VEGFA.  MEQ regulates SeRS transcription by interacting with MTA2 (Metastasis Associated 1 Family Member 2).  MEQ treatment of triple-negative breast cancer (TNBC) cells resulted in increased SeRS mRNA and protein levels and down-regulated VEGFA production.  MEQ inhibited the vascular development of zebrafish and Matrigel plug angiogenesis.  In addition, MEQ suppressed angiogenesis in TNBC allograft and xenograft mouse models which resulted in inhibited tumor growth and prolonged overall survival.  The data suggests that MTA2/SeRS/VEGFA axis is a druggable antiangiogenic target and MEQ is a promising antitumor molecule worthy of clinical investigation.

Systematic Name:  3-(4-methoxyphenyl)quinolin-4(1H)-one

SMILES:  O=C1C(C2=CC=C(OC)C=C2)=CNC3=CC=CC=C31

Formula:   C16H13NO2

Mol Wt: 251.29