RORβ: A Novel Oncology Target

We have successfully identified potent and highly specific ligands for the retinoid-related orphan receptor beta (RORβ), including both antagonists and agonists.

We find that RORβ antagonists are broad-ranging modulators of gene expression, as evidenced in our studies involving a small cell lung carcinoma (SCLC) cell line and other cell-based models.

Based on high level expression in ~10% of SCLC tumors, and growth inhibition by RORβ antagonists in an SCLC cell line, RORβ antagonists may be therapeutically effective in SCLC. RORβ is also elevated in certain leukemias, identifying these hematological cancers as potentially sensitive to growth inhibition by RORβ antagonists as well.

At Orphagen, our commitment to the hunt for novel targeted therapies is embodied in our exploration of RORβ antagonist pharmacology. We are open to collaborations to investigate the properties of RORβ ligands.