Drug development in the field of epigenetics is directed towards the identification of small molecules that inhibit the activities of proteins (epigenetic regulators) that add, remove or recognize various chemical modifications (or marks) to specific sites on DNA or chromosomal proteins. 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). Research at Constellation and by others has shown that abnormal epigenetic regulation contributes to many different diseases.
Constellation’s research is focused on each of the major pillars of epigenetic regulation – chromatin writers, erasers, and readers. Each of these classes of proteins provides a rich collection of targets with strong disease associations. Because of their importance we have developed drug discovery platforms in all three classes of proteins to identify novel small molecules that can modulate their activities. Each platform is now delivering compelling drug candidates moving toward clinical development. Constellation’s lead programs target the BET family of bromodomain-containing proteins and the histone methyltransferase, EZH2 – important drivers in disease. Dedicated to developing novel treatments based on additional epigenetic targets, Constellation has established a groundbreaking strategic alliance with Genentech to broadly evaluate these writers, eraser and readers for their potential therapeutic value. Both companies have dedicated a significant portion of their internal research and development capabilities to the advancement of this collaboration.
A sense of optimism and determination is an integral part of the spirit at Constellation. Each member of our team is committed to addressing the unmet medical needs of patients and to instilling integrity in everything we do. We are passionate about our work, strive for scientific breakthroughs, and view each day as an opportunity to educate and learn from each other. We work and play hard. Whether it's a charity bike race, family fun or getting together after work, we enjoy our colleagues' company outside of the labs and meeting rooms. We believe that the key to a successful company is maintaining a high-performing group of passionate, challenged, appreciated, and rewarded employees.
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The bromodomain and extra-terminal inhibitor CPI203 enhances the antiproliferative effects of rapamycin on human neuroendocrine tumors
Synergistic antitumor activity of lenalidomide with the BET bromodomain inhibitor CPI203 in bortezomib-resistant mantle cell lymphoma
EZH2 Inhibitor Efficacy in Non-Hodgkin’s Lymphoma Does Not Require Suppression of H3K27 Monomethylation