AGX51

AGX51 is an orally active, first-in-class small-molecule pan-Id antagonist and degrader that targets inhibitor of DNA binding/differentiation (ID1–4) helix-loop-helix transcriptional regulators, which are frequently overexpressed in cancer and pathological neovascular diseases.[3][5][8][10][11] By binding a conserved pocket on ID proteins, AGX51 disrupts the ID–E protein interaction, liberating E proteins, which restores transcriptional activity driving differentiation and cell-cycle exit while marking ID proteins for ubiquitin-mediated proteasomal degradation.[3][5][6][10][11] This leads to cell-cycle arrest, increased reactive oxygen species, reduced viability, and predominantly non-apoptotic cell death in proliferating tumor cells, and it suppresses tumor growth, lung colonization, and chemotherapy-resistant breast and colorectal cancer in mouse models, as well as ocular neovascularization in models of age-related macular degeneration and retinopathy of prematurity.[3][5][6] AGX51 has shown good tolerability in animals with no clear evidence of acquired resistance and is being developed by AngioGenex for oncology indications, with additional potential in ocular neovascular and other ID-driven diseases.[5][6][8]

Other names

AGX-051AGX051AGX 051