Constellation Pipeline
Constellation has combined its leading epigenetics drug discovery platform with translational research capabilities and is driving multiple programs toward the clinic in each of these target classes.
The company's research into chromatin readers recently appeared in the Proceedings of the National Academy of Sciences. Constellation scientists demonstrated that MYC transcription can be suppressed using small molecule inhibitors of the BET family of chromatin inhibitors. MYC is a master regulator of diverse cellular functions and has long been considered a compelling therapeutic target because of its role in many human malignancies. Constellation scientists showed rapid, potent and dose-dependent suppression of MYC gene expression using inhibitors of BET bromodomains, a family of proteins involved in regulating gene transcription. By inhibiting the binding of BET bromodomains to chromatin, researchers were able to suppress the transcription of selected genes involved in growth control, thereby blocking proliferation and inducing the death of cancer cells.