About Constellation Pharmaceuticals

Constellation Pharmaceuticals leverages insights from the rapidly expanding field of epigenetics to discover and develop small molecule therapeutics for the treatment of cancer, inflammatory/immunologic disorders and other diseases.

Constellation Pharmaceuticals was founded in 2008 by academic leaders in the field and has assembled a team of seasoned scientific, medical, and business leaders to accomplish its goal of translating stellar science into breakthrough medicines. The company seamlessly integrates a unique target validation platform, expertise in structural biology, automated screening technologies, proprietary biochemical, cellular, and biophysical assays, medicinal chemistry capabilities, and experience in clinical drug development.

The field of epigenetics has demonstrated the importance of chromatin-associated proteins (regulators) that add, remove or recognize various chemical modifications (or marks) to specific sites on chromatin. These marks play a key role in determining whether a gene is on or off. Epigenetic regulators are often referred to as writers (add modifications), erasers (remove modifications) and readers (bind to chromatin).

Constellation Epigenetics Platform

Illustration of how various chromatin regulatory mechanisms (multiple classes of reader, writer and eraser proteins) impact chromatin structure to alter access to DNA

Research at Constellation and by others has shown that abnormal epigenetic regulation of gene expression contributes to many different diseases, including cancer. Constellation’s innovative product discovery engine targets both the enzymes that modify the dynamic structure of chromatin (writers and erasers) and other proteins that interact with chromatin (readers) to selectively manipulate gene expression in cancer cells, immune cells and the tumor microenvironment.

Restoration of normal gene expression through highly selective and specific inhibitors of chromatin-modulating proteins promises to be a powerful avenue for the development of important new medicines.

Modulation of Chromatin

Modulation of chromatin regulatory pathways by small molecules that target chromatin writer, reader and eraser proteins alter transcriptional programs that cancer cells depend on

Constellation’s fully integrated drug discovery and development platform is creating a robust pipeline of programs across the writer, eraser, and reader classes of epigenetic targets to develop new drugs in oncology