AUR107

AUR107 is a small molecule inhibitor of Enhancer of Zeste Homolog 2 (EZH2) being developed by Aurigene Discovery Technologies for the treatment of lymphomas. EZH2 is the catalytic subunit of the Polycomb Repressive Complex 2 (PRC2) and functions as a histone methyltransferase that adds methyl groups to lysine 27 of histone H3 (H3K27). This epigenetic modification typically leads to the silencing of genes involved in cell cycle regulation and differentiation. In many lymphomas, EZH2 is overexpressed or mutated, leading to the constitutive repression of tumor suppressor genes. By inhibiting EZH2, AUR107 aims to reverse these epigenetic changes, restore normal gene expression, and inhibit tumor cell proliferation. The drug is currently in Phase 1 clinical development.